Title of Invention

TOPICAL COMPOSITION AND METHOD OF MANUFACTURING THE COMPOSITION FOR TREATING ACNE AND ROSACEA WITH GALVANIC GENERATED ELECTRICITY

Abstract (54) Title: METHODS OF TRATING ACNE AND ROSACEA WITH GALVANIC GENERATED ELECTRICITY (57) Abstract:
Full Text WO2005/004982 PCT/US2004/020271
METHODS OF THEATIHG ACNE AND ROSACKA
WITH GALVANIC GEHEEATED ELECTRICITY
CROSS REFERENCE TO RELATED APPLICATIONS
This is a continuation-in-part of co-pending
application Serial Mo. 10/685,282, filed on Oct. 14, 2003,
which a continuation-in-part of copending application
Serial No. 10/609,727, filed on June 30, 2003, which are
hereby incorporated by reference in its entirety.
BACKGROUND OF THE INVEHTION
Usirtg a galvanic couple as the power source in
ionrtophoresis device is well known in the art. See e.g.,
U.S. Patent Nos. 5,147,297, 5,l62,043, 5,298,017,
5,326,341, 5,405,317, 5,635,037, 6,584,349, 6,421,561 and
6, 653, 014. Typical materials from which a galvanic couple
is made includes a zinc donor electrode and a. silver
chloride counter electrode. Such a. combination produces an
electric potential o* about one volt. Such a galvanic
couple powered iont-ophoreais system, absent some
COTNtrolling means, activates automatically when body
tissue and/or fluids form a complete circuit with the
system to generate the electricity.
SURFACE OF THE INVENTION
In one aspact, the present invention features a
method of treating acne, rosaces, and/or wounds and/or
reducing the appearance of pigmentation by applying
electricity to a barrier membrane in need of such
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treatment,wherein the electricity is geneisied by a first
conductive electrode in electric communication with a
second conductive electrode, wherein both, the first
coniuctive electrode and the second conductive electrode
are in ionic communication with the barrier membrane,
wherein the difference of the standard potentials of the
first conductive electrode and the second conductive
electrode is at least 0.2 V and wherein the electrons that
pass between the first conductive electrode and the second
conductive electrode are generated as a result of such
difference of the standard potentials,
In another aspect, the present invention features a
method of promoting a product including a topical carrier,
a first conductive electrode in the form of a particulate,
and a second composition comprising second conductive
electrode in the form of a particulate wherein the
differsnce of the standard potentials of the first
conductive electrode and the second conductive electrode
is at least 0-2 V, such method includinig promoting the
topical application of such composition for the treatment
of pene, rosaces, and/or wounds, and/or reducing the
appearance of pigmentation.
In another aspect, the present invention features a
method of administering an active agent to a human barrier
membrane by applying to the membrane a device including a
housing having the barrier membrane contacting surface, a
first conductive electrode, a second conductive electrode.,
and a carrier containing the active agent, wherein the
first conductive electrode ia in electric communication
with the second conductive electrode, wherein the first
conductive electrode and the second conductive electrode
are in ionic communication with the carrier, and wherein
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the carrier is in communication with the barrier membrane
through the barrier membrane contacting surface, wherein
the difference of ths standard potentials of the first
conductive electrode and the second conductive electrode
is at least D.R. v and wherein the electrons that pass
between the first conductive electrode and the second
conductive electrode are generated as a result of such
difference of the standard potentials.
In another aspect, the present invention features a
method of administering an active agent to a human, barrier
membrane by topically applying a composition to such
meirbrane, the composition including the active agent, a
first conductive electrode in the form of a particulate
and a second conductive electrode in the form of a
particalate, wherein the difference of the standard
potentials of the first conductive electrode and the
second conductive electrode is at least 0.2 V.
Other features and advantages of the present
invention will be apparent from the detailed description
of the invention and from the claims.
BRIEF DESCRIPTION OF THE DRAWINGS
FIG- 1 is a cross-sectional view of one embodiment oF
thE galvanic couple powered device suitable for practicing
the invention. The conductive alectrodes l20 and 240 are
connected respectively by the lead wires 110 and 210 to
electrically insulated connecting wire 350 located, at the
back of the device 500.
FIG. 2 is a cross-sectional view of one embodiment of
the galvanic couple powered device suitable for practicing
the invention. The conductive electrodes 140 and 240 are
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connected respectively by the lead wires 110 and. 210 to
electrically insulated connecting wire 350 embedded in the
cairier layer 120 of the device 500.
FIG. 3 is a Cross-sectional view of one embodiment of
end galvanic couple powered device suitable for practicing
the invention. The conductive electrodes 140 and 240 are
cauiected respectively by Lhe lead wires 110 and 210 to
electrically insulated connecting wire 35 0 embedded in the
carrier layer 120.
FIG. 4 is a cross-sectional view of one embodiment of
the galvanic couple powered device suitable lor practicing
the invention. The conductive electrodes 140 and 240 are
in electric communication with each other by direct
cortnection. The two conductive electrodes forms a galvanic
couple which is in contact with the carrier layer 120.
FIG. 5 is a cross-sectional view of one embodiment in
aciordacce with the invention. The device 800 contains two
electrode assemblies 200 and 600.
FIG. 6 is a top view of one embodiment in accordance
with the invention showing the conductive electrodes 140
and 240 connected by electrically insulated connecting
wire 350 embedded in the carrier layer 120. The conductive
electrodes 14O and 240 are arranged in an inter-digitated
configuration.
FIG. 7 is a top view ot one embodiment in accordance
with the invention showing the conductive electrodes 140
and 240 connected by electrically insulated connecting
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wire 350 embedded in the carrier layer 120. The conductive
electrodes 140 and 240 are arranged in a concentric
configuration .
FIG. 3 is a top view of one embodiment in accordance
with the invention showing a plurality of sets of
conductive; electrodea 140 and 240 connected to each other
by connecting wire 350 to form a plurality of galvanic
couple power sources, which are in contact with the
carrier layer 120. The conductive electrodes 140 and 240
are arranged, in a parallel configuration.
FIG. 9 is a top view of one embodiment in accordance
with the invention showing a plurality of sees of
conductive electrodes 140 and 240 connected no each other
by a direct physical contact at intersections 370 to form
a plurality of galvanic couple power sources, which are in
contact with the carrier layer 120. The conductive
electrodes 140 and 240 are arranged in a perpendicular
corif iy uration.
FIG. 10 ig a top view of one embodiment in accordance
with the invention showing the conductive electrodes 140
ana 3A0 eownected by electrically insulated cortnecting
wire 340 embadded in the carrier layer 120.
FIG, 11 is a top view of one embodiment in accordance
witih the invention showing the conductive electrodes 140
and 240 embedded in the carrier layer 120.
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DETAILED DESCRIPTION OF THE INVENTION
It is believed that, one skilled in the art can, based
upon the description herein, utilize the present invention
to its fullest extent . The following specific embodiments
are to be construed as metely illustrative, and; not
limitative of the remainder of the disclosure in any way
whatsoever.
Unless defined, otherwise, all technical and
scientific terms used herein have the same meaning as
coramaoly understood by one of ordinary skill in the art to
which the invention belongs. Also, all publications,
patent applications, patents, and other references
mentioned herein are incorporated by reference. Unless
otherwise indicated, a percentage refers to a percentage
by weight (i.e. (W/W)
What is meant by a "product" is a product containing
the device in finished packaged form. In one embodiment,
the product contains instruct ions directing the user to
apply the device to the barrier membrane [e.g., to treat a
akin condition) . Such instructions may be printed put the
device, label insert, or on any additional packaging.
In one aspect, the present invention features
promoting a device of the present invention for its
intended. use What is meant by "promoting" is promoting,
advertising or marketing. Examples of promoting include,
but are not limited to, written, visual, or verbal
statements made on the product or in stores, magazines,
newspaper, radio, television, internet, and the like.
As used herein, "pharmaceutically-acceptable" means
that the ingredients which the terra describes are suitable
for use in contact with the barrier membrane (e.g., the
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skin or mucosa) without undue toxicity, incompatibility,
instability, irtitation, allergic- response, and the like.
As used herein, "safe and effective amount" meanc an
amount of the ingredient or of the composition sufficient
to provide nhe desired benefit at a desired level, but low
enough to avoid serious side effects. The safe and
effective amount of the ingredient or composition will
vary with the area being treated, the age and skin type of
the end user, the duration and nature of the treatment,
the specific ingredient or composition employed, the
particular pharmaceutically-acceptable carrier utilized,
ana like lactors.
As used herein. The term "treatment" means the
treatment (e.g., alleviation or elimination of symptoms
and/or cure) and/or prevention or inhibition of the
condition (e.g., a skin condition} . What is meant by a
"skin condition" is a derntatological disease or disorder
Concluding, but not limited, acne, rosaces, or skin
infections} or skin characteristic [including, but not
limited to, pigmentation, hair growth regulation, skin
teixture, skin tirtmess, skin elasticity, akin vasculature,
dark circles, cellulite, sebum regulation, and skin
shine) . Examples of skin infections include, but are not
limited to, those due to susceptible pathogens such, as
acne, rosaces, impetigo, folliculitia, funmculosis,
ecthyma, eczema, psoriasis, atopia dermatitis, harper,
epldermolysis bulloss, icthyosie, and infected traumatic
lesions (e.g., ulcers, minor burns, truts, airafiiona,
lacerations, wounds, biopsy sites, surgical incisions and
insect bites).
The present invention relates to a device for the
delivery of electricity (e.g., to induce a desirable
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biological response) and/or an active agenx into a barrier
membrane. In one embodiment, the device of the present
indention is a self-contained device containing at least a
pair of two dissimilar conductive electrodes in electric
communication as a power source. By "electric
communication" is meant that electrons can directly pass
between the clements of the device (e.g., between the
conductive electrode of the device). In one embodiment,
the two conductive electrodes are in electric
communication via direct contact with each other.
By "ionic communication" it meant that electrons can
pass between the elements (e.g., the conductive electrode,
the carrier and/or the conductive electrode and the skin)
through the migration of ions as "electron inovers" in
contact with such elements (e.g., electrons pass between
the conductive electrode and the akin via ionic transport
of electrolytes (e.g., in the carrier) in contact with the
cobductive elect.rode and the akin).
In one embodiment, the two conductive electrodes are
in ionic communication with the carrier containing an
elsctrolyte (e.g., ions of one or more electrolytes in the
carrier are in contact with the conductive electrode) and
the carrier is in ionic communication with the skin. This
electrode configuration differs from those in conventional
iontophoresis devices in which each conductive electrode
is in contact with a separate carrier (e.g., each
electrodc is contained in a separate compartment and
affixed to the skin with electric insulation between them
in order that all the electric current travels through the
skin to complete the electric circuit). An advantage of
such an embodiment of the present invention, includes the
capability of delivering simultaneously active agents of
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opposite charges from the same carrier into substantially
the same skin site under the conductive electrodes.
Another advantage is that the devices of the present
invention are much easier to manufacture than conventional
iontophoreais devices, and therefore, are enable
substantial cost-savings.
The device contains a. barrier membrane contacting
surface (e.g., a skin contacting surface) that is applied,
to the membrane {e.g., applied by the user to the user's
skin) . Ths device ia arranged such that carrier is in
communication with the barrier membrane contacting surface
{e.g., such that electricity and/or the active agent may
be administered from the carrier into the barrier
membrane). In one embodiment, the carrier is the barrier
membrane contacting surface (e.g., the carrier is a
hydrogel) . In one embodiment, the device contains a light
etritting diode such that light from the light emitting
diode is in communication with the barrier membrane
contacting surface {e.g., such that the light may be
administered to the barrier membrane .
In one embodiment, the device of the present
invention delivers an active agent into the barrier
membrane. The active agents to be delivered by the device
of the present invention include active agents either
initially incorporated in the carrier or electirochemically
generated by the elect tic current passing from a
conductive electrode through the carrier during use. What
is meant by "electrochemically generated" is that the
chemical specie is created as a result of an
e lectrochemical reaction resulting from electric current
flowing through an electrode, such a chemica1 specie
released from a reactive electrode (e.g., an
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electrochemically generated zinc ion) , a chemical specie
electrochemically generated on the surface of an inert
electrode, or a chemical specie that is a subsequent
reaction product of such eletrochemically generabed
spiscie.
Galvanic Couple
The device/composition of the present invention has
a galvanic couple as its power source, wherein the
electrons that pass between the first conductive electrode
and the second conductive electrode are generated as a
result of the difference of the standard potentials
between the electrodes (e.g., the ele-ctriclty is not
generated by an external battery or other power source
such as an AC power source}. Examples of such galvanic
couples include, but are not limited to, zinc-copper,
zinc-copoer/copcer halide, zinc-copper/copper oxide,
magnesium- copper, magnesium-copper/copper ha.lide, zinc-
silver, zine-silver/silver oxide, zinc-silver/silvar
hal ide, zinc -silver/ silver chloride, zinc -silver/ silver
bromide, zinc-silver/silver iodide, zine-sliver/silver
fluoride, zine-gold, magnesium-gold, aluminum-gold,
magnesium-silver, magnesium-silver/silver oxide,
mag nesium-silver/silver halide, magnesium- silver/silver
chloride, mignesium-silver/si1ver bromida, magnesium-
silver/silver iodide, magnesium-silver/silver fluoride,
magnesium-gold, aluminum-copper, aluminum-silver,
aluminun-silver/silver oxide, aluminum- silver /silver
halide, aluminum-silver/silver chloride, aluminum-
silver/silver bromide, aluminum-silver/silver iodide,
aluminum-silver/silver fluoride, copper-silver/silver
halide, copper-silver/silver chloride, copper-
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silvrer/silver bromide, copper-silver/silver iodide,
copper-silver/silver fluoride, iron-copper, iron-
copper/copper oxide, iron-crupper/ copper halide, iron-
silver, iron.-silver/silver oxide , iron-Silver/silver
halide, iron-silver/silver chloride, iron-silver/silver
bronide, iron-silver/silver iodide, iron-silver/silver
flunride, iron-gold, iron-conductive carbon, zinc-
coniuctive carbon, copper-conductive carbon, magnesium-
coniuctive carbon, and aluminum-carbon. The materials
whih serve to make up the galvanic couple may also serve
as the conductive electrodes of the device,e.g.zinc as
the conductive anode and silver/silver chloride as the
conductive cathode or zinc as the conductive anode and
copper as the conductive cathode. The metals serve as the
galvanic couple and conductive electrodes may also be
allays. Non-limiting examples of the alloys include alloys
of zinc, copper, a1uminum, magnesium as anode materials,
and alloys of silver, copper, gold as cathode materials.
In one embodiment, the materials that make up the
galvanic couple have a standard potential difference equal
to or greater than about 0.1 volts, such as gireater than
about 0.2 voltg such as greater than about 0.5 volts. In
one embodiment, the materials that make up the galvanic
couple have a standard potential difference equal to or
less than about 3 volts.
In one embodiment, the device or composition of the
present invention generates and/or is capable of
generating current into the barrier membrane of from about
1 nano-A/cm2 to about 4OO micro-A/cm2 of electricity such
as from about 100 A./cm2 to about 50 micro A/cm2 .
In one embodiment, one of the conductive electrodes
is in the form of a metal sheet, a metal wire, or a metal
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coated on a aubscrate, and the other conduceive electrode
is attached or deposited to the first conductive
electrode. In a further embodiment, the metal sheet is
perforated. In one embodiment, such perroraced metal
sheet 13 in the form of a mesh such as a mesh of zinc,
magnesium, aluminum, copper, or their alloys thereof. In
one embodiment, the second conductive electsrode is in the
form a fabric coated with a metal, and its oxide, halide,
and sulfide, such as a fabric coated with silver,
silver/silver oxide, silver/silver halide, zinc,
magnesium, copper, copper/copper halide, copper/copper
oxide. In another embodiment, the second conductive
electrode is deposited to the first conductive electrode
by chemical or electrochemical deposition such as
electrodes plating for chemical deposition and
electroplating for electrochemical deposition a a known in
the art, In a further embodiment, the second conductive
electrode is deposited to the first conductive electrode
by physical deposition, such as spray coating, plasma
coating, conductive ink coating, screen printing dip
coating or vacuum deposition.
In one embodiment, the device is a single compartment
treatment device. What is meant by a "single compartment
treatment device" is a device in which both conductive
electrodes of the device; are in contact with the same
carrier, Examples of; such devices are shown in Figures 1-
4 and 6-11-
carrier
The carrier of the present invention is a liquid
(e.fg., a solution, a suspension, or an emulsion which may
be immobilized within an absorbent material such ae gauze
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or non-wpon pad , a semi -solid (e.g. , a gel, a cream, a
lotion, miroeitiiilEion, or hydrogel) , or a solid {e.g., a
3 yapbillzed composition containing active agents, which
may be reconstituted by adding s liquid prior to use) that
during use is capable of conducting electricity from a
conducting electrode {e.g, the carrier contains one or
mora electrolytes, organic solvents, and water . In one
embodiment, the carriar (e.g, a liquid or semi-solid) is
added to the device by the user prior to applying the
device to the barrier membrane.
Examples of electrolytes include, but are not limited
to, pharmaceutically acceptable organic and. organic salts
and buffers. Examples of salts include, but are not
limited to, chloride salts (such as sodium chloride,
potassium chloride, lithium chloride; calcium chloride,
strontium chloride, magnesium chloride or other chloride
salts), as well as salts of sodium, potassium, lithium,
calcium, magnesium, strontium, fluoride, iodide, bromide.
Examples of buffers include, but are not limited to,
phosphates, citrates, acetates, lactatea, and borates.
In one embodiment, the electrolyte is an active
agent, or becomes an active agent after the passage of the
electric curraat through, the carrier. Examples of such
electrolyte-active agents include, but are not limited to,
eaicylic acid, salicylates, and other weak acid OR WEAK
base active agents.
In one embodiment, the carrier contains water. In a
further embodiment, the carrier may also contain one or
MORE organic solvents. Examples of organic solvents
include, but are not limited to, dimethyl isosorbide
isopropylrrnristate; surfactants of cat ionic, anionic and
non-ionic nature; vegetable oils, mineral oils; waxes;
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gums, synthetic and nacutal gelling agents, alkanols;
glycols; and polyols.
Examples of glycols include, but are not limited to,
glycerin, propylene glycol, butylene glycol, penta1ene
glycol, hexylene glycol, polyethylene glycol,
polypropylene glycol, diethylene glycol, triethylene
glycol, glyoerol, and hexaetrol, and copolymers, or
mixtures thereof- Examplea of alkanols include, but are
not limited Co, those having from about 2 carbon atoms to
about 3.2 carbon atoms (e,g. from about 2 carbon atoms to
about 4 carbon atoms), such as isopropanol and ethanol.
Examples of polyola include, but are not limited, to, those
naving from about 2 carbon atoms to about is carbon atoms
(e.g., from about 2 carbon atoms to about 10 carlaon atoms)
such as prapylsne glycol.
The organic solvents may be present in the carrier in
an amount, based upon the total weight of the carrier, of
from about 1 percent to about 90 percent {e.g., from about
5 percent to about 50 parcent). Water may be present in
the carrier (prior to use) in an amount, based upon the
total weight of the carrier, of from about 5 percent to
about 95 percent (e.g., frotn about 50 percent to about 90
percent).
The carrier may also contain preservatives (such as
cresol, chloracresal, benzyl alcohol, methyl p-
hydroxylbenzoeats, propyl p-hydroxybensoate, phenol,
thimerosal, bensalkoniuni chloride, benzethonium chloride,
and phenylmer curie nitrate) , stabilizing agents a or
antioxidanta (such as ascorbic acid, ascorbic acid estars,
butyihydroxy anieole, butylhydroxy toluene, cysteine, N-
aretylcysteine, sodium bisulfite, sodium metabiaulfite,
sodium formaldehydesulfoxylate, acetone sodium bisulfite,
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tocopherols, and nordhydroguaiarecie acid) ; chelatins
agents (such as ethyl esiedi ami netietrgacetic acid and its
salts}, buffes (such as acetic acid, citric acid,
phosphoric acid, glufcamic acid, and salts thereof) and
tonicity adjusting agents (such as sodium chloride, sodium
sulfate, dextrose and glycerin) .
In one embodiment, the carrier may also contain a
suspending material and/or- a fluid-absorbing material,
[e.g., for physically stabilising the ingredients of the
carrier) . Examples of suspending materials include, but
are not limited to cotton-based gauze; non-woven pads
made of rayon or a mixture of rayon, polyester and/or
other polymer fibers, open-cell foam and sponge-like
materials contained of polyurethane, polyester and/or
other polymers and cross-linked and noncross-linked
galling materials, such as polyacrylamide, polyvinyl
alcohol, gelatin, hydroxymethylcellulose,
hydrcsxyethylcellulose, hydroxypropylcllulose,
methyl cellulose, and carboxymethyieellulase .
Examples of fluid-absorbing materials include, but
are not limited to; cross-linked and (ion-cross-linked
polymers; swellable polymers such aa water-swollen
cellulose derivatives (e,g., methylcellulose (MC),
hydroxyethyl methyl cellulose (HEMA.) , liydroxypropyl
methylecellulose (HPMC) , ethylhydroxyethy 1 celluloae
CEHEC) , hydi-o-iy ethyl cellulose (KEC) ,
hydroxypropylcellulose (HPC] and carbonethlcellulose
{CMC) and thsir salts); polyvinyl alcohol (PVA);
polyvinylpyrrolidone (PVP); polyethylene oxide (PEO);
polymers prepared by monomers such as hydroxyethyl
methacrylate {HEMA) , hydroxyethoxyethyl emthacrylste
(HEEMA) , hydroxydiethoxyethl methscrylate (HDEEMA) ,
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imethyoxyethyl methacrylate (MEMA) , methoxyethoxyechyl
imsth aery late (MEEMA) , methyldiethoxyethyl methacrylate
(MDEEMA) , ethylene glycol dimethacrrylate (EGDMA), n-vinyl-
2pyrrolidone (NVF) , methacrylic acid (MA) and vinyl
acetace (VAC) ; poly cry 1 amide; gel ah in, gums and
polysacchar ides such as gum arable, gum karaya, gum
tiragacanth, guar gum, gum benzoin, and algiriic acid and
their salts; polyethylene glycol (PEG) , polypropylene
giycol (PPG); and clays or other swellable minerals such
as bentonite and montmori11onite. The amount of fluid
abaorfaable material in the carrier may range from about
0.1% no about 95%, by weight, such as from about 1% to
about 20%, by weight, of the carrier.
Another embodiment of the present invention is
directed to pairing one or more inert conductive
electrodes in order to electrochemically generate
oxidizing or reducing agents from electiochinically
reactive materials in situ in the cairier. such oxidising
or reducing agents can be used as active agents to treat
barrier membrane conditions.
Examples of the electrochemically reactive materials
in the carrier according to the present invention include,
but are not limited to, water and compounds containing the
elements selected from the Periodic Table of the Elements
VIB and VIIB (such as oxygen, sulfur, fluorine, chlorine,
bromine, and iodine).
In one embodiment, the reactive material reacts with
the inert anode to form an oxidizing agent. Examples of
isuch a reactive material includes, but is not limited to,
the ions OH-, Cl-, I-, Br-, so32- and HCO3-, The present
device, thus, enables to generation of oxidising agents,
such as nascent oxygen (e.g., singlet oxygen), chlorine
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and chlorine dioxide gases, which are difficult to
formulate in a conventional topical product.
In one embodiment; the reactive mecsrial reacts with
the inert cathode to form a reducing agent. Examples of
such a reactive material includes, but is not limited to,
oxidized or bisulfide forms of thio-compounds with one or
more aulfhydryl functional groups, thio-containing amino
acids and their salts or eaters, and sulfides. Examples of
such thio-compounds include, but are not limited to;
thioglycolic acid and its salta, such as thioglycolates of
calcium, sodium, strontium, pocassium, ammonium, lithium,
magnesium, and other metal salts; thioethylene glycol;
thioglycexol; thioetharasl; thioactic acid; and
thioealicylic acid; and. thsir salts. Examples of the thio-
containing antino acids include, but are not limited to, L-
cysteine, D-cysteine, DL-cyeteine, N-acetyl-L- cyatsijne,
DL-horaocysteine, L-cysteine methyl ester, L-cysteine ethyl
ester, Pf- cairbamoyi cysneine, glut athione , and cystemine.
Examples of aulfides, include but are not limited to,
calcium, sodium, potassium, lithium and strontium sulfides
and glutathione disulfide. The inert cathode converts the
aforementioned reactive oxidized or disulfide form of a
sulfur-containing compound to 3 thio-containing compound,
or a gulfydryl-containing compound. Examples of such, a
conversion is the conversion of cystine to cystsine and
the conversion of the oxidized form of glutatnione to
glutathdone.
In one efntaodiment, the concentration of the reactive
material in the carriar may range from about 0.01% to
about 25%, by weight, such as from about 0.1% to about
10%, by weight, of the carrier. The pH value of the
carrier may range from about pH 1-5 to about pH 9,
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preferably from pH 2 to pH 7, and most preferably from
about pH 3 to pH 5.
In one embodiment, the carrier contains an adhesive.
The adesive is used, to affix the device to the barrier
membrane. Examples at hydrophobia adhesivea include, but
are not limited tO, silicones, polyisobutylenes and
derivatives thereof, acrylics, natural rubbsra, and
combinations thereof. Examples of silicons adhesives
include, but are not limited to, Dow Corning 355 available
from Dow coming of Midland, MI; Dow Corringo X7-2920; Dow
Corning X7-2960; and GE 6574 available from General
Electric Company of WaterCord, NY. Examples of gcrylic
adhesives include, but are not limited to, vinyl (D
acetate-aerylate) multipolymers auch aa Gelva 7371,
available from Monsanto Company of St. Louis, MO; Gelvao
7881; Gelva 2943; and 1-780 medical grade adhesive
available from Avery Demison of Painesville, OH. Examples
of hydrophilic adhesives include, but are not limited to,
gum papaya and other natural gums, MC, HEMA., HPMC, EHEC,
HEC, HPG, CMC, PVA, PVP, PBO, HEMA, HEEMA, HDEEMA, MEHR,
MBEMA, MDEEMA, EGDMA, NVP MA, VAC, polyerylamide.
getatine, gum arabic, gum kargya, gum tragacanth, guar
gum, gum benzoin, and alginic acid and their salts,
polyethylene glycol [PEG), and polypropylene glycol (PPG),
In one emboditnent, the concent ration of the adhesive
in the carrier may range from about 0.1% to about 95%, by
weight, such as from about 1% to about 20%, by iveigiit, of
the carrier.
Electrodes
The conductive electrodes of the present invention
may be a reactive conductive electrodes or inert
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WO2005/004982 PCT/US2004/020271
conductive electrodes. What is meant by a "reactive
conductive electrode" is that the conductive electrode
itself goes through a change in its chemical composition
during the electrode chemical reactions occurring with the
electric current passing through the electrode during the
process, In one embodiment, the reactive conductive
electrade is an anode made of reaqtivs materials such as a
pure metal or a metal alloy including, but not limited to,
zinc, aluminum, copper, magnesium, manganese, silver,
titanium,, tin, iron, and alloys thereof. The materials
which serve to make up the galvanic couple described
earlier may also serve as the reactive conductive
electrode. Upon passage of an electric current, metal ions
such as zinc, copper, magnesium, manganese and/or aluminum
cations are released from the anode into the carrier and
delivered into the barrier membrane. Such ions may serve
therapeutic benefits such as anti-microbial effects,
immunologic modulation, enzymatic regulation, and/or anti-
inflammatory effects.
In one embodiment, the reactive conductive electrode
is made of reactive materials such as metal halides (e.g.,
silver-silver chloride (Ag/AgCl), silver-silver bromide,
and silver-silver iodide). In this case, the primary
electrochemical reaction at the cathode surface is
conversion of solid silver halide to metallic silver with
little unwanted consumption of the oxidising agents
generated by the anode. The released halide ions may be
subsequently oxidised to oxizing agsnts, such as
chloride ions to chlorine (Cl2) , hypoctiloroua acid (HC1O),
and hypochlorite ions {C1CT} , and iodide ions to iodine.
What is meant by an "inert conductive electrode" is
that the conductive electrode itself does not go through a
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WO2005/004982 PCT/US2004/020271
change in its chemical composition. In one embodiment,
the anode is made of an inert conductive electrode, so
that the electrochemical croceas al the surface of the
anode generates oxidizing agents such as rscent oxygen
(e.g., by electrolysis of water) and/or chlorine-
containing oxidizing agents such as chloride,
hypochlorite, chlorate and perchlorate, and chlorine
dioxide. Nascent oxygen is an oxidizing agent thau is
inhibitive to P. acnes, and chlorine-containing oxidizing
agents are patent antimicrobial agent with bacteriocidal
activity.
In one embodiment.,the conductive electrode is made
of, or coated on the surface with, an inert materials such
as noble metals {e.g., gold, platinum, or gold-coated
conductive metals), conductive carbon (e.g., glassy carbon
or graphite), carbon-enibedded polymers (e.g., carbon
silicons rubbers) conductive carbon polymree form or
sponge, silver halide-coated silver (e.g., silver
chloride-coated silver, silver bromide-ceased silver, and
silver iodide-coacad silver), and crortosive resistant
alloys.
In one embodiment, the anode of the device, serving
as the conductive electrode as well as a part of the
galvanic couple power source, is made of aforementioned
reactivs conduotivs oxidisable metala such as sine,
calcium, magnesium, aluminium, iron, tin, copper, or alloys
thereof, while the cathode, also serving as the conductive
Slectrodte as well as a part of the galvanic couple power
source, is made of the aforementioned reactive reducible
Conductive materials each as a more chemically stable
metal and its metal halides, oxidet, sulfide or other
metal salts, such as silver and silver halides (e.g.,
20

WO2005/004982 PCT/US2004/020271
silver chloride, silver bromide, silver iodide, silver,
fluoride) , silver oxide, silver sulfitife. in one
embodiment, the reducible conductive material is in direct
contact; with a good electric conductor, such as a thin
layer of silver chloride, silver oxide, or silver sulfide
over metallic silver; silver chloride powder with a binder
(e.g., silver cihloxide ink) ; and/or silver chloride powder
mixed, with silver or conductive carbon powder held
together by a binder in a matrix form (e.g. , silver-silver
chloride ink and silver chloride-carbon ink) .
In another embodiment, the anode of the device in the
present invention is made of aforementioned reactive
Conductive oxidizeble metals while the cathode is made of
aforementioned more chemically stable electrode materials
such as conductive carbon, metallic silver, gold or
platinum, or a powder mixture of conductive carbon and the
noble metal in a rastrix fount as disclosed in U.S. Patent
No. 5,l62,043.
In one embodiment, the device of the present
invention enables the targeted delivery of beneficial sine
through hair follicles to the piloscbacaous unit {i.e. a
sebaceous gland and the associated hair follicle} to treat
acne or rosacea. Zinc is an essential metal to the human
body because it participates in various biological
actrities in the body (a.g.,the body of 3. 70-Kg person
contains about 2.3 grams of sine). It is known that the
lack of zinc in the body may lead to skin diseases such as
acne.
In another embodiment, the deviee of the present
invention enables the targeted delivery of other
beneficial metals into the hair follicles and the
piloseboaceous glands by using an anode made of sine alloy
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WO2005/004982 PCT/US2004/020271
containing small quantities of other beneficial metals.
Such beneficial metals includes, without limitation,
certain metals essential to the human body such asiron,
copper, magnesium, manganese, calcium, potatssium,
aluminum, and selenium. As the zinc alloy anode oxidizes,
it releases into the carrier zine ions and other
beneficial metala in the sine alloy, which ingredients
subsequently migrate into the hair follicles under the
applied electric potential over the skin. In one
embodiment, the content of the sine alloy in the anode in
greater than about 50% by weight, such, as greater than 90%
by weight.
In one embodiment, the ratio of the conductance
measured between the first conductive and second
conductive electrode of (i) the carrier and (ii) the skin
hydrated with such carrier (wherein substantially all of
the cuurrent passes between the electrodes through the
skin) is in a range from about 10 000:1 to about 1:100. In
other words, the electric current distribution between
Icarrier and Iskin is such that the value of Icarrier/Iskin is
between about 10,000 and about 0.01. Icarrier is the portion
of the total current going through the device (Itotal) that
only passes through the carrier layer between the anode
and cathode without traveling through the skin, whereas
Iskin is the portion of Itotal that passes through the skin,
namely, Itotal = Icarrier + Iskin.
Decreasing the ratio of the conductance of the
carrier to the conductance of the skin will result in a
greater percentage of current passags through the skin,
thereby enhancing iontophoretic delivery of any active
agents being so delivered into the skin. Decreasing the
conductivity of the carrier can nonexclusively be
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WO2005/004982 PCT/US2004/020271
accomplished by adding less condvctive materials to the
carrier. Examples of such less conductive materials
include, but are not limited to, oils such as silicons or
hydrocarbon oils, air pockets such as air bubbles or air
pockets in a serai-solid carrier, or polymer or clay beads.
In one embodiment where the primary intention is to
electroeheinieally generate species in the carrier, the
value of Icarrier / Iskin is between about 10,000 and about 1.
in another embodiment where the primary intention is to
deliver electricity and/or active agents into the skin,
the value of Icarrier/ Iskin is between about 10 and about
1.01. Adjustmnent of the value of Icarrier / Iskin for a
particular application can also be achieved by changing
the distance between the first and the second electrode,
or the distance between the two conductive electrode and
the skin. For example, as the distance between the two
conductive electrode decreases, the conductance measured
between the two electrode increases and so is the Icareer.
leading to a increased value of lcarrier / Iskin. On the other
hand, if the distance between the two conductive
electreaties and the skin increases the Iskin increases,
leading to decreased value of Icarrier / Iskin.
Active Agents
In out embodiment, the carrier contains one or mote
active agents. What is meant by an "active agent" is a
compound (e.g., a synthetic compound or a compound
isolated from a natural source) that has a cosmetic or
therapeutic; effect on the barrier membrane and the
surrouitdina, tissues (e.g., a material capable of exerting
a biological effect on a human body) such as therapeutic
drugs, including, but not limited to, organic and
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WO2005/004982 PCT/US2004/020271
macromolecular compounds. Examples of such therapeutic
drugs include peptides, polypeptides, proteins, and
nucleic acid, materials comprising DNA; and. nutrients.
Examples of polypeptide and protein active agents include
thyrotrap in-releasing hormone (TRH), vasopressin,
gonadatropin-releasing hormone (GnRH or LHRH) ,
melimotiropin-stimulating hormone (MSH) , calcitonin, growth
horraoae releasing factor (GRF), insulin, erytbropoietin
(EPO), Interferon alpha, interferon beta, oxytocin,
captopril, bradykinin, atriopeptin, cholecystokinin,
endorphins, nerve growth factor, melanocyte inhibitor-I,
gastrin antagonist, soxnafcotstia, encephalins, melatonin,
vaccines, botox (Botulinutn neurotoxins) , cyclosporin and
its derivatives (e.g. biologically active fragments or
analogs) , Other active agents include anesthetics;
analgesics (e-g., fentanyl and salts thereof such fentanyl
citrate); drugs for treating psyctkiacric disorders,
epilepsies, and migraine; drugs for stopping drug
additione and abuses; anti-inftamiatoiry agents; drugs to
treat hypertension, cardiovascular cisaaaee, gastric
acidity and ulcers; druge for hormone replacement
cherapies and cootraceptives such as estrogens and
androgens; antibiotics, antifungal a, antiviral and other
ancimiccobial agents, antineoplaatic agents,
immunosuppessive acents and imnnotimulants; and drugs
acting on blood and the blood forming argans including-
heruatopoietic agents and anticoagulants, throtnbolytics,
and antiplatslet drugs. Other active agents that can be
delivered into the body using the shear device in the
present invention include vaccines for various diseases,
such as those for iniluensa, AIDS, hepatitis, measles,
mutnps, rubella, rabies, rubella, avercella, tetanus,
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WO2005/004982 PCT/US2004/020271
hypogsmmaglobulinsmia, Rh disease, diphtheria, botulism,
snakebite, back yidow bite and other itisect bite/sting,
idiopathic throiiibccytopenic purpura (ITP) , chronic
lymphocyt i c Jeukp.nia, crtom&galoiirus (CNV) infection,
aculie renal rejection, oral polio, tuberculosis,
pertussis. Haemophilias b, Pnsumococcus, and. Staphylococcus
aureus.
In one embodiment, the carrier contains an anti-acne
and/or ant±-rosacea agent. Examples of anti-acne and
anti-roaacea agents include, but are not limited to:
retinoids such as tretinoin, isotretinoin, motretinide,
adapalene, tazarotene, azelaic acid, and retinol,
salicylic acid; benzoyl peroxide; resorcinol; sulfur;
salfacetamide; urea; antibiotics such as tetracyclirue,
clindamycin, metronidasole, and erythroraycin anti-
inflarntnatory agents such as corticosteroids (e.g.,
hyictrocortisone) , ibuprofen, naproxen, and hetprofen; and
imidazoles such as ketoconazole and elubiol; and salts and
prodrugg thereof. Other examples of anti-acne active
agents include essential oils, alpha-bisabolol,
dipotassium glycvrrhisinate, camphor, b-glucan, allantoin,
feverfew, flavonoida such as soy isoflavones, saw
palmetto, chelating agents such as EDTA, lipase inhibitors
such as silver and copper iong, hydrolyzed vegetable
proteins, inorganic ions of chloride iocliole, fluoride,
and their nonionic derivatives chlorine, iodine, fluorine,
and other valences, synthetic phospholipida and natural
phospholipids such as Arlasilk™ phospholipida CDM, SV,
EFA, PLH, and QUA. (Oniqema, ICI Group of Companies,
Wilcon, UK).
In one embodiment, the device of the present
invention contains an anti-aging agent. Examples of
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WO2005/004982 PCT/US2004/020271
suitable anti-aging agents include, but are not limited
co. inorganic sunscreens such as titanium dioxide and zinc
oxide, organic sunscreens such as octyl-methoxy
cinnatflates; retinoids; dimethylaminoathana1 (DMAE), copper
containiny peptides, vitamins such as vitamin E, vitamin
A, vitamin C, and vitamin B and vitamin salts or
derivatives such as ascorbic acid di-glucoside and vitamin
E acetate or parmitate; alpha hydrcocy acids and their
precursors such as glycolic acid, citric acid, lactic
acid, malic acid, mandelic acid, ascorbic acid, alpha-
hydroxybutyrie acid, alpha- hydroxyisobunyric acid, alpha-
hydroxyisoeaproic acid, atrrolactic acid, alpha-
hydroxyisovaleiric acid, ethyl pyruvate, galacturonic acid
glticoheptonic acid, glucoireptona 1.4-lactons , gluconie
acid, gluconolactone, glucuronic acid, glacuronolactone,
isapropyl pymvate, methyl pyiuvace, mucic acid, pyruvic
acid, saccharic acid, saccaric acid 1,4-lactone, tartoric
acid, and tartronic acid; beta hydroxy acids such as beta-
hydroxybutyric acid, beta-phcnyl-lactic acid, and beta-
phenylpyruvic acid; zinc and zinc containing compounds
such as sine oxides; and botanical extracts such as green
tea, soy, milk: thistle, algae, aloe, angelica, bitter
orange, coffee, goldthread, grapefruit, hoellen,
honeysuckle, Job's tears, lithospermum, mulberry, peony,
pueiarua, nice, and safflower and salts and prodrugs
thereof.
In. one embodiment, the carrier contains a
depigmerrtaticm agent. Examples of suitable depigmentgition
agents include, but are not limited to: soy extract; soy
isoflsvones; retinoids such as retinol; kojic acid; kojic
dipalmi tate; hydroquinone; arhucin, transexatnic acid;
vitamins such as niacin and vitpmin. C; aeelaic acid;
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WO2005/004982 PCT/US2004/020271
linoletic acid and linoleic acid; placertia; licorice, and
extracts such, as chamopiile and green tea; and galte and
prodrugs chereof.
In one embodiment, the carrier contains, a plant
extract. Rxamples of plant extracts include, but are not
limited to, feverfew, soy, glycine soja, oatmeal, what,
aloe Vera, cranberry, hasel witch, alnus, arnica, artemisia
capillaris, aeiasarum root, birch, calendula, chacnornile,
cnidium, cornEiiey, fennel, galla rhois, hawthorn,
houttuynia, hypericum, jujube, kiwi, licorice, magnolia,
olive, peppermint, philodendron, sal via, sasa albo-
marginata, natuiral isoflavonoids, soy isoflavones, and
natural easential oils.
in one embodiment, the carrier contains metals such
as metal ions, metal salts, metal complexes, fine metal
pawdexs, fine metal coated fibera and fabrics of synthetic
or natural origin, or fine metal fibers. Examples of such
metals include, but are not limited to, zinc, copper,
aluminum, gold, silver, titanium. The metal ions provide
benefits such as antimicrobial, anti-inflammatory, and/or
sebum-reduction effects. The beneficial metal ions may be
released from the metal anode as the result of an
electrochemical oxidation reaction concurrent with
electric current passage (e.g., zinc ions
electrochsmieally- generated from a zine anode).
In another embodiment, the beneficial ions may be
generated indirectly from the electrochemical reactions at
the electrode surface, sucn as the generation of hydrogen
or hydroxyl ions at an inert electrode, which subsequently
leads to a process to generate beneficial ions. For
example, a device of the present invention may contain a
power source, an inert anode (e.g., platinum, platinum
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WO2005/004982 PCT/US2004/020271
coated conductive electrode, gold, or gold-coated
conductive electrods) , a reactive cathode (e,g.,
silver/silver chloride electrode) , and an aqueous carrier
composition containing an oxide (e.g., zinc oxide
particles) among other active agents. During application
to the skin, the electrolysis of water at the inert anode
produces excess hydrogen ions which acidify the carrier
toward a lower pH value, while the electrochemical
reaction at the reactive cathode (e.g., the conversion of
silver chloride to silver ions) does not affectthe pH. As
the solution becomes more acidic, the oxide starts to
dissolve to release ions (e.g., zinc ions) for their
beneficial effects to the barrier membrane.
Other active agent a include those commonly used as
for topical treatment and in cosmetic treatment of skin
tissues, such, as topical antibiotics for wounds, topical
antifungal drugs to treat fungal infections of the skin
and nails, and antipsorianic drugs to treat psoriatic
lesions of the skin and paoriatic nails.
Examples of antifunctal drugs include but are not
limited to miconazole, econazole, ketoconazole,
sertacontisole, itraconaaole, fluconasole, voriconazole,
clioquinol, bifoconaaale, terconazole, butoconazole,
tioconazole, oxiconazole, sulconazole, saperconasole,
clotrimazole, undecylenic acid, halopieogin, butenafine,
tolnaftate, nystatin, ciclopirox olemine, terbinafirte,
amorolfine, naftifine, elubiol, griseofulvin, and their
pharmaceutically acceptable salts and prodrugs. In one
embodiment, the antifunga1 drugs are an azole, an
allylamine, or a mixture thereof.
Examples of antibiotics (or antiseptics} include but
are not limited to raupirocin, neomycin sulfate bacitracin,
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WO2005/004982 PCT/US2004/020271
as from about 0.01 percent to about 5 percent, by weight,
of the carrier.
Light Emitting Diode
In one embodiment, the device contains one or more
light emitting diodes. "Light emitting diodes (LEDS) of
certain spectrum may be incorporated into the device to
emit light to the-barrier membrane (e.g., to treat skin
conditions such as acne and rosacea) , The light emitting
diode may also provide a signal to the user indicating
that the device is operating properly.
In one embodiment,the LED is one that emits light
periodically (i.e., a blinking LED) , In a further
embodiment, such LED also modulates the current passing
chrough the barrier membrane to form a pulsatile DC
current. Such pulsatile DC current can enhance delivery of
active agents into the barrier membrane, stimulate
biological responses in the barrier membrane such a.s
enhancing wound healing (e.g,, in acne lesions), and/or
enhanced skin in sensation which serves a signal to a user
chat the device is working. Another potential advantage of
using a blinking LED is to produce pulsatile DC current
without the nsed of a complex electric circuit.
The spectrum of the LED's according to the current
invention may range front about 300 nm to about 150 um,
such as from about 350 nm to about 1000 mn. In one
embodiment, the range of the LED includes violet-blue,
green, red and infrared ranges, e.g., from about 400 nm
to about 450 nm such as from about 407 ran to about 420 nm
from about 510 nm to about 55 0 nm; from about 600 nm to
about 700 nm; and from about 1300 nm to about 1500 nm. In
one embodiment, the device contains two LEDB, one that
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WO2005/004982 PCT/US2004/020271
emits light, having a wavelength of from about 400 nu to
about 500 nm and one "which emits light from about. 700 nm
to about 1000 nm.Photoseneitizer agents, such as 5-
aminolaevulinic acid (ALA) , hypericin, Se John's wort
powder or extract, or other synthetic or natural
photosnsitisier agents, may toe incorporated into the
carrier as active agents to be delivered and irradiated by
the device with LED's of the present invention. The light
irradiation from the LED's, together with the
photoeenaitiaer agent(s) and other aforementioned active
agents, electrochemically generated oxidizing agents
(e.g., peroxides, nascent oxygen, chlorine dioxide, and
chlorine) , and/or electric stimulation of the barrier
membrane may work synergistically to achieve an improved
efficacy in treating membrane disorders such as acne and
rosacea.
Genera1 Use
In one embodiment, the device is used for the
treatment of a barrier membrane condition (e.g., the
delivery of an active agent light, and/or electricity into
the membrane such as the skin, eye [cornea, retina, etc.),
oral, buccal, nasal, vaginal, gastrointestinal, or rectal
rnucosa barrier membrane, of a human). In one embodiment,
the device is used for the treatment of skin conditions.
Examples of such treatments include, but are not limited
to treatment of acne, rosscea,, or other microbial
infections of the skin, reduction the visible signs of
akin aging (e.g., wrinkles, sagging, and age-spots)
folliculitis and pseudo-folliculitis barbae, treatment of
wounds and lesions (e.g., enhancing healing and soar
reduction); sebum regulations {e.g., sebrum reduction or
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WO2005/004982 PCT/US2004/020271
oily/shining skin appearance inhibition or control) ;
pigmentation regulation (e.g., reduction of
hyperpigmentation or pigmentation of light skin) ; hair
growth retardation (e.g., skin on the leg) or hair-
stimulation (e.g., scalp); and treatment of dermatitis
(e.g., atopic, contact, or seborrheic dermatitis} and/or
paoriesis.
In another embodiment, the device is used for the
treatment of micosal conditions (e.g., mucosa in the oral
or vaginal cavities). Examples of such treatments include,
but are not limited to treatinent of vaginal candidiaeis
and vaginosis, genital and oral herpes, cold sore, canker
sore, oral hygiene, periodontal disease, and other
nticrabisl infections of the ntucosa.
Another embodiment of the present invention is the
device induces certain desirable biological responses that
facilitate the treatment of the barrier membrane
conditions. These desirable biological responses may be
induced by the electric current passage through the
barrier membrane, and/or the electrochemically generated
oxidising materials, together with the active agents
delivered by iontophoresis from the carrier, in treating
the barrier conditions. Examplea of the desirable
responses of the barrier membrane may include, but are not
limited to, xxx regulation (e.g., reduction of sebaceous
gland activity), inhibition of anaerobotic microbial
growth, and establishment of a healthier membrane
microflora or (e.g, reduction of p. acne growth and of
production of irritating fatty acids), blood
vasoconstriction (thus promoting local accumulation of
active agents or removal of dark circle under the eye due
to deoxyhernoglobina) , enhanced tissue nnmunological
34

WO2005/004982 PCT/US2004/020271
activity (e.g, increased elimination of pathogenic
microbes on tissue's own defense ayatetns) , iinproved tissue
repairing (e.g., enhanced healing and reduced scarring of
lesions such as acne lesions}, and improved keratolytic
activity or the carrier (e.g., softening of keratin plugs
of comedos in whiteheada and blackheads of acne, and
Facilitating their removal).
In another aspect, the invention also features the
method of converting an active agent from a less active
form to a more active form via oxidation or reduction, via
an inert eleccrade (e.g., cystine to cyeteine, diaulfide
acetyl-Cygteine to acetyl-cysteine, and retinol to
retinoic acid). Thue, an unstable agent can be stored in
a more stable form and converted to its active form prior
to administration. In a further aspect, the generation of
reducing agents by the device of the present invention can
be used to stabilise oxygen-labile active agents.
Examples of such oxygen-labile active agents include, but
are not limited to, retinoids, ascorbic acid, and oenzoyl
peroxide.
In one embodiment, the invention also features the
method of converting an active agent from a leas active
form to a more active form via. oxidation at an reactive
anode, such as an anode made of zinc, magnesium, copper,
aluminum, slloy or mixture of these metals for example,
an anode made of sine releases zinc ions with the passage
of an electric current through the electroda. The zinc
ions generated by such an electrochemical reactions are
then subsequently delivered by the electric repulsion of
the positively charged anode into the barrier membrane.
In one embodiment, such ions are deposited into the hair
follicles and/or sebaceous glands to inhibit p. acnes
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WO2005/004982 PCT/US2004/020271
growth arid/or suppress skin tissue inflamnation resulted
from p. acnes ovsr growth before the treatment Similarly,
a sine-copper alloy anode or another zinc-beneficial metal
alloy releases both zinc ions and copper ions or the other
beneficial ions, respecytively, into the hair follicles
and sebaceous glands for acne treatment and prevention.
Skin Conditions
In one embodiment, the device of the present
invention is used to treat skin conditions such as: acne
and acne (e,g. , blscklieads and whiteheads} and acne-
related skin conditions such as roeacea and nodule-cystic;
hypeirpigmentation such as freckles, tnelasttta, actinic and
senile lentigines, age-spcts, post-inflammatory
hypetmnelanoaia, Becker's naevus, datk circles under the
eye, ersd facial melanoais; stretch marks; and skin aging
effects on the skin (such as those caused by photodamage)
including wrinkling, roughness, pigmentary alterations,
sallovnesa, fine lines, and laxity, by delivering active
agents that including pra-formulated active agentig in the
carrier and electrochemically generated active agents
(e.g., beneficial metal ions) by the electrodes, and/or by
providing electric stimulation to the skin tissues.
In one embodiment, the device of the present
invention provide multiple mechanism of actions to treat
such conditions: namely, (a) target- delivering pre-
foxraulated. active agents into the piloaebaceous unit by
iontcsphoresia and electro-oamosis; {b) electro chemically
generating new active agents (e.g, the beneficial metal
ions from a reactive anode) and targeted delivery of the
freshly generated active agents to the pilosebaceous unit
(e.g., beneficial iona such as sine and copper have known.
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WO2005/004982 PCT/US2004/020271
to enhance skin's own immune system) ; and/or (c) providing
electric stimulation to the pilosebaceous unit and its
surrounding skin tissues to increase blood circulation,
and to treat the skin by reducing inflammation, enhancing
wound healing, and/or increasing skin exfoliation.
Mounds and Sears
In one embodiment, the device of the present
invention can be incorporated into wound dressings and
bandages to provide electric therapy for healing
enhancement and scar prenvetion. In one embodiment, the
wound exudation fluid and/or wound cleansing solution
serves tts activate a galvanic wound dressing /bandage to
deliver active agents pre-incorporated in the wound
dress ing/bandage and/or to generate clectrochemically
beneficial metal ions followed with delivery of the
beneficial metal ions into the wound. The device also
treats the wound with therapeutic electric current which
may increase blood circulation, stimulate tissue immune
response, and/or suppress tissue inflammation, which may
lead, to accelerated healing and reduced scarring.
Enhanced Chemical Peel
chemical peel treatments are an in-office procedure
that involves the application of a chemical agent to the
skin to induce controlled destruction or exfoliation of
old skin and stimulation of new epidermal growth with more
evenly distributed melanin. When peel agents reach the
dermal layer, important wound-healing activities occur
that cause skin remodeling and skin smoothing, both are
anti-agins benefits. Delivery of chemical peel agents
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WO2005/004982 PCT/US2004/020271
idoensyma, or zymogen form. Examples include pepsin,
Bromelain, papaya, and cathepain- Further examples
include natural extract chemical peeling agents such as
fruit extracts, muattrooni extract, and other plant
esnrarts.
In one embodiment, the duration of the application of
the device to the skin is froin about 2 to about 10 minutes
depending on the individual skin, conditions. In one
embodimerit, the carrier contains from about 0.1% to about
70% by weight of such chemical peel agent, such as from
about 0.5% to about 20% such as from about 3% to about
103.
Shape
The device includes a housing that may be fabricated
into various shapes and sizes to fit the contoura of
various anatomical surfaces of the barrier membranes. For
examples, the housing may be a substrate made in the shape
of a whole facial mask with openings/holes to expose the
eyes, eye bows, nose, and mouth; a partial facial mask
covering only the upper or lower half of the face; or a
patch coveting only the forehead, or the under eye region,
the chin and jaw region, the neck, the back, wound, acne
lesion or pimple, or other specific area of a barrier
membrane in need of treatment.
In one embodiment of the present invention, the
housing is a water-insoluble substtate containing a
galvanic couple, for example, a tine sine wire or a fine
zinc-coated fiber {e.g., zine-coated polymer fiber)
connected to a fine copper wire or a fine copper-coated
fiber (e.g., copper-coated polymer fiber). One or more
such fine galvanic couple wire(s) or fiber (a) may be
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WO2005/004982 PCT/US2004/020271
incorporated into the substrate to create a dsvics which,
when, in contact with the carrier (such as tap water or a
liquid or semi-liquid composition including active agents)
generates an electric current. In one embodiment, a
galvanic couple-containing suistiate may be made of
multiple layer, for exampla, a layer of the zinc
containing subscracs (e.g., a fine zinc wire- or a fine
zine-coated fiber in a woven or non-woven fabric) over a
layer of copper-containing substrate (e.g., a fins copper
wire- or a fine copper-coated fiber in a woven, or non-
woven fabric). During use, the layers contact each other
to form the galvanic couple. In a further embodiment, the
device releases beneficial ions (e.g., zinc ions or
aluminum ions) that are delivered to the barrier membrane
(e.g., the skin) when such a substrate is applied by the
user (e.g., used as a wipe for cleaning the skin or a
facial patch or mask to treat the skin) . Active agents may
also be incorporated into the substrate during
manufacturing processes or be subsequently applied to the
substarts prior to the application to the barrier membrane
(e,g. , in the fornt of an electrolyte or active agent
containing liquid, apray to wet the substrate}. In one
embodiment the fabric is used as a dry wipe or a dry full
or partial facial mask, to be wetted immediately before
use, by applying water to the dry wipe or facial mask to
pre-moisturised skin {e.g, by washing with tap water).
By "water insoluble" is meant that the substrate,
upon immersion in distilled water at 25oC, does not
readily diasolve in or readily break apart. The water-
insoluble substrate may, however, be disintegrated and/or
dissolved slowly, i.e., over a period of several hours up
to several days. A wide variety of materials can be used
40

WO2005/004982 PCT/US2004/020271
as the water-insoluble subserve. Examples of suitable
substrates include, but are not limited, to, non-woven
substarates, woven substrates, hydno-entarigleid substrates,
air entangled substrates, natural sponges, synthetic
aponges, and polymeric netted meshes.
The Water insoluble substrates may be fluehable. As
used bereia, by "flutshable" is meant that the substrate
will pass through at least l0 foat of waste pipe in two
toilet flushes. The material may also be biodegradable.
In one enibodiment, the substrates contain a non-woven
material. By "non-woven" is meant that the substrate, or
a layer of the substrate, is comprised of fibers that are
not woven into a fabric but rather are formed into a
sheet, mat, or pad layer. The fibers can either be random
i.e., randomly aligned) or they can be carded (i.e.,
combed to be oriented in primarily one direction.
Purthermore, the non-woven substrate can be composed of a
combination of layers of random and carded fibers).
Non-woven substrates may be comprised of a variety of
natural and/or synthetic materials. By "natural" is meant
that the materials are derived from plants, animals,
insects, or byproducts of plants, animals, and insects. By
"synthetic" is meant that the materiala are obtained
primarily from various man-made materials or from natural
materials, which havs been further altered.
Nan-limiting exemples of natural materials useful in the
present invention are silk fibers, Keratin fibers (such as
wool fibers, camel hair fibers) and cellulesic fibers
(such as wool pulp fibers, cotton fibers, hemp fibers,
jute fibers, and flax fibers}.
Examples of synthetic materials include, but are not
limited to, those selected from the group containing
41

WO2005/004982 PCT/US2004/020271
attetace fibers, acrylic fibers, cellulose eater fibers,
ctrtton fibers, raodacryl ic fibers, polyaniide fibers,
pclyoster fibers, polyolefixi fibers, polyvinyl alcohol
fibers, rayon fibers, polyurethane foam, and mixtures
thereol .
Substrates made from one ore more of the natural and
synthetic naterials useful in the present invention can be
obtained from a wide variety of connnercial sources such as
Freudenberg & Co. (Durham, NC USA), BBA Nonwovens
(Nashville, TN USA) , PGI Nonwovena (North Charleston, SC
USA), Buckeye Technologies/Walkisoft (Mamphis, TN USA),
and Fort James Corporation (Deerfield, IL USA} .
Methods of making non-woven substrates are also well
known in the art. Such, methods include, but are not
limited to, air-laying, water-laying, melt-blowing, spin-
bonding, or carding processes, The resulting substrate,
regardless of its method of production or composition, is
then subjected to at least one of several types of bonding
operations to anchor the individual fibers together to
from a self-sustaining web. The non-woven substrate can be
prepared by a variety of processes including hydro-
entanglement, thermally boudirtig, and combinations of these
processes. Moreover, the substrates can have a single
layer or multiple layers. In addition, a multi-layered
substrate can include film layer (s) (e.g., aperture or
non-aperture film laysrs) and other non-fibrous materials.
Strength or firmness of the non-woven material may be
a desirable attribute. This can be achieved, for example,
by the addition of binding materials, such as wet strength
reiains, or the material may be made of polymer binder
coatings, stable fibres, e.g. based on cotton, wool, linen
and the like. Examples of wet strength resins include, but
42

WO2005/004982 PCT/US2004/020271
are not limited to, vinyl acretate-ethylene (VAE) and
athylene-vinyl. chloride (EVCL) Airflex emulsions (Air
Products, Lehigh, PA), Flextaond. acrylic polymers (Air
Ptoducrs, Lehigh, PA) , Rhoplex ST-954 acrylic binder (Rohm
and Haas. Philadelphia, PA) , and Ethylene-vinyl acetate
(EVA) emulsion (DUR-O-SET* by National Starch Chemicals,
Bridgewater, NJ} . The amount of binding material in the
substrate may range from about 5% to about 20%, by weight,
of the substrate.
Non-woven materials Of increased strength can also be
obtained by using the so-called spunlace or hydxro-
sntanglement technique. In this technique, the indivictual
fibers are twisted together so that an acceptable strength
if firmness is obtained without the need to use binding
naterials. The advantage of the latter technique is the
lesteclient softness of the non-woven material.
In one embodiment, the non-woven material is made of
a super absorbent polymer. For the purposes of the present
invention, the term " superabsorbant polymer" refers to
materials which are capable of absorbing and retaining" at
least about 10 times their weight in body fluids under a
0.5 pai pressure. The superabsorbent polymer particles of
the invention may be inorganic or organic crosslinked
hydrophilic polymers, such as polyvinyl alcohols,
polyethylene oxides, cross linked starches, guar gum,
xanthan gum, and other material known to the art of
absorbent article manufacture,
Additives may also be added in order to increase the
softness of the substrates. Examples of such additives
include, but are not limited to, polyols such as glycerol,
propylene glyeol and polyethylene glycol, phthalate
43

WO2005/004982 PCT/US2004/020271
contains a removable release liner 100, a carrier layer
120, a First conductive electrode 140, a second conductive
clectrude 240, electric lead wires 110 and 210 connecting
the two ends of an elecirrically insulated connecting wire
350 to the two dissimilar conductive electrodes, an
optional electric powsr switch 330 located on the lead
wire 210, a backing layer 160, and a cover layer 340.
The gap "b" depicts the distance between two
conductive electrodes 140 and 240 to the release liner (or
the membrane following application of the device) , and the
gap "a" represents the distance between two oppositely
charged conductive electrodes. In one embodiment, gap "a"
is between 0 to about 20 centimeter. and gap "b" is
between 0 and to about 1 centimeters. In another
embodiment, the ratio of gap "a" to gap "b" is from about
0 to about 20.
The backing layer 160 may be impermeable to the
active agent contained within the carrier layer 120, and
is preferably not permeable to water or other solvents in
the carrier layer 120. The backing layer 160 and cover
layer 340 may be made of flexible material that is
impermeable to water and electrically insulating, e.g.,
polymers suah as polyethylene, polypropylene, polyvinyl
acetate, polyurethane, silicone rubber, or polyvinyl
ahloride.
In a further embodiment the backing layer 160 is
permeable to electrocherically generated gases (e.g.,
oxygen, chlorine, and hyirogen) in order to limit excess
accumulation of the gases in the carrier which can cause
tissue irritation and/or undesirable deformation of the
device. Examples of such "breathabl backing" material
include, but are not lited to, a cotton or synthetic
45

WO2005/004982 PCT/US2004/020271
woven and nonwoven fabric Iayer, such as those fabric
materials commonly used for bandages and sports bandages.
The carrier layer 120 is an adhesive hydrogel
containing the active agent. The active agent may be
incorporated into the carrier layer 120 as dissolved
molecules and ions, dispersed solid particles, or liquid
droplets such as creats, lotion, emulsion, multi-emuision,
microemulsion, and/or liposome compositions. The carrier
layer 320 may also contain a, solid supporting matrix
(e.g., a gauze, non-woven or sponoe-like material) .
A removable liner sheet 100 covers the carrier layer
120, The selection of the removable release-liner 100 is
dependent on the type of the adhesive hydxogel used in
carrier layer 120. The release liner sheet 10 0 is
typicslly a polymer sheet or a paper or fabric coated with
a polymer, which has weak adhesion toward the adhesive
hydrogel layer 120, thereby allowing it to be easily
removed from the carrier layer 120 prior to use without
damaging the carrier layer 120. Examples of the polymere
typically used for the release liner 100 are silicones and
polyethylenes. Alternatively a wax may be used in the
place of the polyrner to coat the release liner 100.
In addition to, or in lieu of, the use of an adhesive
in the carrier layer 120, the device 500 may be .fastened
to the barrier membrane with an adhesive tape, an elastic
band, a band with a buckle (similar to a leather watch
band) or a velcro hand.
In order to use device 500, the renovahle release
liner sheet 100 is peoled off, and the carrier hydrogel
layer 120 of the device 500 is affixed, to a barrier
membrane, such, as the skin of mucosal membranes each as
vaginal, oral, buccal, nasal, gastrointestinal or rectal
46

WO2005/004982 PCT/US2004/020271
each other through direct connect ion, naraely, the gap "a"
(the distance between, two oppositely charged conductive
electrodes) is equal to zero. Two conductive electrodes
forms a galvanic couple which is contact the carrier layer
120 enclosed in backing layer 160 with an opening affixed
to the release liner 100 with an adhesive layer 130. One
major advantage of this configuration is its simplicity
and easiness to manufacture.
Another embodiment of the present invention is
represented achematically in FIG. 5. The electrotransport
device 800 containes two electrode assemblies 200 and 600,
reeptccive adhesive layers 230 and 630, respective carrier
layete 220 and 620, respective conductive electrodes 240
and 640, respective backing layers 270 and 670, respective
eiectric leads 210 and 610, electrically insulated
connecting wire 350 and optional electric switch 330.
Similar to the aforementioned typical iontophoresis
device, the two electrode assemblies 200 and 600 are to be
affixed to the barrier membrane apart from each other,
after the release liner 100 is removed prior to use.
In one embodiment, the carrier layer 120 contains at
least two active agents carrying opposite electric
charges. One example of such a composition is a
composition containing from about 0.5 to about 2% of
salicylic acid. and from about 0.01 to about 0,2% of a
cationic quaternary ammonium antimicrobial agents (such as
benzalKonium chloride, benzechoium chloride, methyl
benzetlionium chloride, and cetylpyridirsium chloride),
phenol, and/or chloarhexidine gluconate. The device 500 of
the present invention can simultaneously deliver both
active agents of opposite charges into the membrane.
49

WO2005/004982 PCT/US2004/020271
Fig’s 5 and 7 show two examples of different
configurations of dissimilar conductive electrodes 140
(shown by a double line) and 240 (shown by a single line)
in carrier layer 120, connected by electrically insulated
wires 350 (shown by a triple line) to form a galvanic
couple power source. FIG. 6 shows that the conductive
electrodes 140 and 240 are arranged in an inter-digitated
configuration. FIG, 7 shows the conductive electrodes in a
concentric configuration.
FIG's 8 and 9 show two examples of other
configurations of dissimilar conductive electrodes 140 and
240 in carrier layer 120, connected to each other either;
connective wire 350 as in FIG 8 or by a direct physical
contact at each intersection 370 as in FIG 9 to form a
plural of galvanic; couple power sources, which are in
contact with the carrier layer 120. The conductive
electrodes 140 and 240 in FIG'a 8 and 9 are arranged in
parallel and perpendicular configurations, respectively.
The alternating parallel arrangement of the
conductive electrodes 140 and 240 in FIG. 8 provides a
more uniform electric current distribution throughout the
carrier layer 120 and the underlying skin tissue, and
consequently, assist in enabling a more uniform delivery
of active agents into the skin. One exemplifying
fabrication method for the galvanic device shown in FIG. 8
is by weaving a silver-coated polymer fabric and zinc-
coated polymer Cabrie (or zinc wire} into a liquid-
absorbant fabric layer according to the parallel electrode
pattern, then connecting zinc and silver electrodes by
printing over the silver and sine regions with an electric
conductive ink (e.g., conductive silver or carbon ink).
Covering another layer of an electric insulating ink over
50

WO2005/004982 PCT/US2004/020271
the electric; conductive ink will produce the electrically
insulaLed connecting wire 350.
Another fabrication method for the device of FIG 8 is
via printing; to prinL onto a non-conductivs polymeric
substrate layer (e.g. the polymer material made of the
bicking layer 160) using a conductive silver or silver-
silvear chloride ink to produce the first conductive
electrode; and to print the second conductive electrode
using a conductive sine ink. The two dissimilar
conductive electrodes are then connected by printing cross
them with either the conductive Silver or zinc ink (or a
different conductive ink such as carbon ink). A covering
ink may then optionally be printed over the connecting
wire to produce an electric insulating polymer layer over
it. If the device is made without insulating with an
electrically insulating coverying layer, the resulting
device is a variation of that depicted in FIG. 9.
FIG 9 is a top view of one embodiment in accordance
with the invention showing the conductive electrodes 140
and 240 connected to each other by direct physical contact
at the intersections 370 to form a galvanic couple power
source, which is in contact with the carrier layer 120.
The conductive electrodes 140 and 240 are arranged in a
Perpendicular configuration. The aforementioned
fabrication methods for the device in FIG. 8 is also
suitable to produce this device.
FIG. 10 is a top view of one embodiment in accordance
with the invention showing a device made of a zinc meth
having conductive electrodes 140 (shown in bold lines) and
electrodes 240 (shown in double lines) connected by
ilcctrically insulated connecting wires 350 (shown in
single lines') embedded in the carrier layer 120. The
51

WO2005/004982 PCT/US2004/020271
sbrsductive electrodes 140 are uncoated regions of the zinc
mesh. The conductive elefctrodis 240 is prepared by coating
the designated portion of the zinc mesh with a silver-
silver chloride ink. The electrically insulated coiinecting
wire 350 is prepared by coating th^ designated portion of
the zinc mesh with an electrically insulating paint, ink.,
or polymer solution.
FIG, 11 is a top view of one embodiment in accordance
with the invent ion showing the conductive electrodes 140
and 240 embedded in the carriex layer 120. The conductive
electrodes 140 are made of a piece of zinc mesh. The
conductive electrodes 240 are prepared by costing the
designated portion of the zinc mesh with a silver-silver
chloride or silver ink, or by other silver seposifcing
methods such as electroless deposition (chemical reduction
ieposition), electroplating, plasma spray, or vacuum
deposition. Elimination of the electrically insulated
connecting wire 350 in this design would simplify the
manufacturing process. The location, pattern, shape, and
size of the electrode of metallic silver, silver-silver
chloride or silver-silver oxide may vary depending on the
need, of a particular products.
zine mesh, (or expended zinc" as common called in
battery and anti-corrosion fields) may be prepared from a
thin zinc fol] with mechanical perforation and subsequent
expansion into net-like patterns. The major advantages of
a zine mesh enode in the galvanic device of the present
invention are its ability of forming and retaining the
desirable mask/patch shape by a uaer,stretching by a user
toward any directions to form mask/patch of desirable
size, and being breathable.
52

WO2005/004982 PCT/US2004/020271
It should be noted although the use of zinc mesh is
described here as an example of electrode designs, other
aforement ioned materials suitable for galvanic couple
formulation and for conductive electrodes can also be made
into a mesh or an expanded form to provide the same
function.
Zinc mesh also has the ability to conform to the
shape of the membrans surface (e.g. the shape of an
individual's face} by gently pressuring it, and to retain
this shape. This capability makes it uniquely suitable for
a facial mask, or certain skin patches to better fit the
contours of certain anatomic features of the face (e.g., a
NOse patch) or body areas. This unique feature also
ansists in better electric contact and may also reduce
dependence on using adhesives to affix the device to the
skin.
It is also highly convenient and desirable to a
consumer if a facial mask or patch can be stretched to
different sizes in order to cover a particular skin area
without compromising its electric performance. A zinc mesh
aiode tor other mesh conductive electrode) is uniquely
Cipable to fulfill this consumer need. In another
e nbodiment the mesh is not expanded before use so that
the device is smaller and more compact for easy storage
and jsnymg. Rather it is stretched open to a desired
size during application by a consumer.
Good breatliability is important for a facial mask or
a patch ox relatively large sise, especially if the device
is designed to be worn by a user for an extended period of
time (e.g., longer than one half hour such as overnight).
In order Co make aforementioned device etretchable and/or
breathable, the carrier layer 120 and backing layer 160
53

WO2005/004982 PCT/US2004/020271
should also be stretchable and breathable, such as
stretchable woven and nonwaven fabric teaheriala.
In anothe embodiment, the baking layer 160 in FIG'S
3-5, can be pert orated or eliminatetd entirely for a mask
or patch device, which is especially suitable for the
application of short duration, e.g., from about 5 to about
30 minutes. As water in the carrier composition
evaporates, the electric conductance and the electric
current decrease. Eventually, the electric current will
significantly diminish, providing in essence a self-
terminating device to serve as a safety measure for the
user to prevent any unintentional over-exposure of the
skin to the electric current and potential resulting skin
damage.
One example of such a self-terminating device is a
galvanic cloth facial mask made with a sine mesh partially
coated with silver-silver chloride ink, which is placed in
between a backing film/housing (e.g., a perforated or
nonperforated polyethylene film) and a nonwoven fabric
(e.g., a polyester and/or rayon nonwoven sheet) using a
binding process based on heating, ultrasound or other
mechanism Prior to application, a liquid or semisolid
earner composition containing ionic and non-ionc active
agents and other optional electrolytes is applied to the
non-woven AND OF the device to activate the galvanic power
source. The galvanic device is then pressed onto the
light's face with the nonwoven side in direct contact with
the skin. Alternatively, the active agents and other
optional electrolyte may be incorporated in nonwovan layer
during manufacturing process in an anhydrous stats. In
use, the device can be applied to water-wetted face, and
the water will dissolve the active agents and electrolytes
54

WO2005/004982 PCT/US2004/020271
to activate the galvanic current. The anhydrous active
agenta may be in the form of dry powder immobilized onto
the inhers or the nonwoen, or dissolved firgt in an
organic solvent (e.g., polyethylene glycol, propylcne
glycol, glycerin, and/or alcohol) to form a non-conductive
or very law conductive solution, which is absorbed in the
ion woven layer .
The zinc anode materials may be manufactured with a
wide variety of manufacturing process, including, but not
limited to, metal processing, electroless deposition,
electroplating, plasma spray, vacuum deposition, print
processes such as screen, printing using a zinc conductive
ink, textile or nonwoven technologies. Similarly, other
conductive metal materials, such as silver-silver
chloride, silver-silver oxide, copper, magnesium, aluminum
alloys Of sine, magnesium, copper and aluminum, may be
manufactured into the aforementioned electrode forms uaing
the manufacturing processes disclosed above.
Topical Compositions Containing Galvanic Pairs
In one embodiment, the present invention features a
topical composition containing a first conductive metal
particulates such as fine flakes, wires/fibers or metal-
coated fibers) selected from zinc, aluminum, copper, and
their alloys; and a second conductive metal particulates
(such as fine flakes, wires/fibers or metal-coated fibers)
selected from silver, copper, gold, and their alloys. The
first and second metal particulates can be selected from
aforementioned electrode materials to form galvanic
couples. Upon contact, the first conductive metal and the
second conductive metal form a galvanic pair, generates
electric current, and electrochemicaliy generates ions.
55

WO2005/004982 PCT/US2004/020271
In a further embodiment, the difisrence of the standard
potentials ef the first conductive metal end the second
conductivs metal is at least about 0.lv, such as at least
abput 0.5 V. For example., upon contact with a first
conductive metal that contains sine (such as fine zinc
wires, sine flakes or polymer fibers coated with sine) and
a second conductive metal that contains silver (such as a
fine silver wires/fibers, silver flakes, or polymer fibers
coated with silver), the cortpositien. generates electric
current and zinc ions within the topical composition.
The composition may additionally contain an active
agent, such as an anti-acne agent (such as ealicylic acid,
benzoyl peroxide, retinoic acid and/or retinol). The
topical composition containing the first mecal and the
second metal is preferably a semi-solid dosage form (such
as a gel, a hydragel, a water-in-oil emulsion, an oil-in-
water emulsion, a cream, a lotion, an ointment, a multi-
emiilsion, a liposome, and/or a microcapsule formulation),
and may contain the aforementioned fluid suspending or
fluid absorbing materials. The topical composition may be
prepaired as such that one of the conductive metal is
formulated in a. separate phase from other conductive
metal, for example, the first conductive metal (e.g., zinc
flakes) is formulated in the discontinuous oil phase of an
oil-in-water emilsian (e.g., a creem), while the secornd
conductive metal (e.g, silver flakes) is formulated in
the continuous aqueous phase of the emulsion. The topical
composition of the present invention may also further
contain a humectant (such as glycerin, propylene glycol,
polyethylene glycol, aotbitol and/or urea) and
aforementioned electrolytes to maintain certain moisture
level and conductivity of the skin.
56

WO2005/004982 PCT/US2004/020271
In one embodiment, during storage of such a topical
composition, the first conductive metal and the second
conduct metal are suspended substantially apart, in a semi—
solid composition (e.g., are not in contact with each
other) . Upon application to the membrane (such as the skin
or mucose) and partial drying of the liquid carrier, the
contact of the first conductive metal and the second
conductive metals results in galvanic couple fonraatioin and
generation of electric current and metal ions of the first
conductive metal, which provides benefits to the membrane
such as antimicrobial, antiinflammation, wound healing,
iontophoretic delivery of active agents, tissue
stimulation, and/or sebum reduction.
In one embodiment, the wires/fibers, flakea of
conductive metals, or polymer fibers coated With the
conductive metals are fine enough that they can be
isuspended in the semi-aolid composations during storage.
In a further embodiment, they are in elongated shapes. The
advantages of elongrated shapes of the conductive metals
(e.g., fine wires/fibets, flakes and polymer fibers coated
with the conductive metals) include a lovrer apparent
density and, therefore, a better floating/snapending
capability in the topical composition; a higher
probability at connected with each other when low
concentrations of the conductive metals are used; and a
wider and deeper range of the membrane tissue (e.g, the
skin) that the galvanic current travels through and
provides the benefits to.
In one embodiment, the first and second conductive
metal particles are formulated into different compositions
and are stored in separate compartments of a, dual chamber
dispensing package. For example, the less chemically
57

WO2005/004982 PCT/US2004/020271
stable (e.g., more oxidizable)zinc or its alloy
particulates may be formulated in an anhydrous,
essentially non-conductive composition with organic
solvents; such as polyethylene giycols, gropyletie glycol,
glycerin, liquid siliane and/or alcohol, or other
pharmaceutically-acceptable organic solvents. The more
chemically Stable (e.g., less oxidxzable) silver and
silver chloride; particulates may be formulated in an
aqueous compositon. The active agents may be formulated
into either composition depending on their chemical
stability and solubility. In use, the compositions are
dispensed from dual chamber package (e.g., dual chamber
pump, tube, pouch, bottle, etc.) and mixed prior or during
application to the skin to form galvanic couples in situ
to generate galvanic current and to treat the skin
conditions.
In another embodiment, the aforementioned, galvanic
couples are manufactured as particuIatee to be
incorporated into topical compositions. The particulates
may be of any shape, including but not limited to,
Spherical or non-spherical particles or elongeted or
flattened shapea (e.g., metal or metal-coated spheres,
hollow metal or metal-coated epheres, short metal-coated
fibere or fabrics, and flakes), regular shapes (e.g.,
metal crystals), and irregular shapes (e.g., aggtegsued
Spheres). In one embodiment, the parciculates have an
average particle size of from about 1 micrometer to about
5 centimeters. What is meant by the particle size the
maximum dimension in at least one direction. In one
embodiment, the particulates have an average particle size
of from about 1 micrometer to about 2 millimsters for non-
elongated shapes. In another embodiment, the particulates
58

WO2005/004982 PCT/US2004/020271
with elongated shapes have an average particle size from
about 10 micrometers to about 2 centimeters such as from
about 100 micrometerg to about 50 millimeters. For
example, a polymer fiber of about 100 micrometers to about
10 millimeters in length may be coated partially with
silver or silver-silver chloride on one end (or only on
certain portions of the fiber),and zinc on the other end
(or on the remaining portions). In another example, the
polymer fiber is coated completely with the first
conductive metal (e.g., silver-silver oxide or silver-
silver chloride), and one end {or certain portions of the
fiber) is coated with the second conductive metal (e.g.,
zinc or magnesium) .
In practice, silver-coated, polymer fibers
mnufactured by Noble Fiber Technologies, Inc. [Clarks
Summit, PA.) may be coated with zinc using methods such as
conductive sine ink printing, electroplating, electroless
depositior, vacum deposition, and spray coating.
Alternatively, a metallic sine or magnesium particulate
(e.g., bead or thin wire) may be coated at one end or at
certain portions) with silver-silver oxide or silver-
silver chloride. Spherical or non-spherical particles
with an average particle size ranging from about one
micrometer to about 5 millimeters may be partially covered
with the first and second conductive metal coatings in a
similar fashion.
The coating methods for such first and second
conductive metals in preparing the galvanic couples may be
electroless deposition, electric plating, vacuum vapor
deposition, arc spray, conductive metal ink, and other
known metal coating methods commonly used in electronic
and medical device manufacturing processes. The galvanic
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WO2005/004982 PCT/US2004/020271
couple particulates ate preferably stored in
aforementioned anhydrous forms, e.g., as a dry powder or
immobilized in a fabric with binding agents, or as at
essentially anhydrous non-conducting origanic solvent
composition (e.g., dissolved in polyethylene ctlycols,
prupylene glycol, glycerin., liquid gilicone, and/or
alcohol) . The galvanic particulstas have great versatility
in applications, and can be used in many consumer and
medical products such as patches, bandages, masks,
garments, cloths, socks, bed sheets (e.g., by immobilized
into the carrier or fabric) , spread -on facial mask
composition (such as a paste, cream or gel), creams,
lotions, gels, shampoos, cleansers, powders, or
incorporated into personal and medical products such as
toothbrushes, dental flosses, wound dressings, diapers,
sanitary napkins, dry wipes, pre-moistured wipes (with
aforementioned anhydrous solvents), tampons, and rclal
and vaginal suppositories. The galvanic particulares may
also be incorporated into transdermal drug delivery
patches to enhance drug penetration into the skin by
iontophoresis and to reduce skin irritation by electrie
stimulation and electrically generated beneficial ions
such as zinc ions.
Example 1: Carriers
Examples of several carriers, including the weight
percentage range of the ingredients of such, carriers, are
set forth in Table 1.


61
WO2005/004982 PCT/US2004/020271


WO2005/004982 PCT/US2004/020271
In order to evaluate the proposed mechanism of action
for the electrochemically generated beneficial agents, an
in vitro inicrobiologic study was conducted to investigabe
effect of electrolysis on p. acne inhibition in certain
electrochemical systems; and an in vivo study was
conducted in human volunteers using e commercial
iontophoresis device,
EXAMPLE 2. In. vitro Inhibition of P. acnes by
Electrolysis
A BacT/ALERT system (BioMerieux, Inc., Durham, Nc)
was used in the P. acnes inhibition experiment. Briefly,
40 ml of an anaerobic casein and soy based broth culture
medium in a bottle (BacT/ALERT SN, Organon Tekniks Corp.,
Durham, NC) was inoculated with P. acnes. The fully
automated BacT/ALERT system was used to detect P. acnes
growth over a 14-day study at 35°C by continuous monitoring
of CO2 production using an optical colorimetric sensory
system. A selected pair of the electrodes (Table 2,
Columns 2 and 3) was disinfected with 70% isopropyl
alcohol, and inserted through the rubber stopper into the
culture medium in a nitrogen glove box. Some electrodes
were connected to the poles of a battery (either 1.5 or 3v
as indicated in Table 2, Column 3) for 30 minutes. The
electrodes more then immediately removed from the
BacT/ALERT bottle, which was then placed into the
automated incubation and monitoring system for two weeks.
Other elscrodes (i.e., Nos. 3 & 5 in Table 2), were not
connected to an external battery, but rather were directly
connected, to each other at their ends outside the
BacT/ALERT bottle to form galvanic couple. The electrodes
of these galvanic couples (i.e., NON. 3 & 5) remained in
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contact with the culture medium in the bottle during the
14-day study.
Zinc as the positive electrode (anode), with various
materials as the negative electrode (cathode) , was
evaluated through the test conditions 1 to 7 (No.l-7 in
Column 1). Column 4 shows the voltage applied to the
conductive electrode by the external battery. However, by
simply connecting two conductive electrode materials, a
voltage was also generated just from the galvanic pair.
For example, zinc-silver/silver chloride galvanic couple
has a voltage of 0.9849V or about IV (zn2+ + 2e- = Zn,
standard potential: -0.7626V, and AgCl + e- = Ag + Cl-,
standard potential: 0.2223V} and zinc-copper- galvanic
couple has a voltage of about 1.1-1.3V (Cu2 +2e- = Cu,
standard potential: 0.340V, and Cu+ + e- = Cu, standard
potential: 0.520V} Reference; Electrochemistry Handbook,
1995, Table 14.1, McGraw-Hill, Inc. New York, NY).
In the test condition No. 7, the electrodes {i.e.,
zinc-silver/silver chloride galvanic couple) were taken
from a commercial iontophoresis device (lontoPatch, Sp,
Birch Point Medical, Inc., Oakdale, MN) . The lontoPatch is
an iontophoresis device powered by a galvanic couple
battery strip made of zinc and silver/silver chloride in
a bandage-like device. In this experiment, the "battery
strip" in the Iontopatch was taken out of the bandage-like
device, and placed into the BacT/ALERT bottle. The
electrodes of the commercial zinc-silver/silver chloride
galvanic couple (NO- 7) remained in the BacT/ALERT bottle
through out the entire two-week experiments. Test
conditions of Noa. 15-27 were positive controls (i.e.,
without electrodes) : Test condition No.15 used a
concentrated P. acne culture that was used to inoculate
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WO2005/004982 PCT/US2004/020271
the rast of the culture medium in each EaeT/ALERT bottle
to P. acmes counts of 106 per ml and Test conditions No. 16
and No.17 used, the inoculated culture mediura of P. acnes
counts or 105 per ml (with the rubbed stoppers of No.16
additionally being punctured in a way similar to the rest
of electrode-tested conditions in order to eliminate any
false p.acnes inhibition results due to potential
enviromental oxygen entry into the test bottle and
affecting anaerobic P. acnes growth).

64


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WO2005/004982 PCT/US2004/020271
positive P. acnes growth probably due bacterial
centamination, see Note C of Table 2) . The copper anode
was also found to significantly inhibit P acnes growth
(Nos, 8-9) . Under Lhese experimental conditions, the
platinum anode shewed little P. acne inhibition affect and
the silver or silver/silver chloride anodes provided only
a weak P, acne inhibition. Since all the positive control
(renditions (N0s. 15-17) showed positive P. acnes growth
less than two days after the beginning of the study, the
negative F. acnes growth can be attributed, to the
inhibition effect of the electracheraically generated
species or electric current passage through, the culture
medium. Because electric current passage in NOS. 10-14
failed to show strong P. acnes inhibition as those in Nos.
1-9, the observed bacterial inhibition in Nos. 1-9 were
likely due to certain electrochemical reactions occurred
at the anode, namely, when zinc and copper were used as
the anode. It was also unexpected that the silver ions
released; from silver or silver/silver chloride anode under
these expearimental conditions failed to show the same P,
acnes inhibition (Nos. 12-14) , since silver ion is well-
known anti-microbial agent. See. e.g., Spacciapoli et
al. ("Antimicrobia) activity of silver nitrate againts
periodontal pathogens.", J Periodontal RSE 36: 2, 103-13,
Apr, 2001) . It was surprising that, in the absence or
external battery {Nos. 3, 5 and 7), a pair of electrodes
of galvanic couple with sine as anode were sufficient to
inhibit P-acnes growth during the entire two week Study •
EXAMPLE 3- In vitro Electrode-salicyljc acid compatibility
The following experiment was conducted to determine
the compatibility of electrodes with salicylic acid. A
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WO2005/004982 PCT/US2004/020271
pair of test electrodes was immersed in 5 ml oE 1.5%
salicylic acid solution (solvent 50% ethanol/ 50% water).
A pre-determined voltage was applied to the electrodes (by
connecting the electrodes to a battery or batteries) for
certain length of time as indicated in Table 3.
Observations were made on color change of the test
solution.
The solution with the sine anode showed no
discoloration, indicating good compatibility with
salicylic acid during the passage of electric current.
Use of the platinum anode unexpectedly resulted in
discoloration, indicating incompatibility with salicylic
acid under this experimental condition.

EXAMPLE 4: In vivo human iontophoresis stuudy
An in vivo study was conducted in human volunteers
using a commercial iontophoresis device (IontoPatch*,
Model: SP, Birch Point Medical Inc., North Oakdale, MN).
The study recruilted the healthy female volunteers with
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WO2005/004982 PCT/US2004/020271
oily skin, aged from 20-45 years. The sebumeter reading
from each subject's forehead was at least greater than 150
mg/cm2/hr . The study was blind and controlled. Briefly,
an iontoPatch® with a voltage of 1 volt , an operating
current of 0.06 mA; and an active treatment area of 1.25
in2, was applied to the treatment site of the human subject
(e.g. fotehead}. The positive electrode and negative
consisted of zinc and silver/silver chloride
(Ag/AgCl) material, respectively. Both, electrodes were
filled with saline (0.9% NaCl). As soon as the saline
solution was added into the different electrodes, the
electric patch begin to function. The patch was left on
the treatment area overnight {e.g., approximately 8
hours).
The following evaluations were conducted: (i) the
effects of electrolysis on the skin condition were
monitored using a normal photography and (ii) The change
in p. acnes counts was determined through analyzing the
cup wash solution for the treatment site before and after
wearing the patch overnight.The cup wash micro sampling
procedure was performed as follows; a cylindrical cup (2.1
cm diameter and 2.5 cm height) having two open ends was
fastened onto the treatment area. The treatment area
inside the cylinder was then washed with 3 ml of cleansing
buffer (eterile 0.075M Phosphate Buffer containing 0.1%
Triton X-ioo) while the same area with a sterile polished
glass. The wash solution was then collected. This
washing procedure was then repeated. The two collected
samples were pooled and used in the P-acnes aanalysis
The p. acnes counts were determined by Spiral Plating
the scrub samples anaerohically in Actinomyces Agar for 5
days, and the predominant contaminants on the spiral
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WO2005/004982 PCT/US2004/020271
plates were Gram stained and identified using the VITEK
system Using an automated colnny counter, the P-acne
count per mL of each sample Durtsr was determined.
After only one overnight patch application, P. acne
quantification measurment an the treatment area shows a
45% p, acne reduction relative to the baseline under the
sine anode and 30% under the Ag/AgCl cathode. After four
consecutive overnight patch applications, photo images
displayed the clear evidences of significant reduction in
the color and size of post-acne hyperpigmentation apot
under the zinc electrode. This test subject had a post-
ache hypeipigmentation spot at the test akin site. The
sppeaiance of the hypexpigmented spot was improved from a
very dark color to a lighter color.
Also, after four consecutive overnight patch
applications, photo images also displayed the evidence of
significant reduction in the color and size of an acne
pimple under the Ag/AgCl electrode. This test subject had
an acne pimple at the test skin site. The redness of the
pimple was rapidly reduced from very red color to became
almost invisible while the pimples at the non-treated skin
area remained largely unchanged.
EXAMPLE 5:In vivo human iontophoresis study using
histamine hidrochloride as marker
An in vivo study was conducted in three human
volunteers using a galvanic sine-silver/silver oxide
device to deliver histamine hydrocholoride as a marker into
the skin. Histamine-induced skin erythema and itchinees
were recorded during and after- the study. The study
recruited two healthy male and one female volunteers with
ages ranging 41 to 49 years. The galvanic devices were
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WO2005/004982 PCT/US2004/020271
prepared by cutting a thin Zinc foil (0.25mm thick, Alfa
Aesar, word Hill, MA) into rectangular piece (2.5cm wide &
3cm long) - A silver ink {Silver Print, M.G- Chemicals,
Toronto, Ontario, Canada) was painted onto one side of the
sine foil as a 0.5cm wide stripe along the long-axis at
the center. The ink Was air-dried to produce the silver
eletyode stripe on the zinc foil. Two rectangular
adhesive Scotch® tape stripes of 0.5cm wide and 3cm long
were placed on the both sides of the silver electrode
stripe creating an electric insulating gap on the surface
(electrode gap = 0.5cm). A rectangular piece of nonwoven
fabric (50% Rayon/50% PET, 75 gsm, PGI Polymer Group Inc. ,
Landisville, NJ) of 3cm wide and 3.5cm long was placed
over the zinc-silver electrode side of the zinc foil. A
rectangular adhesive backing film of 4cm wide and 5cm long
was affixed to the opposite side of the zinc foil to
complete the zinc-silver galvanic device.
A second type of the zinc-silver galvanic device
without and electric insulating gap on the
surface (electrode gap = 0cm) was prepared by simply
omitting the addition of the adhesive Scotch® tape. A
third type (control) patch was prepared by using only the
zinc foil, the nonwoven pad, and the adhesive backing film
to construct the device.
To begin histamine iontohorasis, o.8ml aquepua
solution of 0.1% histamine hydrochloride (sigma-Aldrich,
St. Louis, Mo) was added to each device, which was then
affixed to the forearm skin of each volunteer for 30
minutes.
At the end of the study, red spots (histamine induced
erythema) appeared under both zinc-silver galvanic patch
devices, which disappeared within about one half hour. A
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WO2005/004982 PCT/US2004/020271
close examination showed the red spots around the hair
follicles. There was also itchiness reported at the
galvanic patch sites reported during the patch
application. In contrast, there were no change in skin
color under, nor any itchiness reported with, the control
patch devices.
EXAMPLE 6: In vivo human iontophoresis study using
histamine_hydrochloride with a galvanic nose patch
comprising zinc mesh
As a continuation of the human in vivo study in the
previotis example, a galvanic patch device (designated here
as "Test Device D" ) comprising a zinc mesh (diamond
openings of lcm long & 0.4cm wide, Exmet Corporation,
Naug attick, CT) instead of sine foil was prepared with the
same dimension and procedure as the galvanic device (gap
electrode = 0) in EXAMPLE 5. The device thus prepared
Resembled to the design shown in FIG. 11 with three
parallel electrodes the silver electrode in the center
and sine electrodes on both sides. Two male volunteers
participated this study using a similar test conditions as
in EXAMPE 5. One Test Device containing 0.8 ml of 0.1%
histamine hydrochloride was applied to the nose of each
volmitee for 30 minutes. It chiness was reported within 5
minutes of the nose patch application, indicating rapid
delivery of histamine into the relatively larger skin
pores on the nose. For both test subjects, pronounced
erythema was observed at the akin site under the nose
patch after patch removal at the end of the study, in
comparison to the study conducted on the forearm skin.
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WO2005/004982 PCT/US2004/020271
It is "understood that while the invention has been
described in conjunction with the detailed description
thereof, that the foregoing description is intended to
illustrate and not limit the scope of the invent ion, which
is defined by the scope of the appended. claims. Other
aspects, advantages, and modifications are within the
claims.
What is claimed is:
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WO2005/004982 PCT/US2004/020271
1. A method of treating acne or rosacea on the
skin said method comprising applying electricitiy no skin
in need of such treatment wherein said electricity is
generated by a first conductive electrode in electric
communication with a second conductive electrode, wherein
both said first conductive electrode and said second
conductive electrode are in ionic communication with said
skin wherein the difference of the standard potentials of
said first conductive electrode and said second conductive
electrode is at least 0,2 V and wherein the elections that
pa.se between said first conductive electrode and said
second conductive electrode are generated as a result of
said difference of the standard potentials .
2. A method of claim 1, wherein said, first
Conductive electrode comprises zinc.
3. A method of claim a, said method comprising
applying to said skin a device, said device comprising:
a housing having a skin contacting surface,
a first conductive electrode;
a second conductive electrode; and
a carrier,
Wherein said first conductivs electrode is in ionic
communication with said carrier and wherein said carrier
is in communication with said skin through said skin
contacting surface.
4. A method of claim 3, wherein said first
conductive electrode comprises zinc.
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WO2005/004982 PCT/US2004/020271
5. A method of claim 3, wherein said second
conductive electrode is also an iconic communication with
said carrier.
6. A method of claim 4, wherein said second
conductive electrode is also in iotiic communication with
said carrier.
7. A method of claim 3, wherein said housing is a
non-woven subatrats.
8. A method of claim 3, wherein carrier is added to
said device by the user prior to application to said skin.
9. A method of claim 5, wherein carrier is added to
said device by the user prior to application to said skin.
10. A method of claim 3, wherein said carrier
further canr-priseE an anti-acne agent selected from the
group comprising tretimoin, isotratiuoin, motretinicte,
adapalene, casarotena, aaelaic acid, retinol, salicylic
acid, benzoyl peroxide, rsaorcinsl, sulfur, sulfacetamide,
tfetrsycline, clinciaxnycin, metrcriirfazole, erythromycin,
and salts thereof.
11. A method of claim 1, wherein said method
comprises topically applying a composition to said skin
said composition comprising said first conductive
electrode in the form of a, particulate and a second
conductive electrode an the form of a particulate.
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WO2005/004982 PCT/US2004/020271
application, said mrsu conctuttive eieccroae is storea
separately from said composition.
14. A method, of claim 11, wherein said firsc
conductive electrode and said second conductive electrode
on the same partictilate.
15. A method of claim 11, wherein said composition
further corapriaes an anti-acne agent selected from the
group comprising tretinoin, isotretinoin, raotretinide,
adapalene, tazarotene, azelaic acid, retinol, salicylic
acid, benzayl peroxide, resorcinol, sulfur, sulfacetamide,
tetracycline, clindaniycin, metronidaaole, erythxoraycin,
and salts thereof.
16. A method of promoting a product comprising a
topical carrier, a first conductive electrode in the form
of a particulars, and a second composition comprising
second conductive electrode in the form of a participate
whenein. the difference of the stsndard potentials of said
firgt conductive electrode and said second conductive
electrode is at least 0.2 V, said method comprising
promot±ng the topical application of such composition, for
the treatment of acne or roaacea.
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WO2005/004982 PCT/US2004/020271
conductive electrode is suspended in said carrier and said
second conductive electrode is contained separate front
said carrier.
20. A method of claim 11, wherein said composition
further comprisea an anti-acne agent selected from the
group comprising tretinoin, iaotretinoin, motretinide,
adapslsne, taafotene, azelaic acid, recinol, salicylic
acid, benzoyl peroxide, resoreifiol, sulfur, gulfacetamide,
tetracycline, cliadamycin, mettonidazole, erythromycin,
and salta thereof.

76

(54) Title: METHODS OF TRATING ACNE AND ROSACEA WITH GALVANIC GENERATED ELECTRICITY
(57) Abstract:

Documents:

http://ipindiaonline.gov.in/patentsearch/GrantedSearch/viewdoc.aspx?id=Guxpl4czapLx7+q3iEqxvA==&loc=wDBSZCsAt7zoiVrqcFJsRw==


Patent Number 270588
Indian Patent Application Number 714/KOLNP/2006
PG Journal Number 02/2016
Publication Date 08-Jan-2016
Grant Date 31-Dec-2015
Date of Filing 24-Mar-2006
Name of Patentee JOHNSON & JOHNSON CONSUMER COMPANIES, INC
Applicant Address 199 GRANDVIEW ROAD, SKILLMAN NEW JERSEY 08558, U.S.A
Inventors:
# Inventor's Name Inventor's Address
1 WU, JEFFERY 126 BUTTERCUP BLVD, WARRINGTON, PENNSYLVANIA 18976, U.S.A
2 CHANTALAT, JEANNETTE 101 CLARIDGE COURT #7, PRINCETON NEWJERSEY 08540, U.S.A
3 OMER, ALIYA 909 BLUE SPRING ROAD PRINCETON, NEW JERSEY 08540, U.S.A
4 SUN, YING 90, WOODVIEW DRIVE, BELLE MEAD, NEW JERSEY 08502, U.S.A
5 LIU, JUE-CHEN 268 BERKLEY AVENUE, BELLE MEAD, NEW JERSEY 08502, U.S.A
PCT International Classification Number A61N 1/30
PCT International Application Number PCT/US2004/020271
PCT International Filing date 2004-06-24
PCT Conventions:
# PCT Application Number Date of Convention Priority Country
1 10/874,917 2004-06-23 U.S.A.
2 10/885,282 2003-10-14 U.S.A.
3 10/809,727 2003-06-30 U.S.A.