U.S. patent application number 11/278105 was filed with the patent office on 2007-03-01 for compositions and methods for treating acne.
This patent application is currently assigned to REVANCE THERAPEUTICS, INC.. Invention is credited to Jane Lee, Jacob M. Waugh.
Application Number | 20070048234 11/278105 |
Document ID | / |
Family ID | 37054204 |
Filed Date | 2007-03-01 |
United States Patent
Application |
20070048234 |
Kind Code |
A1 |
Waugh; Jacob M. ; et
al. |
March 1, 2007 |
COMPOSITIONS AND METHODS FOR TREATING ACNE
Abstract
This invention provides anti-acne kits that are useful for
treating acne, especially severe cases of acne. The anti-acne kits
include a vasoconstrictor and an anti-acne agent, and optionally
one or more of a skin lightening therapeutic, a sealing layer, a
skin cleanser, an astringent, a skin penetration enhancer, a
sunscreen, and nutritional supplements that promote healing of acne
lesions. This invention also provides methods for treating acne
using a vasoconstrictor in conjunction with an anti-acne agent.
Inventors: |
Waugh; Jacob M.; (Mountain
View, CA) ; Lee; Jane; (Union City, CA) |
Correspondence
Address: |
KING & SPALDING
1185 AVENUE OF THE AMERICAS
NEW YORK
NY
10036-4003
US
|
Assignee: |
REVANCE THERAPEUTICS, INC.
Mountain View
CA
|
Family ID: |
37054204 |
Appl. No.: |
11/278105 |
Filed: |
March 30, 2006 |
Related U.S. Patent Documents
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Application
Number |
Filing Date |
Patent Number |
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60666531 |
Mar 30, 2005 |
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Current U.S.
Class: |
424/61 ; 424/725;
424/74; 424/747; 424/757; 424/764; 424/769; 424/770; 514/159;
514/263.31; 514/568 |
Current CPC
Class: |
A61K 8/9789 20170801;
A61P 9/00 20180101; A61K 8/9794 20170801; A61K 36/61 20130101; A61Q
17/04 20130101; A61K 45/06 20130101; A61K 31/522 20130101; A61K
8/9761 20170801; A61Q 19/00 20130101; A61K 36/53 20130101; A61K
31/60 20130101; A61K 36/28 20130101; A61K 36/539 20130101; A61K
31/192 20130101; A61K 36/534 20130101; A61P 17/02 20180101; A61K
36/185 20130101; A61K 36/14 20130101; A61K 36/484 20130101; A61K
36/605 20130101; A61K 8/9767 20170801; A61P 17/00 20180101; A61K
8/922 20130101; A61Q 19/02 20130101; A61K 36/45 20130101; A61P
17/10 20180101; A61K 36/185 20130101; A61K 2300/00 20130101; A61K
36/28 20130101; A61K 2300/00 20130101; A61K 36/45 20130101; A61K
2300/00 20130101; A61K 36/484 20130101; A61K 2300/00 20130101; A61K
36/53 20130101; A61K 2300/00 20130101; A61K 36/534 20130101; A61K
2300/00 20130101; A61K 36/539 20130101; A61K 2300/00 20130101; A61K
36/605 20130101; A61K 2300/00 20130101; A61K 36/61 20130101; A61K
2300/00 20130101; A61K 31/192 20130101; A61K 2300/00 20130101; A61K
31/522 20130101; A61K 2300/00 20130101; A61K 31/60 20130101; A61K
2300/00 20130101; A61K 36/14 20130101; A61K 2300/00 20130101 |
Class at
Publication: |
424/061 ;
424/074; 424/725; 424/747; 424/764; 424/769; 424/770; 514/263.31;
514/159; 514/568; 424/757 |
International
Class: |
A61K 8/97 20060101
A61K008/97; A61K 31/60 20060101 A61K031/60; A61K 31/522 20060101
A61K031/522; A61K 31/192 20070101 A61K031/192; A61K 36/534 20060101
A61K036/534; A61K 36/48 20060101 A61K036/48; A61K 36/28 20060101
A61K036/28; A61K 36/13 20060101 A61K036/13 |
Claims
1. A kit for the treatment of acne, said kit comprising a
vasoconstrictor; an anti-acne agent; and optionally one or more
components selected from the group consisting of a skin-lightening
therapeutic, a skin cleanser, an astringent, a sun screen and a
sealing layer.
2. The kit according to claim 1, wherein said vasoconstrictor is
selected from the group consisting of tetrahydrozoline HCl 0.05%,
naphazoline HCl 0.03%, oxymetazoline HCl 0.025%, guava extract,
ellagic acid, caffeine, cypress oil, witch hazel, peppermint
extract, chamomile oil, and bugleweed.
3. The kit according to claim 1, wherein said anti-acne agent is
selected from the group consisting of benzoyl peroxide and
salicylic acid.
4. The kit according to claim 1, wherein said skin-lightening
therapeutic is selected from the group consisting of albatin,
arbutin, bearberry extract, mulberry extract, licorice extract,
skull cap, azelaic, ascorbyl glucosamine, magnesium ascorbyl
phosphate, ascorbic acid, coltsfoot extract, gallic acid, nutmeg,
ramulus mori extract, and kojic acid.
5. The kit according to claim 1, wherein said sealing layer
comprises mica.
6. A method of treating acne, said method comprising: applying a
vasoconstrictor; subsequently applying an anti-acne agent; and
optionally applying, after application of said anti-acne-agent, one
or more components selected from the group consisting of a
skin-lightening therapeutic, a skin cleanser, an astringent, a sun
screen and a sealing layer.
7. The method according to claim 6, wherein said vasoconstrictor is
selected from the group consisting of tetrahydrozoline HCl 0.05%,
naphazoline HCl 0.03%, oxymetazoline HCl 0.025%, guava extract,
ellagic acid, caffeine, cypress oil, witch hazel, peppermint
extract, chamomile oil, and bugleweed.
8. The method according to claim 6, wherein said anti-acne agent is
selected from the group consisting of benzoyl peroxide and
salicylic acid.
9. The method according to claim 6, wherein said skin-lightening
therapeutic is selected from the group consisting of albatin,
arbutin, bearberry extract, mulberry extract, licorice extract,
skull cap, azelaic, ascorbyl glucosamine, magnesium ascorbyl
phosphate, ascorbic acid, coltsfoot extract, gallic acid, nutmeg,
ramulus mori extract and kojic acid.
10. The method according to claim 6, wherein said sealing layer
comprises mica.
11. An anti-acne kit for treating acne occurring on sensitive skin,
said anti-acne kit comprising: a vasoconstrictor; an anti-acne
agent; and optionally one or more components selected from the
group consisting of a skin-lightening therapeutic, a skin cleanser,
an astringent, a sun screen and a sealing layer; wherein said
anti-acne agent is triclosan or an herbal extract.
Description
BACKGROUND OF THE INVENTION
[0001] Acne is a disease of the sebaceous hair follicles, often
called pores. At the base of each hair follicle is a gland called
the sebaceous gland, which produces sebum. Sebum is an oily
substance that keeps the skin moist and pliable, which under normal
circumstances travels along the hair follicle to the surface of the
skin. A blemish begins approximately 2-3 weeks before it appears on
the skin's surface. As the skin renews itself, the old cells die
and slough off. When cells are shed unevenly and clump together
with the sebum it forms a plug. Sebum which normally drains to the
surface gets blocked and bacteria begin to grow. The rapid growth
of the bacteria in combination with the accumulated sebum cause the
follicle to enlarge and result in a mild form of acne called
comedones, which are non-inflammatory. Both whiteheads and
blackheads start out as a "microcomedone" and then become skin
blemishes called comedones, either a whitehead or a blackhead. Acne
is trapped sebum and bacteria (propionibacterium acnes) growing in
a plugged follicle. Sebaceous glands are most numerous on the face,
chest, back, neck and scalp; consequently, these are the most
common sites of acne. The most common factors that cause acne are
hormones, increased sebum production, bacteria (Propionibacterium
Acnes), and changes inside of the hair follicle. Acne may progress
to an inflammatory type of acne lesions that are red in color
called papules, pustules and nodules.
[0002] There are many types of acne, ranging in severity from mild
to severely disfiguring. Acne vulgaris is the most common form of
acne which includes several types of pimples. These acne lesions
include blackheads, whiteheads, papules, pustules, nodules and
cysts.
[0003] Mild to moderate acne vulgaris is characterized by
whiteheads, blackheads, papules, and pustules. A whitehead is
formed when a pore is completely blocked, trapping sebum, bacteria,
and dead skin cells below the skin surface causing a white
appearance on the surface. Whiteheads are normally quicker in life
cycle than blackheads. A blackhead is formed when a pore is only
partially blocked, allowing some of the trapped sebum, bacteria,
and dead skin cells to drain to the surface slowly. The black color
is due to a reaction of the skin's own pigment, melanin, reacting
with the oxygen in the air. A blackhead tends to be a stable
structure. Blackheads can often take a long time to clear because
the contents very slowly drain to the surface. Papules are small,
red, tender bumps with no head. Papules are the earliest stage in
the development of what are normally considered the typical
"pimple". Papules are an intermediate in the progression of acne
between the non-inflammatory and inflammatory stages. Pustules are
similar to whiteheads, but are inflamed, and appear as a red circle
with a white or yellow center.
[0004] Severe acne vulgaris is characterized by nodules and cysts.
Nodular acne consists of acne spots which are much larger, can be
quite painful, and can sometimes last for months. Nodules are
large, hard bumps under the skin's surface. Scarring is common with
nodules. An acne cyst can appear similar to a nodule, but is
pus-filled, and can been described as having a diameter of 5 mm or
more across. They can be painful and scarring is common with cystic
acne.
[0005] Acne rosacea can look similar to the aforementioned acne
vulgaris, and the two types of acne are sometimes confused for one
another. Rosacea affects millions of people, most of whom are over
the age of 30. It appears as a red rash which is normally confined
to the cheeks, nose, forehead and chin. The redness is often
accompanied by bumps, pimples, and skin blemishes. Blood vessels
may also become more visible on the skin. Blackheads are not a part
of rosacea. It is more prevalent in women, but often more severe
when found in men. Left untreated, it can cause swelling of the
nose and the growth of excess tissue, a condition called
rhinophyma.
[0006] Acne conglobata is the most severe form of acne vulgaris and
is more common in males. It is characterized by numerous large
lesions, which are sometimes interconnected, along with widespread
blackheads. It can cause severe, irrevocable damage to the skin,
and disfiguring scarring. It is found on the face, chest, back,
buttocks, upper arms, and thighs. The age of onset for acne
conglobata is usually between 18 and 30 years, and the condition
can stay active for many years.
[0007] Acne fulminans is an abrupt onset of acne conglobata which
normally afflicts young men. Symptoms of severe nodulocystic, often
ulcerating acne are apparent. As with acne conglobata, extreme,
disfiguring scarring is common. Acne fulminans is unique in that it
also includes a fever and aching of the joints.
[0008] Gram-negative folliculitis is a bacterial infection
characterized by pustules and cysts, possibly occurring as a
complication resulting from a long term antibiotic treatment of
acne vulgaris. It is a rare condition, and prevalence in males
versus females is unknown.
[0009] Pyoderma Faciale is severe facial acne affects only females,
usually between the ages of 20 to 40 years old, and is
characterized by painful large nodules, pustules and sores which
may leave scarring. It begins abruptly, and may occur on the skin
of a woman who has never had acne before. It is confined to the
face, and usually does not last longer than one year, but can wreak
havoc in a very short time.
[0010] Teenage (adolescent) acne: Most cases of acne that require
treatment occur in individuals 9 to 19 years of age. Boys and girls
are equally affected but the condition is usually more severe in
boys. No ethnic groups are predisposed to acne, but certain
cosmetic practices, such as the use of oily grooming agents, can
lead to a specific pattern of lesions. Internal factors that may
cause adolescents acne include endogenous hormones (androgens,
progesterone) and specific drugs (oral contraceptives, isoniazid,
phenyloin, corticosteroids, lithium-containing compounds). External
factors include skin bacteria, especially Propionibacterium acnes;
industrial chemicals (petroleum, animal and vegetable oils); oil-
or wax-containing cosmetics; greasy sunscreen or suntan
preparations; and local pressure from objects such as headbands,
shoulder pads, or helmets. Excessive perspiration and emotional
stress can also aggravate acne. Androgens (e.g., testosterone) will
increase the size of sebaceous glands and, in people prone to acne,
increase the production of sebum. In women, fluctuations in
estrogen during the menstrual cycle change the sensitivity of
sebaceous glands to androgens. During puberty, the skin cells
lining the follicle shed more quickly, mix with the increased
levels of sebum and increase the likelihood of the pores becoming
clogged.
[0011] Adult acne: Twenty percent (20%) of the adult population is
afflicted by adult acne, most of them women. Modern-day job related
stress, pollution, poor nutrition and bad cosmetics are among the
major contributing factors. A common case of adult acne consists of
blackheads and whiteheads, while others developed inflamed acne
papules or pustules.
[0012] Approximately 85% of people worldwide suffer from acne at
some point in their lives, leading to more than 103 million
affected by acne at any given moment. Approximately 17 million
people in the U.S. have acne resulting in approximately 5.5 million
visits to the physicians each year.
[0013] Acne vulgaris occurs in up to 95% of the population in
westernized societies; acne vulgaris is a nearly universal skin
disease afflicting 79% to 95% of the adolescent population. In men
and women older than 25 years, 40% to 54% have some degree of
facial acne, and clinical facial acne persists into middle age in
12% of women and 3% of men. (Cordain L, Lindeberg S, Hurtado M,
Hill K, Eaton S B, Brand-Miller J. Acne vulgaris: a disease of
Western civilization. Arch Dermatol 2002 December;
138(12):1584-90).
[0014] Current medications include a variety of topical and
systemic medications such as antibiotics, anti-infectives,
anti-inflammatories, hormone therapies, keratolytics, and
retinoids. The over the counter medication include benzoyl peroxide
salicylic acid, sulfur, and resorcinolr
[0015] Benzoyl peroxide medication is very effective for killing
acne-causing bacteria. Benzoyl peroxide first saw use in the
1930's, and remains a mainstay of acne treatment because it has
proven itself to work well. To this day, benzoyl peroxide actually
kills propionibacterium acnes (P. Acnes) better than any other
medication on the market, prescription or otherwise. Benzoyl
peroxide is available in non-prescription concentrations of 2.5%,
5% and 10%.
[0016] Many anti-acne agents, including benzoyl peroxide, have a
high flux into the skin. While this penetration is advantageous
during the initial application, the rapid subsequent diffusion in
the skin means that the anti-acne agent will diffuse away from the
acne lesion to be treated (a phenomenon known as "outflow"). In
turn, this means that the efficacy of the anti-acne agent is
lessened, because of the relatively short dwell time of the
anti-acne agent in the area of the acne lesion. Thus, it would be
advantageous to have a method and a kit that would decrease the
outflow of the anti-acne agent from the area of the acne
lesion.
SUMMARY OF THE INVENTION
[0017] This invention provides methods and kits for treating acne,
especially severe cases of acne. The invention involves using a
vasoconstricting agent in conjunction with an anti-acne agent to
treat acne lesions. In preferred embodiments, the vasoconstricting
agent is applied prior to the anti-acne agent, and serves to reduce
the outflow of anti-acne agent from the treated acne lesion. The
vasoconstricting agent also simultaneously decreases the redness
and swelling of the acne lesion. Thus, the vasoconstricting agent
helps to conceal the acne lesion, while also helping to maintain a
higher concentration of anti-acne agent in the area of the acne
lesion. This, in turn, promotes healing and helps to prevent
further acne outbreaks.
[0018] In addition to a vasoconstricting agent and an anti-acne
agent, the kits of this invention may include components that
promote the healing of existing acne lesions and/or help to conceal
the acne lesions.
[0019] Accordingly, one object of this invention is to provide a
kit for the treatment of acne. The kit includes a vasoconstrictor
and an anti-acne agent, and optionally a skin lightening
therapeutic and/or a sealing layer.
[0020] Another object of this invention is to provide a method for
the treatment of acne. The method includes applying a
vasoconstrictor, following by an anti-acne agent. If desired, a
skin-lightening therapeutic and/or a sealing layer may be applied
as well.
DETAILED DESCRIPTION OF THE INVENTION
[0021] This invention treats acne, including severe cases of acne,
by enhancing the efficacy of topical anti-acne agents. The
invention involves applying a vasoconstricting agent to the acne
lesion, usually prior to the application of the anti-acne agent.
Without wishing to be bound by any particular scientific theory, it
is believed that the enhanced efficacy of a topical anti-acne agent
that is observed when used in conjunction with a vasoconstrictor
results from reduced outflow of the anti-acne agent from an acne
lesion. Thus, the local dermal dwell time of the anti-acne agent is
increased relative to the situation where no vasoconstrictor is
applied, so that a greater anti-acne effect is observed for a given
dosage of anti-acne agent. The vasoconstrictor also has the
beneficial effect of reducing the redness and swelling of the acne
lesion (usually within minutes after application), so as to help
conceal the acne lesion.
[0022] Accordingly, this invention provides an anti-acne kit for
treating acne. The anti-acne kit includes at least a
vasoconstrictor and an anti-acne agent. The anti-acne kit may
optionally contain a skin-lightening therapeutic to help conceal
the acne lesion and/or a sealing layer to minimize evaporation and
provide some degree of occlusion. Other components that may be a
part of the kit include compositions or patches that act as sealing
layers, skin cleansers, skin penetration enhancers, and nutritional
supplements. Different anti-acne kits can be tailored for spot
treatment versus more diffuse treatment, for different skin types,
and for night versus day treatment. The anti-acne kits according to
the invention can additionally be included as a part of a larger
kit or skin care regimen that includes tailored cleansers, toners,
balancers, moisturizers and/or various cosmetic or therapeutic
topicals.
Vasoconstrictors
[0023] The vasoconstrictors contemplated by the invention are not
particularly limited and include any compound that has
vasoconstricting properties and the ability to penetrate the skin.
In preferred embodiments, the inherent chemical properties of the
vasoconstrictor allow it to penetrate the skin easily. However,
this invention also contemplates modulating the ability of a
vasoconstrictor to penetrate the skin by combining the
vasoconstrictor with other components. For example, the skin
penetration ability of a vasoconstrictor with normally low
transdermal flux may be increased through the use of skin
penetration agents, as disclosed herein. On the other hand, if
desired, the skin penetration ability of the vasoconstrictor may be
intentionally decreased. For example, a vasoconstrictor may be
mixed with an appropriate emulsion that has the effect of slowing
the penetration of the vasoconstrictor.
[0024] Non-limiting examples of the vasoconstricting agents
contemplated by the invention include tetrahydrozoline HCl 0.05%,
naphazoline HCl 0.03%, oxymetazoline HCl 0.025%, guava extract,
ellagic acid, caffeine, cypress oil, hamamelis (witch hazel),
peppermint extract, chamomile oil, and bugleweed. Generally,
vasoconstrictors according to this invention may be dissolved in an
appropriate pharmaceutically or cosmetically acceptable solvent and
applied directly to the skin. However, in preferred embodiments,
the vasoconstrictors are combined with a cream or gel base, so that
application of the vasoconstrictor is more easily localized and
controlled. Any pharmaceutically or cosmetically acceptable gel or
cream bases may be used. Suitable gels include, for example,
cellulose-based gels, (e.g., hydroxyethyl cellulose (HEC),
hydroxypropyl cellulose (HPC), and carboxymethyl cellulose (CMC))
and acrylate copolymers. Suitable cream bases include emulsions
formed from a water phase of a humectant, a viscosity stabilizer
and water, an oil phase of fatty acid alcohol, a semi-solid
petroleum hydrocarbon and an emulsifying agent and a phase
containing the vasoconstrictor of the invention dispersed in an
aqueous stabilizer-buffer solution. If desired, stabilizers may be
added. Any conventional stabilizer can be utilized in accordance
with this invention. Cream-base pharmaceutical formulations
containing the vasoconstrictor may be composed of, for example,
aqueous emulsions containing a fatty acid alcohol, semi-solid
petroleum hydrocarbon, 1,2-ethyleneglycol and an emulsifying
agent.
[0025] While the vasoconstrictor itself aids in reducing the
swelling and redness associated with an acne lesion, the invention
also provides for skin-lightening therapeutics to decrease the
appearance of redness and discoloration further. These
skin-lightening therapeutics enhance the cosmetic concealing effect
of the vasoconstrictor and typically are applied after the
vasoconstrictor, although concurrent application with the
vasoconstrictor is also contemplated by the invention. By way of
example only, the skin lightening therapeutic may be albatin,
arbutin, bearberry extract, mulberry extract, licorice extract,
skull cap, azelaic, ascorbyl glucosamine, magnesium ascorbyl
phosphate, ascorbic acid, coltsfoot extract, gallic acid, nutmeg,
ramulus mori extract or kojic acid.
Anti-Acne Agents
[0026] The anti-acne kits according to this invention also include
a topical anti-acne agent. As used herein, an anti-acne agent is
any compound with antibacterial and/or anti-inflammatory properties
that kills the bacteria associated with acne and/or reduces the
inflammation of the acne lesion. Non-limiting examples of suitable
anti-acne agents include benzoyl peroxide, salicylic acid, glucose
oxidase, magnesium hydroxide, lactoperoxidase, pyridoxine
hydrochloride, magnesium gluconate, usnic acid, and triclosan. This
invention, however, also contemplates using anti-acne agents
derived from herbal extracts. Examples of suitable herbal extracts
include, but are not limited to eupatorium ayapana extract, fumaria
officinalis extract, oak root extract, spikenard, spilanthes
acmella extract, szechuan pepper, echium lycopsis extract,
lemongrass extract, oregano, orobanche cernua extract, terminalia
sericea, alkanna tinctoria extract, anise, barberry, calendula
extract, centella asiatica, chitosan, coriander, echinacea,
eucalyptus extract, farnesol, gentian violet extract, goldenseal,
grape seed extract, hoelen, hops, hyssop, labdanum oil,
lactoferrin, lentinus edodes extract, manuka oil, melaleuca
cajeputi oil, myrrh, niaouli oil, parietaria officinalis extract,
pine cone extract, ranunculus ficaria extract, red raspberry
extract, sea whip extract, soapwort, sulfur, thuja occidentalis
extract, vetiver oil or extract, ganoderma lucidum extract, witch
hazel, melilot, cucumber extract, aloe vera, aloe extract, areca
nut extract, green tea extract, grapefruit seed extract, black
cumin, garlic oil or extract, lavender extract, lemon peel extract,
walnut extract, amica extract, angelica root extract, bayberry
extract, echinacea, quassia extract, sage oil and extract, thyme
oil and extract, rosemary extract, ivy extract, sage extract,
sandalwood extract, nettle extract, bearberry extract, and licorice
extract.
[0027] In preferred embodiments, the anti-acne agent is applied
following the application of the vasoconstrictor. This sequence is
used in order to prevent the outflow of the anti-acne agent from
the area of the acne lesion. In some cases, the anti-acne agent is
applied immediately after the application of the vasoconstrictor.
However, in other cases, there is a delay period between the
application of the vasoconstrictor and the anti-acne agent.
Examples of suitable delay time includes anywhere from 15 seconds
to 30 minutes, more preferably between 45 seconds and 15 minutes,
and even more preferably between one minute and five minutes. Note,
however, that the invention is not restricted to sequential
application of the vasoconstrictor and the anti-acne agent. This
invention also contemplates concurrent application of the
vasoconstrictor and the anti-acne agent. An example where this
embodiment is useful is when the user does not have time to perform
multiple steps, and/or the outflow of the anti-acne agent is not
significant on the timescale that the vasoconstrictor takes
effect.
Sealing Layers
[0028] Certain embodiments of this invention provide for a topical
sealing layer after application of the anti-acne agent. This
optional sealing layer is used to seal the treated area and/or to
occlude it in order to improve tissue levels. For example, the
sealing layer may be a temporary occlusive barrier that acts as a
temporary patch for night treatment. The patch may contain, for
example, silicone, polytetrafluroethylene (PTFE), polyethylene
glycol (PEG), hydroxypropyl cellulose (HPC), petrolatum, or
acrylate copolymer.
[0029] Alternatively, the sealing layer may be a topically applied
emulsion that creates a protective barrier while providing a
cosmetic effect (for daytime treatment for example). A cosmetic
effect may be achieved, for example, if the emulsion includes an
agent capable of diffracting, refracting, or reflecting light (such
as mica) and/or if the emulsion is tinted to match the color of
unblemished skin. The cosmetic effect is beneficial because it
remains even after the effect of the vasoconstrictor has
abated.
Skin Cleanser
[0030] In certain embodiments of the invention, a skin cleanser is
used prior to the application of the vasoconstrictor. The skin
cleanser is used to reduce pro-acne factors, including excess oil,
bacteria, and dead skin that may clog pores.
[0031] Suitable skin cleansers are not particularly limited, and
may be any cosmetically acceptable cleanser. For example, the skin
cleanser can contain any anionic surfactant having a hydrophobic
moiety, such as a carbon chain having about 8 to about 30 carbon
atoms, and more preferably about 12 to about 20 carbon atoms, and
further having a hydrophilic moiety, such as sulfate, sulfonate,
carbonate, phosphate, or carboxylate. The hydrophobic carbon chain
may also be etherified, such as with ethylene oxide or propylene
oxide, to impart a particular physical property, such as increased
water solubility or reduced surface tension to the anionic
surfactant.
[0032] Non-limiting examples of suitable anionic surfactants
include alkyl sulfates, alkyl ether sulfates, alkyl ether
sulfonates, sulfate esters of an alkylphenoxy polyoxyethylene
ethanol, alpha-olefin sulfonates, beta-alkoxy alkane sulfonates,
alkylaryl sulfonates, alkyl monoglyceride sulfates, alkyl
monoglyceride sulfonates, alkyl carbonates, alkyl ether
carboxylates, fatty acids, sulfosuccinates, sarcosinates, octoxynol
or nonoxynol phosphates, taurates, fatty taurides, fatty acid amide
polyoxyethylene sulfates, isethionates, or mixtures thereof.
Additional anionic surfactants are listed in McCutcheon's
Emulsifiers and Detergents, 1993 Annuals, McCutcheon Division, MC
Publishing Co., Glen Rock; N.J., pp. 263-266, incorporated herein
by reference. Numerous other anionic surfactants, and classes of
anionic surfactants, are disclosed in Laughlin et al. U.S. Pat. No.
3,929,678, which is hereby incorporated herein by reference.
[0033] Appropriate anionic surfactants include a C.sub.8-C.sub.18
alkyl sulfate, a C.sub.8-C.sub.18 fatty acid salt, an ethoxylated
C.sub.8-C.sub.18 alkyl ether sulfate, a C.sub.8-C.sub.18 alkamine
oxide, a C.sub.8-C.sub.18 alkyl sarcosinate, a C.sub.8-C.sub.18
sulfoacetate, a C.sub.8-C.sub.18 sulfo succinate, a
C.sub.8-C.sub.18 alkyl diphenyl oxide disulfonate, a
C.sub.8-C.sub.18 alkyl carboxylate, a C.sub.8-C.sub.18 alpha-olefin
sulfonate, a methyl ester sulfonate, and mixtures thereof. The
C.sub.8-C.sub.18 alkyl group may be straight chain (e.g., lauryl)
or branched (e.g., 2-ethylhexyl). The cation of the anionic
surfactant can be an alkali metal (preferably sodium or potassium),
ammonium, C.sub.1-C.sub.4 alkylammonium (mono-, di-, tri), or
C.sub.1-C.sub.3 alkanolammonium (mono-, di-, and tri-).
[0034] Non-limiting examples of surfactants that are appropriate
for the skin cleanser of this invention include lauryl sulfates,
octyl sulfates, 2-ethylhexyl sulfates, lauramine oxide, decyl
sulfates, tridecyl sulfates, cocoates, lauroyl sarcosinates, lauryl
sulfosuccinates, linear C.sub.10 diphenyl oxide disulfonates,
lauryl sulfosuccinates, lauryl ether sulfates, myristyl sulfates,
oleates, stearates, tallates, cocamine oxide, decylamine oxide,
myristamine oxide, ricinoleates, cetyl sulfates, and similar
anionic surfactants.
[0035] The skin cleansers contemplated by this invention may also
be combined with exfoliating agents, in order to help reduce the
blockage of skin pores. Examples of suitable exfoliating agents
include fine silica particles and polymer microparticles.
Skin Penetration Enhancers
[0036] In certain embodiments of the invention, the area of skin
containing the acne lesion is treated with a penetration enhancer
during or immediately after the cleansing step in order to enhance
the penetration of the subsequently applied vasoconstrictor.
Suitable skin penetration enhancers include, for example,
surfactants such as sodium laurate, sodium lauryl sulfate,
cetyltrimethylammonium bromide, benzalkonium chloride, Poloxamer
(231, 182, 184), Tween (20, 40, 60, 80) and lecithin (U.S. Pat. No.
4,783,450); the 1-substituted azacycloheptan-2-ones, particularly
1-n-dodecylcyclazacycloheptan-2-one; alcohols such as ethanol,
propanol, octanol, benzyl alcohol, and the like; fatty acids such
as lauric acid, oleic acid and valeric acid; fatty acid esters such
as isopropyl myristate, isopropyl palmitate, methylpropionate, and
ethyl oleate; polyols and esters thereof such as propylene glycol,
ethylene glycol, glycerol, butanediol, polyethylene glycol, and
polyethylene glycol monolaurate; amides and other nitrogenous
compounds such as urea, dimethylacetamide (DMA), dimethylformamide
(DMF), 2-pyrrolidone, 1-methyl-2-pyrrolidone, ethanolamine,
diethanolamine and triethanolamine; terpenes; alkanones; organic
acids, particularly salicylic acid and salicylates, citric acid and
succinic acid.
Orally Administered Nutritional Supplements
[0037] This invention also contemplates using orally administered
nutritional supplements in conjunction with the anti-acne agents
disclosed herein. For example, the nutritional supplements may be
in the form of a multivitamin tablet or capsule that contains
vitamins and minerals known to promote wound healing. In
particularly preferred embodiments, such vitamins and minerals are
selected from the group consisting of vitamin A, B-vitamins,
vitamin C, vitamin E, and zinc. The specific form of the vitamin or
mineral is not limited, provided that it is pharmaceutically
acceptable. For example, vitamin A may be administered as vitamin A
palmitate or as beta-carotene. As another example, zinc may be
administered as zinc ascorbate or zinc amino acid chelate.
[0038] Other, non-vitamin supplements that are beneficial for wound
healing are also contemplated by the invention. Such non-vitamin
supplements include, for example, ornithine alpha-ketoglutarate
(OKG), glucosamine sulfate, chondroitin sulfate, aloe vera, gotu
kola extract, and echinacea.
Astringents
[0039] In certain embodiments of the invention, an astringent is
used to provide skin tightening or toning effect or to help reduce
sebum production or cleanse skin. In most cases, the astringent is
applied before the vasoconstrictor. The astringent may be used in
conjunction with, or in lieu of, the skin cleansers as described
herein. Non-limiting examples of astringents include zinc oxide,
zinc sulfate, calendula extract, sambucus extract, sandalwood
extract, oak bark extract, white lily extract, arnica extract,
plantain extract, St. John's wort extract, yarrow extract, sage
extract, passion fruit extract, walnut extract, chamomile extract,
cucumber extract, mulberry glycolic extract, gentian root extract,
lemon extract, rose bud extract, with hazel extract, comfrey
extract, geranium extract, mint extract, rosemary extract, myrrh
extract, apple extract, bayberry extract, bilberry extract, clary
sage extract, cornflower extract, cranesbill extract, hawthorn
extract, horse chestnut extract, raspberry concentrate, red
raspberry extract, rose oil and extract, horsetail extract, ivy
extract, birch bark extract, watercress extract, alfalfa extract,
bay oil, cabbage rose, citrus extract, dandelion extract,
goldenseal extract, hops extract, orange extract, tea tree oil,
aqleppo gall, areca nut extract, yarrow extract, elecampane, nettle
extract, eyebright extract, juniper oil, tamarind, kola extract,
lemongrass oil, rhubarb extract, olive leaf extract, sorrel
extract, sumac extract.
Analgesic Agents
[0040] In certain embodiments of the invention, an analgesic agent
is used to alleviate pain associated with acne lesions The
analgesic agent may be a separate component of the kits of this
invention, or it may be combined with other components. In some
embodiments, the analgesic agent is combined with the
vasoconstrictor to provide pain relief at the early stages of the
acne treatment. In other cases, however, the analgesic agent is
applied as a part of the sealing layer. Non-limiting examples of
analgesic agents include Indian olibanum, thorn apple extract,
kava-kava extract, Irvingia gabonensis kernel extract, Portulaca
Oleracea extract, poppy seeds, peppermint extract, tree tea oil,
Cannabis sativa (hemp) extract, Papaver somniferum extract,
Capsicum extract, and Salix (willobark) extract, clover leaf
extract, Coriander leaf extract, lemon balm extract, and rhizome
(ginger root) extract.
Sunscreen Agents
[0041] In certain embodiments of the invention, sunscreen agents
are used to protect skin from the sun by absorbing or blocking
harmful ultraviolet radiation or to help reduce damages from
prolong sun exposure or to prevent sunburns. Furthermore, sunscreen
agents can be combined with anti-inflammatory agents such as aloe
vera and cucumber. Generally, the sunscreen agents are applied
after the anti-acne agent, although this sequence is not limiting.
Examples of sunscreen agents contemplated by the invention include,
but are not limited to, PABA, benzophenone, avobenzone, homosalate,
octinoxate, octisalate, oxybenzone, titanium dioxide, aminobenzoic
acid, padimate, octocrylene, octyl salicylate, octyl
methoxycinnamate, dioxybenzone, menthyl anthranilate, lisadimate,
phenylbenzimidazole, sulisobenzone, zinc oxide, trolamine
salicylate, roxadimate, bumetrizole, octocrylene, Tinosorb S,
Tinosorb M, azelaic acid, vitamin C, kinetin, horse chestnut bark
extract, aleppo gall, shea butter, kukui nut oil, everlasting oil,
aesculin, kojic acid, karite butter, titanium oxide, magnesium
silicate, kalin, ferric oxide, red petrolatum, and magnesium
oxide.
EXAMPLES
Example 1
Two-Step Acne Treatment
[0042] This example provides a two step treatment for acne. The
first step involves topically applying a vasoconstricting
composition to the acne lesion to be treated. Suitable
vasoconstricting compositions include tetrahydrozoline HCl 0.05%,
naphazoline HCl 0.03%, or oxymetazoline HCl 0.025% in an aqueous
base containing HPC to increase the viscosity for ease of
application. Upon application of the vasoconstricting composition,
the redness and swelling of the acne lesion diminishes, making the
acne lesion less noticeable. After about 5 minutes, a second step
is performed which involves topically applying 5% benzoyl peroxide
5% in an oil-in water moisturizer base. In this example, the
benzoyl peroxide 5% is tinted to match the skin tone of the user,
but this tinting is optional. Within two days, the acne lesion has
healed substantially.
Example 2
Three-Step Acne Treatment for Nighttime Use
[0043] This example provides a three-step nighttime treatment for
acne. The first step involves topically applying a vasoconstricting
composition to the acne lesion to be treated. Suitable
vasoconstricting compositions include tetrahydrozoline HCl 0.05%,
naphazoline HCl 0.03%, or oxymetazoline HCl 0.025% in an aqueous
base containing HPC to increase the viscosity for ease of
application. Upon application of the vasoconstricting composition,
the redness and swelling of the acne lesion diminishes, making the
acne lesion less noticeable. After about 5 minutes, a second step
is performed which involves topically applying 5% benzoyl peroxide
in an oil-in water moisturizer base. The acne lesion is then
covered with a patch that includes silicone on the skin-side of the
patch. The patch remains in place overnight and is removed in the
morning.
[0044] The following night, the three-step acne treatment is
repeated. Noticeable improvement in the acne lesion is observed
within two days of the initial treatment.
Example 3
Three-Step Acne Treatment for Daytime Use
[0045] This example provides a three-step acne treatment that is
suitable for daytime use. The first step involves topically
applying a vasoconstricting composition to the acne lesion to be
treated. Suitable vasoconstricting compositions include
tetrahydrozoline HCl 0.05%, naphazoline HCl 0.03%, or oxymetazoline
HCl 0.025% in an aqueous base containing HPC to increase the
viscosity for ease of application. Upon application of the
vasoconstricting composition, the redness and swelling of the acne
lesion diminishes, making the acne lesion less noticeable. After
about 5 minutes, a second step is performed which involves
topically applying 5% benzoyl peroxide in an oil-in-water
moisturizer base. Next, a water-in-oil moisturizer is applied to
minimize evaporation and to help occlude the area.
[0046] This treatment is repeated twice daily. Significant healing
of the acne lesion is noted after two days.
Example 4
Three-Step Daytime Acne Treatment with Mica and Optional
Tinting
[0047] This example provides a three-step daytime acne treatment
that ingredients for making the acne lesions less noticeable. The
first step involves topically applying a vasoconstricting
composition to the acne lesion to be treated. Suitable
vasoconstricting compositions include tetrahydrozoline HCl 0.05%,
naphazoline HCl 0.03%, or oxymetazoline HCl 0.025% in an aqueous
base containing HPC to increase the viscosity for ease of
application. Upon application of the vasoconstricting composition,
the redness and swelling of the acne lesion diminishes, making the
acne lesion less noticeable. After about 5 minutes, a second step
is performed which involves topically applying 5% benzoyl peroxide
in an oil-in-water moisturizer base. Next, a water-in-oil
moisturizer is applied to minimize evaporation and to help occlude
the area. The water-in-oil moisturizer contains mica to provide
cosmetic reduction of the appearance of the acne blemish by
interfering with light passing to or from the lesion. Tinting
compounds are also present to help conceal the acne lesion, but
these compounds are optional.
[0048] This treatment is repeated twice daily. Significant healing
of the acne lesion is noted after two days.
Example 5
Three-Step Daytime Acne Treatment plus Cleanser
[0049] A skin cleanser to may be used prior to the acne treatment
disclosed in Example 3. Generally, the skin cleanser is tailored to
be appropriate to the skin type and anatomic location. In this
example, the skin cleanser is a decyl sulfate-based skin cleanser
that reduces pro-acne components by removing excess skin oils. The
skin cleanser may also contain triethanolamine as a penetration
enhancer that increase the permeability of skin, thereby enhancing
the penetration of the vasoconstrictor and other components of the
anti-acne treatment.
Example 6
Three-Step Daytime Spot Treatment with Cleanser and Moisturizer
[0050] The anti-acne treatment disclosed in Example 5 can be used
in conjunction with a moisturizer to improve skin hydration,
suppleness or appearance, or to decrease tendency to form new acne
lesions in unaffected areas. This moisturizer optionally may have
pigment added for cosmetic benefit. Typically, the cleanser is
first applied, followed by the vasoconstrictor and anti-acne agent.
Next, the moisturizer is applied to soften the skin while helping
to occlude the area. The treatment may be repeated twice daily to
obtain noticeable improvement in skin softness and reduction in
severity of acne lesions.
Example 7
Three-Step Daytime Acne Treatment and Moisturizer with
Sunscreen
[0051] The anti-acne treatment disclosed in Example 3 can be used
in conjunction with a moisturizer with sunscreen to protect skin
from damaging UV rays of the sun and to improve skin hydration,
suppleness or appearance, or to decrease tendency to form new acne
lesions in unaffected areas. This moisturizer optionally may have
pigment added for cosmetic benefit. Typically, a vasoconstricting
composition is topical applied and then anti-acne agent. Next, a
water-in-oil moisturizer with 7.5% octinoxate (octyl
methoxycinnamate) and 3.0% zinc oxide with vitamin C and cucumber
extract is applied to provide sun protection. The treatment may be
repeated twice daily to obtain noticeable improvement in skin
softness and reduction in severity of acne lesions. The moisturizer
with sunscreen may be used before sun exposure each morning and
throughout the day.
Example 8
Three-Step Daytime Treatment with Mica and Oral Vitamins
[0052] The anti-acne treatment described herein can be used in
conjunction with nutritional supplements that speed the healing of
acne lesions or prevent new acne lesions from forming. The
nutritional supplements may be, for example, oral multivitamins. In
this particular example, the anti-acne treatment of Example 3 is
used in conjunction with zinc and Vitamins C and A, supplements
that are well known for their promotion of wound healing. An oral
multivitamin containing 10 mg of zinc amino acid chelate, 250 mg of
ascorbic acid (Vitamin C), and 5000 IU of beta-carotene (vitamin A)
is taken daily in conjunction with the use of the anti-acne
treatment of Example 3. Noticeable improvement in the acne lesions
is observed after two days.
Example 9
Anti-Acne Treatment for Sensitive Skin
[0053] This example provides an anti-acne treatment for sensitive
skin. The treatment includes a vasoconstricting composition
containing oxymetazoline HCl 0.025% with guava extract and witch
hazel in an aqueous base containing acrylate copolymer to increase
the viscosity. The vasoconstricting composition is applied
topically to an acne lesion to be treated. Upon application, the
redness and swelling of the lesion decreases as the blood vessels
in the treated region are constricted. For this particular
sensitive-skin acne treatment, the anti-acne agent is triclosan,
rather than benzoyl peroxide, because about 10% of the population
experiences skin allergies when benzoyl peroxide is topically
applied. Note, however, that any anti-acne agent not containing
benzoyl peroxide may be used. The anti-acne agent is applied about
15 minutes after the initial application of the vasoconstricting
composition. Optionally, a third component containing a concealing
agent (such as mica) or tinting is applied.
Example 10
Two-Step Day Acne Treatment
[0054] This example provides a two-step acne treatment. In the
first step, a composition containing oxymetazoline HCl 0.025% with
guava extract and witch hazel in an aqueous base is topically
applied to the acne lesion to be treated. The viscosity of the
composition is increased with HPC to form a creamy or gel-like base
for ease of application. The vasoconstrictors applied in the first
step decrease the redness and swelling of acne lesion, and help to
reduce the diffusion of subsequently applied anti-acne agent from
the lesion. In the second step, which is performed about 15 minutes
after the first step, a composition that contains 5% benzoyl
peroxide (an anti-acne agent) in a base containing water-in-oil
moisturizer with 5% grapeseed extract is applied to the acne
lesion. The base also contains mica and is optionally tinted to
mask the reappearance of the lesion as the vasoconstrictors in the
first step wear off.
Example 11
Three-Step Daytime Acne Treatment
[0055] This example provides a three step acne treatment. In the
first step, a composition containing tetrahydrozoline HCl 0.05%,
guava extract, and witch hazel in an aqueous base is applied
topically to the acne lesion to be treated. The viscosity of the
composition is adjusted with HPC to form a creamy or gel-like base
for ease of application. The vasoconstrictors applied in the first
step decrease the redness and swelling of acne lesion, and help to
reduce the diffusion of subsequently applied anti-acne agent from
the lesion. In the second step, which is performed about 15 minutes
after the first step, a composition that contains 5% benzoyl
peroxide (as an anti-acne agent) in a water-in-oil moisturizer
containing 5% grapeseed extract is applied to the acne lesion. To
increase flux of the anti-acne agent into the lesion, the third
step of the treatment involves subsequently applying a water-in-oil
moisturizer that help to prevent evaporation and that provides some
degree of occlusion. The water-in-oil moisturizer contains mica and
optionally may be tinted to help conceal the acne lesion.
* * * * *