Methods and compositions suitable for treating acne
A composition of glycolic acid, gluconolactone, and mandelic acid, combined with a salt-tolerant thickening polymer, effectively treats acne by reducing lesions and killing P. acnes bacteria within biofilms, addressing the ineffectiveness and tolerance issues of existing treatments.
Patent Information
- Authority / Receiving Office
- JP · JP
- Patent Type
- Patents
- Current Assignee / Owner
- Filing Date
- 2021-08-13
- Publication Date
- 2026-03-03
AI Technical Summary
Existing treatments for acne are not universally effective and often not well tolerated by the skin, necessitating a need for improved compositions that effectively treat acne while being skin-friendly.
A composition comprising glycolic acid, gluconolactone, and mandelic acid, with a total amount of these acids less than 15% by weight, along with a salt-tolerant thickening polymer, is applied to the skin to treat acne and disrupt biofilms formed by Propionibacterium acnes bacteria.
The composition effectively reduces acne lesions, improves skin texture, and increases skin clarity while being well tolerated, with the ability to penetrate and kill P. acnes bacteria within biofilms.
Smart Images

Figure 0007823026000001 
Figure 0007823026000002 
Figure 0007823026000003
Abstract
Description
[Technical Field]
[0001] FIELD OF THE INVENTION Aspects of the present invention relate generally to compositions suitable for treating acne, particularly compositions comprising alpha hydroxy acids and polyhydroxy acids. [Background technology]
[0002] Acne disorders are often classified as non-inflammatory or inflammatory types. Non-inflammatory acne is characterized by closed comedones (milia) and open comedones (blackheads), which consist of dense masses of keratin, sebum, and bacteria that dilate the follicular duct. Comedones form when the pilosebaceous duct is blocked and / or when sebaceous glands produce increased sebum. The formation of comedones can be followed by inflammation due to bacterial proliferation and / or excessive sebum production. Typically, the bacteria are anaerobic bacteria such as Propionibacterium acnes (formerly Propionibacterium acnes). Inflammatory acne is characterized by papules (pimples), pustules, and nodulocystic lesions, which may lead to scarring. Several factors are thought to play important roles in the pathogenesis of acne, including sebum production, hormonal stimulation, clogged pores, and skin pathogens. Sebum levels are increased by approximately 70% in subjects with acne compared to those in control subjects. Summary of the Invention [Problem to be solved by the invention]
[0003] Although many treatments and products have been tried to treat acne, no treatment has been found to be universally effective, and therefore there remains a need for additional treatments. Furthermore, there continues to be a need to identify acne treatments that are not only effective but also well tolerated by the skin. [Means for solving the problem]
[0004] One aspect of the present invention is a composition for treating acne, comprising: a. about 0.1% by weight to about 7.5% by weight of glycolic acid; b. about 0.1% to about 5% by weight of gluconolactone; c. about 0.1% to about 5% by weight of mandelic acid; d. glycol, e. a salt-tolerant thickening polymer; wherein the total amount of glycolic acid, gluconolactone, and mandelic acid is less than about 15% by weight of the total composition. In one or more embodiments, the total amount of glycolic acid, gluconolactone, and mandelic acid is at least about 2% by weight of the total composition. In some embodiments, the glycol is selected from the group consisting of glycerin, propylene glycol, butylene glycol, pentylene glycol, hexylene glycol, polyethylene glycol, polypropylene glycol, diethylene glycol, triethylene glycol, caprylyl glycol, glycerol, butanediol, and hexanetriol, as well as copolymers and combinations thereof. In one or more embodiments, the composition is in the form of a lotion. In one or more embodiments, the composition is in the form of a lotion. In one or more embodiments, the composition is in the form of a gel. In some embodiments, the composition has a rheometer viscosity of about 2,000 to about 18,000 cPs at 22°C. In one or more embodiments, the composition has a rheometer viscosity of about 8,000 to about 10,000 cPs at 22°C. In some embodiments, the composition has a pH of about 3 to about 5. In one or more embodiments, the composition further comprises about 0.5% to about 5% by weight of salicylic acid. In some embodiments, the composition is substantially free of salicylic acid. In one or more embodiments, the composition is substantially free of lactic acid. In some embodiments, the salt-tolerant thickening polymer comprises sulfonate, acrylate, and / or cellulose moieties. In one or more embodiments, the salt-tolerant thickening polymer is selected from the group consisting of polyacrylate crosspolymer-6, hydroxyethyl acrylate / sodium acryloyldimethyl taurate copolymer, and combinations thereof. In some embodiments, the salt-tolerant thickening polymer comprises hydroxyethyl cellulose.
[0005] Another aspect of the present invention is a composition for treating acne, comprising: a. about 2.5% by weight to about 7.5% by weight of glycolic acid; b. about 1% to about 5% by weight of gluconolactone; c. about 1% to about 5% by weight of mandelic acid; d. about 2.5% to about 7.5% by weight of propylene glycol; e. about 0.5% to about 2% by weight of polyacrylate crosspolymer-6; f. about 0.5% to about 2% by weight of hydroxyethyl acrylate / sodium acryloyldimethyltaurate copolymer; wherein the total amount of glycolic acid, gluconolactone, and mandelic acid is less than about 12% by weight of the total composition. In one or more embodiments, the composition is in the form of a lotion. In one or more embodiments, the composition is in the form of a gel. In some embodiments, the composition has a rheometer viscosity of about 2,000 to about 18,000 cPs at 22°C. In one or more embodiments, the composition has a rheometer viscosity of about 8,000 to about 10,000 cPs at 22°C. In some embodiments, the composition has a pH of about 3 to about 5. In one or more embodiments, the composition further comprises about 0.5% to about 5% by weight of salicylic acid. In some embodiments, the composition is substantially free of lactic acid.
[0006] Another aspect of the present invention relates to a method for treating acne, comprising contacting skin in need of such treatment with a composition comprising a first alpha hydroxy acid, a second alpha hydroxy acid, and a polyhydroxy acid. In one or more embodiments, the first alpha hydroxy acid comprises glycolic acid, the second hydroxy acid comprises mandelic acid, and the polyhydroxy acid comprises gluconolactone. In some embodiments, the total amount of glycolic acid, gluconolactone, and mandelic acid is less than about 15% by weight of the total composition. In one or more embodiments, the total amount of acid in the composition is less than about 15% by weight of the total composition. In some embodiments, the composition is left on the skin. In one or more embodiments, the composition is in the form of a lotion. In some embodiments, the composition has a pH of about 3 to about 5. In one or more embodiments, the composition further comprises a glycol selected from the group consisting of glycerin, propylene glycol, butylene glycol, pentylene glycol, hexylene glycol, polyethylene glycol, polypropylene glycol, diethylene glycol, triethylene glycol, caprylyl glycol, glycerol, butanediol, and hexanetriol, and copolymers and combinations thereof. In some embodiments, the composition is substantially free of lactic acid. In one or more embodiments, the composition is substantially free of salicylic acid.
[0007] Another aspect of the present invention relates to a method of treating acne, the method comprising: treating skin in need of such treatment with a. about 0.1% by weight to about 7.5% by weight of glycolic acid; b. about 0.1% to about 5% by weight of gluconolactone; c. about 0.1% to about 5% by weight of mandelic acid; d. glycol, e. a salt-tolerant thickening polymer; wherein the total amount of glycolic acid, gluconolactone, and mandelic acid is less than about 15% by weight of the total composition. In some embodiments, the total amount of acids in the composition is less than about 15% by weight of the total composition. In one or more embodiments, the composition is left on the skin. In some embodiments, the composition is in the form of a lotion. In one or more embodiments, the composition has a pH of about 3 to about 5. In some embodiments, the composition further comprises a glycol selected from the group consisting of glycerin, propylene glycol, butylene glycol, pentylene glycol, hexylene glycol, polyethylene glycol, polypropylene glycol, diethylene glycol, triethylene glycol, caprylyl glycol, glycerol, butanediol, and hexanetriol, and copolymers and combinations thereof. In one or more embodiments, the composition is substantially free of lactic acid. In some embodiments, the composition is substantially free of salicylic acid. In one or more embodiments, the salt-tolerant thickening polymer comprises an acrylate and / or cellulose moiety. In some embodiments, the salt-tolerant thickening polymer is selected from the group consisting of polyacrylate crosspolymer-6, hydroxyethyl acrylate / sodium acryloyldimethyltaurate copolymer, and combinations thereof.
[0008] Another aspect of the present invention relates to a method for disrupting a biofilm or killing bacteria contained therein, the method comprising applying a composition comprising a first alpha hydroxy acid, a second alpha hydroxy acid, and a polyhydroxy acid to a surface having a biofilm. In one or more embodiments, the surface is a surface on skin. In some embodiments, the skin has acne. In one or more embodiments, the biofilm contains Propionibacterium acnes bacteria. In some embodiments, the first alpha hydroxy acid comprises glycolic acid, the second hydroxy acid comprises mandelic acid, and the polyhydroxy acid comprises gluconolactone. In one or more embodiments, the total amount of glycolic acid, gluconolactone, and mandelic acid is less than about 15% by weight of the total composition. In some embodiments, the total amount of acid in the composition is less than about 15% by weight of the total composition. In one or more embodiments, the composition is in the form of a lotion. In some embodiments, the composition has a pH of about 3 to about 5. In one or more embodiments, the composition further comprises a glycol selected from the group consisting of glycerin, propylene glycol, butylene glycol, pentylene glycol, hexylene glycol, polyethylene glycol, polypropylene glycol, diethylene glycol, triethylene glycol, caprylyl glycol, glycerol, butanediol, and hexanetriol, and copolymers and combinations thereof. In some embodiments, the composition is substantially free of lactic acid. In one or more embodiments, the composition is substantially free of salicylic acid.
[0009] Another aspect of the invention relates to a method of disrupting a biofilm or killing bacteria contained in a biofilm, comprising applying to a surface having a biofilm a composition comprising: a. about 0.1% by weight to about 7.5% by weight of glycolic acid; b. about 0.1% to about 5% by weight of gluconolactone; c. about 0.1% to about 5% by weight of mandelic acid; d. glycol, e. a salt-tolerant thickening polymer; wherein the total amount of glycolic acid, gluconolactone, and mandelic acid is less than about 15% by weight of the total composition, the composition has a pH of about 3 to about 5, and the surface is a surface on skin. In some embodiments, the skin has acne. In one or more embodiments, the biofilm contains Propionibacterium acnes bacteria. In some embodiments, the total amount of acids in the composition is less than about 15% by weight of the total composition. In one or more embodiments, the composition further comprises a glycol selected from the group consisting of glycerin, propylene glycol, butylene glycol, pentylene glycol, hexylene glycol, polyethylene glycol, polypropylene glycol, diethylene glycol, triethylene glycol, caprylyl glycol, glycerol, butanediol, and hexanetriol, and copolymers and combinations thereof. In some embodiments, the composition is substantially free of lactic acid. In one or more embodiments, the composition is substantially free of salicylic acid. In some embodiments, the salt-tolerant thickening polymer is selected from the group consisting of polyacrylate crosspolymer-6, hydroxyethyl acrylate / sodium acryloyldimethyltaurate copolymer, and combinations thereof. DETAILED DESCRIPTION OF THE INVENTION
[0010] definition "Treating acne" means reducing or preventing acne or rosacea.
[0011] By "product" is meant a product in its finished packaged form. In one embodiment, the package is a container, such as a plastic, metal, or glass tube or jar, that contains the composition. The product may further include additional packaging, such as a plastic or cardboard box for storing such a container. In one embodiment, the product includes instructions instructing the user to apply the composition to (i) treat acne, or (ii) reduce the appearance of oil or pores on the skin.
[0012] "Promotion" means promotion, advertising, or marketing. Examples of promotion may include, but are not limited to, written, visual, or verbal messages on a product, in a store, in magazines, newspapers, radio, television, the Internet, etc.
[0013] To facilitate the treatment of acne, examples of such statements include, but are not limited to, "treat acne," "treating acne," "prevent acne," "reduce acne lesions, comedones, or pimples," "reduce the appearance of acne lesions, comedones, or pimples," "reduce acne outbreaks and the appearance of acne," "prevent, control, or regulate acne outbreaks and the appearance of acne," and "reduce the occurrence and appearance of acne."
[0014] To promote a reduction in the appearance of oil on the skin, examples of such statements include, but are not limited to, "reduces the appearance of sebum," "prevents, controls or regulates sebum production," "reduces sebum," "reduces the appearance of oily / shiny skin," "reduces the appearance of oily skin," and "reduces shine on the skin, hair, or scalp." In one embodiment, the composition is applied to skin not requiring treatment for acne (i.e., skin or scalp / hair not affected by acne).
[0015] To promote the reduction of the appearance of pores on the skin, examples of such statements include, but are not limited to, "reducing pore size," "minimizing the appearance of pores," "improving the appearance of pores," "reducing the visibility of pores," and "closing the opening of pores." In one embodiment, the composition is applied to skin not requiring treatment for acne (i.e., skin not affected by acne).
[0016] As used herein, "administering to the skin" or "contacting the skin" means contacting (e.g., by hand or by use of an applicator such as, but not limited to, a wipe, tube, roller, spray, or patch) an area of skin requiring such treatment or an area of skin adjacent to an area of skin requiring such treatment.
[0017] As used herein, "composition" means a composition suitable for topical administration to the skin.
[0018] As used herein, "cosmetically acceptable" means that the ingredient it describes is suitable for use in contact with the skin without undue toxicity, incompatibility, instability, irritation, allergic reaction, etc.
[0019] As used herein, a "safe and effective amount" means an amount of a compound, carrier, or composition that is sufficient to induce increased tissue elasticity, but low enough to avoid unwanted adverse side effects. A safe and effective amount of a compound or composition will vary depending on factors such as the area to be treated, the age, health, and skin type of the end user, the duration and nature of the treatment, the particular compound or composition administered, and the particular cosmetically acceptable carrier utilized.
[0020] The articles "a," "an," and "the" all refer to the plural as well as the singular.
[0021] The term "one or more" is synonymous with "at least one" and includes individual components as well as mixtures / combinations.
[0022] Other than in the examples, or where otherwise indicated, all numbers expressing quantities of ingredients and / or reaction conditions should be understood to be modified in all instances by the term "about," meaning within + / - 5% of the stated number.
[0023] All percentages, parts and ratios herein are based on the total weight of the compositions of the present disclosure unless otherwise indicated.
[0024] As used herein, unless otherwise indicated, "substantially free" or "essentially free" means that the component is added to the composition at less than about 2% by weight, based on the total weight of the composition. The composition may contain less than about 1, 0.5, or 0.1% by weight, or may be free of the component.
[0025] All publications and patent applications cited herein are hereby incorporated by reference for all purposes to the same extent as if each individual publication or patent application was specifically and individually indicated to be incorporated by reference. The present disclosure controls if there is a conflict between the present disclosure and any incorporated publication or patent.
[0026] Methods, Uses and Compositions Various aspects of the present invention relate to methods and compositions suitable for treating acne. In one or more embodiments, the method involves treating skin in need of such treatment with a composition comprising two alpha hydroxy acids and a polyhydroxy acid. That is, in some embodiments, the present invention relates to the use of a composition comprising two alpha hydroxy acids and one polyhydroxy acid for the treatment of acne. Surprisingly, it has been discovered that a combination of these three acids (particularly a blend of glycolic acid, gluconolactone, and mandelic acid) is effective in treating acne. In particular, it has been surprisingly discovered that these three acids can improve acne conditions (e.g., reducing acne lesions, improving skin texture, increasing skin clarity and uniformity, etc.) while being well tolerated by the skin.
[0027] Furthermore, recent evidence suggests that acne may be associated with the formation of skin biofilms by certain bacteria (e.g., Propionibacterium acnes). Accordingly, another aspect of the present invention relates to a method for disrupting a biofilm or killing bacteria contained in a biofilm. As used herein, the term "disrupting a biofilm" means that at least a portion of the bacteria in the biofilm are killed, such that the biofilm matrix degrades, disperses, or disintegrates over time. In some embodiments, the biofilm matrix can be degraded during or immediately after exposure of the biofilm to one or more compositions. The method includes applying a composition comprising a first alpha hydroxy acid, a second alpha hydroxy acid, and a polyhydroxy acid to a surface bearing a biofilm (e.g., skin affected by acne). Surprisingly, it has been discovered that a combination of these three acids (particularly a blend of glycolic acid, gluconolactone, and mandelic acid) is effective in killing Propionibacterium acnes. In particular, it has been surprisingly discovered that these three acids are not only capable of killing P. acnes, but also capable of disrupting biofilms formed by P. acnes or otherwise penetrating the biofilm matrix and killing P. acnes in the biofilm.
[0028] Alpha hydroxy acids are compounds containing carboxylic acids substituted with hydroxyl groups on adjacent carbon atoms. Examples of alpha hydroxy acids include, but are not limited to, glycolic acid, malic acid, tartaric acid, uric acid, mandelic acid, or any combination of any of the foregoing. Each of the alpha hydroxy acids may be present in an amount ranging from about 0.1, 0.2, 0.3, 0.4, 0.5, 0.6, 0.7, 0.8, 0.9, 1.0, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, or 5.5 to about 5, 5.5, 6, 6.5, 7, or 7.5% by weight of the total composition.
[0029] In one or more embodiments, at least one of the alpha hydroxy acids comprises glycolic acid. In some embodiments, at least one of the alpha hydroxy acids comprises mandelic acid. In further embodiments, the composition comprises a blend of glycolic acid and mandelic acid. Glycolic acid is the smallest alpha hydroxy acid and has the molecular formula C2H4O3. Glycolic acid is individually well known in the art and is readily available from a variety of commercial sources. Glycolic acid may be present in the composition in an amount ranging from about 0.1, 0.2, 0.3, 0.4, 0.5, 0.6, 0.7, 0.8, 0.9, 1.0, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, or 5.5 to about 5, 5.5, 6, 6.5, 7, or 7.5 wt.% of the total composition. Mandelic acid is an aromatic alpha hydroxy acid and has the molecular formula CHCH(OH)COH. Mandelic acid is individually well known in the art and readily available from a variety of commercial sources. Mandelic acid may be present in the composition in an amount ranging from about 0.1, 0.2, 0.3, 0.4, 0.5, 0.6, 0.7, 0.8, 0.9, 1.0, or 1.5 to about 1.5, 2, 2.5, 3, 3.5, 4, 4.5, or 5% by weight of the total composition.
[0030] Polyhydroxy acids are acids with multiple hydroxyl groups that can often act as moisturizers, anti-irritants, and hydrating agents. Examples of polyhydroxy acids include, but are not limited to, gluconic acid lactones and aldonic acid lactones, such as alonolactone, altronolactone, gluconolactone, glucoheptonolactone, mannolactone, gulonolactone, idonolactone, galactonolactone, talonolactone, lactobionic acid, maltobionic acid, and tartaric acid. In some embodiments, the polyhydroxy acid comprises gluconolactone. Gluconolactone has the molecular formula CH 10Gluconolactone is a polyhydroxy acid having a hydroxyl group of 0.06. Gluconolactone is individually well known in the art and is readily available from a variety of commercial sources. The polyhydroxy acid (e.g., gluconolactone) may be present in the composition in an amount ranging from about 0.1, 0.2, 0.3, 0.4, 0.5, 0.6, 0.7, 0.8, 0.9, 1.0, or 1.5 to about 1.5, 2, 2.5, 3, 3.5, 4, 4.5, or 5 by weight of the total composition.
[0031] In one or more embodiments, the total amount of alpha hydroxy acids and polyhydroxy acids is less than about 15, 14.5, 14, 13.5, 13, 12.5, 12, 11, or 10.5% by weight of the total composition, hi some embodiments, the total amount of alpha hydroxy acids and polyhydroxy acids is at least about 2, 2.5, 3, 3.5, 4, 4.5, 5, 5.5, 6, 6.5, 7, 7.5, 8, 8.5, 9, 9.5, or 10% by weight of the total composition.
[0032] In some embodiments, the composition comprises glycolic acid, mandelic acid, and gluconolactone as the alpha hydroxy acid and polyhydroxy acid. In one or more embodiments, the total amount of glycolic acid, gluconolactone, and mandelic acid is less than about 15, 14.5, 14, 13.5, 13, 12.5, 12, 11, or 10.5% by weight of the total composition. In some embodiments, the total amount of glycolic acid, gluconolactone, and mandelic acid is at least about 2, 2.5, 3, 3.5, 4, 4.5, 5, 5.5, 6, 6.5, 7, 7.5, 8, 8.5, 9, 9.5, or 10% by weight of the total composition.
[0033] In some embodiments, the composition further comprises a beta-hydroxy acid. Exemplary beta-hydroxy acids include, but are not limited to, salicylic acid, beta-hydroxybutanoic acid, tropic acid, and trethocanic acid. Other suitable beta-hydroxy acids are described in 5665776 (Yu). In some embodiments, the composition comprises salicylic acid as the beta-hydroxy acid. When present, the beta-hydroxy acid may be present in an amount ranging from about 0.1, 0.2, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, or 3 to about 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, or 5% by weight. In some embodiments, the salicylic acid may be present in an amount ranging from about 0.1, 0.2, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, or 3 to about 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, or 5% by weight.
[0034] In one or more embodiments, the composition may comprise less than 0.6, 0.5, 0.4, 0.3, 0.2, 0.1, or 0.05 of other acids. In further embodiments, the composition is substantially free of or free of (i.e., contains no) other acids. In one or more embodiments, the composition may comprise less than 0.6, 0.5, 0.4, 0.3, 0.2, 0.1, or 0.05 of salicylic acid. In further embodiments, the composition is substantially free of or free of (i.e., contains no) salicylic acid. In one or more embodiments, the composition may comprise less than 0.6, 0.5, 0.4, 0.3, 0.2, 0.1, or 0.05 of lactic acid. In further embodiments, the composition is substantially free of or free of (i.e., contains no) lactic acid.
[0035] In some embodiments, the total amount of acid in any type of composition is less than 15, 14.5, 14, 13.5, 13, 12.5, 12, 11.5, 11, 10.5, or 10% by weight of the total composition.
[0036] In one or more embodiments, the composition further comprises a glycol. Without being bound by theory, it is believed that the glycol increases the biodelivery of the one or more acids. In one or more embodiments, the glycol is selected from the group consisting of glycerin, propylene glycol, butylene glycol, pentalene glycol, hexylene glycol, polyethylene glycol, polypropylene glycol, diethylene glycol, triethylene glycol, caprylyl glycol, glycerol, butanediol, and hexanetriol, as well as copolymers and combinations thereof. In a further embodiment, the glycol comprises propylene glycol.
[0037] In some embodiments, the composition further comprises a salt-tolerant thickening polymer and / or dispersion polymer. As used herein, the term "salt-tolerant thickening polymer" refers to a polymer that can increase the viscosity of a composition while maintaining stability in the presence of relatively high concentrations of salt in the formulation. In some embodiments, the salt-tolerant thickening polymer can increase the viscosity of a composition having a salt concentration of greater than about 2.0%. In particular, the salt-tolerant thickening polymer can tolerate relatively high concentrations of salt and function as a thickener at relatively low pH (e.g., less than about 4.5 or 4). Because salt is derived from the ionized form of an acid, salt content is related to pH. Thus, for example, one or more of the compositions described herein may be formulated to have a viscosity that is greater than the pK of an acid (e.g., mandelic acid, glycolic acid, gluconolactone, salicylic acid, etc.). a The dispersion polymer is prepared at a pH above 3.8-4.0. Thus, 50% or more of the acid is present in the formulation as a salt. As used herein, the term "dispersion polymer" refers to a polymer that allows for the suspension of particles and / or droplets.
[0038] The salt-tolerant thickening polymer may be crosslinked or non-crosslinked. In one or more embodiments, the salt-tolerant thickening polymer may comprise a polyacrylate-based thickener, a polyacrylamide thickener, or a crosslinked copolymer containing acrylate and / or acrylamide moieties. In one or more embodiments, the salt-tolerant thickening polymer comprises sulfonate groups. In one or more embodiments, the salt-tolerant thickening polymer comprises structural units derived from acrylamidoalkylsulfonic acid or a salt thereof. In such embodiments, the salt-tolerant thickening polymer may comprise: - polymers based on 2-acrylamido-2-methylpropanesulfonic acid and / or its salts, such as those sold under the name Aristoflex™ and described in EP 0 816 403, EP 1 116 733 and EP 1 069 142. Polymers based on 2-methyl-2-[(1-oxo-2-propenyl)amino]-1-propanesulfonic acid and / or its salts, as described in US Pat. No. 1,084,9845 (B2). - a polymer containing structure (I):
[0039] [ka] (In the formula, R 3 is a hydrogen atom, methyl or ethyl, Y is an alkylene group having 1 to 9 carbon atoms, and X is an ammonium, alkali metal or alkaline earth metal ion.) The salt-tolerant thickening polymer may contain other neutral and / or hydrophobic monomers.
[0040] Suitable neutral monomers include, but are not limited to, N,N-dialkylacrylamides, where each alkyl group contains 1 to 4 carbon atoms, more specifically N,N-dimethylacrylamide, N,N-diethylacrylamide, N,N-dipropylacrylamide, or N,N-diisopropylacrylamide.
[0041] Suitable hydrophobic monomers (also called "associative" monomers) for use in hydrophobically modified polyelectrolytes are described, for example, in U.S. Pat. Nos. 5,292,843, 6,897,253, 7,288,616, 3,035,004, and U.S. Patent Application Publication No. 2006 / 0270563, the contents of each of which are incorporated by reference herein in their entirety.
[0042] "Hydrophobic moiety," as used herein, refers to a nonpolar moiety comprising at least one of the following: (a) a carbon-carbon chain of at least five carbons, wherein none of the five carbons is a carbonyl carbon or has a hydrophilic moiety directly attached thereto; (b) two or more alkylsiloxy groups (-[Si(R)2-O]-); and / or (c) two or more consecutive oxypropylene groups. The hydrophobic moiety may be or may comprise a linear, cyclic, aromatic, saturated, or unsaturated group. In certain preferred embodiments, the hydrophobic moiety comprises a carbon chain of at least six carbons, more preferably seven carbons or more, wherein none of the carbons in such a chain has a hydrophilic moiety directly attached thereto. Certain other preferred hydrophobic moieties include moieties comprising a carbon chain of about eight carbon atoms or more, more preferably about ten carbon atoms or more, wherein none of the carbons in such a chain has a hydrophilic moiety directly attached thereto. Examples of hydrophobic functional moieties may include ester, ketone, amide, carbonate, urethane, carbamate, or xanthate functional groups, which have a carbon chain of at least four carbons incorporated therein or attached thereto, and none of the four carbons has a hydrophilic moiety directly attached thereto. Other examples of hydrophobic moieties include groups such as poly(oxypropylene), poly(oxybutylene), poly(dimethylsiloxane), and fluorinated hydrocarbon groups, which have a carbon chain of at least four carbons, and none of the four carbons has a hydrophilic moiety directly attached thereto.
[0043] As used herein, a "hydrophilic moiety" is any polar, anionic, cationic, zwitterionic, or nonionic group. Non-limiting examples include anionic materials such as sulfate, sulfonate, carboxylic acid / carboxylate, phosphate, phosphonate, etc.; cationic materials such as ammonium, pyridinium, imidazolinium, amidinium, poly(ethyleneiminium), including amino, mono-, di-, and trialkylammonium species; zwitterionic materials such as ammonium alkylsulfonate, ammonium alkylcarboxylate, amphoacetate, etc.; and nonionic materials such as hydroxyl, sulfonyl, ethyleneoxy, amide, ureido, amine oxide, etc.
[0044] Specific examples of hydrophobic monomers include, but are not limited to: Acrylic hydrophobic monomers according to the following structure (II):
[0045] [ka] During the ceremony, ·R 21 is a linear, branched or cyclic (C5-C50) alkyl, hydroxyalkyl, alkoxyalkyl, aryl or aralkyl; ·R 25 is H, or methyl, or ethyl, p and q are each independently 2, 3, or 4; r and s are each independently 0 to 50; t is 1 to 50.
[0046] In one embodiment, the hydrophobic monomer is R 21 is a straight chain (C8-C20) alkyl. In one embodiment, the hydrophobic monomer is a compound according to structure II, where p=0 and s=0, and R 21is a straight chain or branched (C8-C20) alkyl group. In one embodiment, the hydrophobic monomer is a compound according to structure II where p=2, s=0, and t=1.
[0047] Suitable ethylenically unsaturated hydrophobic monomers include: alkyl(meth)acrylates containing at least one linear or branched (C5-C40) alkyl group per molecule, such as pentyl(meth)acrylate, hexyl(meth)acrylate, tridecyl(meth)acrylate, myristyl(meth)acrylate, cetyl(meth)acrylate, stearyl(methyl)acrylate, behenyl polyalkoxylated (meth)acrylate, and mixtures thereof; alkyl-polyether (meth)acrylates containing at least one linear or branched (C5-C40) alkyl-polyether group per molecule, such as hexyl polyalkoxylated (meth)acrylate, tridecyl polyalkoxylated (meth)acrylate, myristyl polyalkoxylated (meth)acrylate, cetyl polyalkoxylated (meth)acrylate, stearyl polyalkoxylated (methyl)acrylate, eicosyl polyalkoxylated (meth)acrylate, behenyl polyalkoxylated (meth)acrylate, melissyl polyalkoxylated (meth)acrylate, tristyrylphenoxyl polyalkoxylated (meth)acrylate, and mixtures thereof; alkyl-polyether (meth)acrylamides containing at least one (C5-C40) alkyl-polyether substituent per molecule, such as hexyl polyalkoxylated (meth)acrylamide, tridecyl polyalkoxylated (meth)acrylamide, myristyl polyalkoxylated (meth)acrylamide, cetyl polyalkoxylated (meth)acrylamide, stearyl polyalkoxylated (methyl)acrylamide, eicosyl polyalkoxylated (meth)acrylamide, behenyl polyalkoxylated (meth)acrylamide, melissyl polyalkoxylated (meth)acrylamide, and mixtures thereof; alkyl-polyether vinyl esters, alkyl-polyether vinyl ethers, or alkyl-polyether vinyl amides containing at least one (C5-C40) alkyl-polyether substituent per molecule, such as vinyl stearate polyalkoxylates, myristyl polyalkoxylated vinyl ethers, and mixtures thereof; - as well as mixtures of any two or more of the above alkyl-polyether acrylates, alkyl-polyether methacrylates, alkyl-polyether acrylamides, alkyl-polyether methacrylamides, alkyl-polyether vinyl esters, alkyl-polyether vinyl ethers, and alkyl-polyether vinyl amides. Cyclohexyl (meth)acrylate, 2-ethylhexyl (meth)acrylate, isodecyl (meth)acrylate, lauryl (meth)acrylate, isobornyl (meth)acrylate, benzyl (meth)acrylate, phenoxyethyl (meth)acrylate, tetrahydrofurfuryl (meth)acrylate, glycidyl (meth)acrylate, vinyl 2-ethylhexanoate, and N-tert-octyl (meth)acrylamide. In one embodiment, the hydrophobic monomer is one or more alkyl-polyalkoxylated (meth)acrylates containing one linear or branched (C5-C40) alkyl-polyethoxylated group per molecule, more generally one (C10-C22) alkyl-polyethoxylated group, such as, for example, decyl-polyethoxylated (meth)acrylate, tridecyl-polyethoxylated (meth)acrylate, myristyl-polyethoxylated (meth)acrylate, cetyl-polyethoxylated (meth)acrylate, stearyl-polyethoxylated Polyethoxylated methyl acrylate, eicosyl-polyethoxylated (meth)acrylate, behenyl-polyethoxylated (meth)acrylate, and more commonly decyl-polyethoxylated methacrylate, tridecyl-polyethoxylated methacrylate, myristyl-polyethoxylated methacrylate, cetyl-polyethoxylated methacrylate, stearyl-polyethoxylated methyl acrylate, eicosyl-polyethoxylated methacrylate, behenyl-polyethoxylated methacrylate, and mixtures thereof.
[0048] Salt-tolerant thickening polymers may be prepared by mixing other monomers, such as ethylenically unsaturated monomers such as acrylamide, dimethyl-acrylamide, and diacetone (meth)acrylamide, vinyl esters such as vinyl acetate, vinyl propionate, N-vinylamides such as N-vinylpyrrolidone, N-vinylcaprolactam, N-vinylformamide, and N-vinylacetamide, and vinyl ethers such as methyl vinyl ether, ethyl vinyl ether, butyl vinyl ether, and hydroxybutyl vinyl ether, and ethylenically unsaturated aryl compounds such as styrene, acetone, methyl vinyl ether, ethyl vinyl ether, butyl vinyl ether, and hydroxybutyl vinyl ether. The monomers may include ethylenically unsaturated alkyl esters of dicarboxylic acid monomers such as butylmethyl maleate, dimethylaminoethyl (meth)acrylate, diethylaminoethyl (meth)acrylate, and tert-butylaminoethyl (meth)acrylate.
[0049] In one or more embodiments, the salt-tolerant thickening polymer and / or dispersion polymer comprises 2-acrylamido-2-methylpropanesulfonate (also known as AMPS) moieties. In some embodiments, the salt-tolerant thickening polymer comprises ammonium acryloyldimethyltaurate moieties. In one or more embodiments, the acrylate-containing polymer is not a homopolymer of acrylate moieties. In some embodiments, the salt-tolerant thickening polymer comprises polyacrylate crosspolymer-6, hydroxyethyl acrylate / sodium acryloyldimethyltaurate copolymer, sodium acryloyldimethyltaurate / VP crosspolymer, or a combination thereof. Polyacrylate crosspolymer-6 is available as Sepimax Zen™ (INCI name: Polyacrylate Crosspolymer-6), which is provided in powder form sold by Seppic. Hydroxyethyl acrylate / sodium acryloyldimethyl taurate copolymer is available as SepinoV™ EMT10 (INCI name: Hydroxyethyl acrylate / sodium acryloyldimethyl taurate copolymer), also sold in powder form by Seppic. Acryloyldimethyl taurate / VP crosspolymer and ammonium acryloyldimethyl taurate / VP copolymer are available from Clariant as Aristoflex® AVS and Aristoflex® AVC (INCI names: Sodium acryloyldimethyl taurate / VP crosspolymer and Ammonium acryloyldimethyl taurate / VP copolymer), respectively. Further information about these polymers can be found in the table below.
[0050] [Table 1]
[0051] Naturally derived salt-tolerant thickening polymers include, but are not limited to, cellulose, xanthan, carrageenan, galactomannan, guar, tara, cassia, sesbania, locust bean gum, gellan gum, welan gum, carob seed flour, guar seed flour, starch, alginate, carrageenan, gellan, pullulan, scleroglucan, schizophyllan, curdlan, diutan, dextran, welan, chitin, and derivatives thereof, particularly alkylated (e.g., methyl ether, ethyl ether, C12-18 alkyl ether), hydroxyalkylated (hydroxyethyl, hydroxypropyl, or mixed ether), and carboxymethylated forms.
[0052] In some embodiments, the salt-tolerant thickening polymer and / or dispersion polymer is a cellulose-containing polymer. That is, the polymer contains a cellulose moiety. In further embodiments, the cellulose-containing polymer is a cellulose ether-based polymer. Examples of cellulose-containing polymers include, but are not limited to, hydroxyalkyl cellulose, carboxyalkyl cellulose, alkyl cellulose, hydroxyalkyl alkyl cellulose, cationic hydroxyalkyl cellulose, hydrophobically modified hydroxyalkyl cellulose, or cationic hydrophobically modified hydroxyalkyl cellulose. In further embodiments, the thickening and / or dispersion polymer comprises hydroxyethyl cellulose, carboxymethyl cellulose, methyl cellulose, hydroxypropyl methyl cellulose, ethyl cellulose, cationic hydroxyethyl cellulose, hydrophobically modified hydroxyethyl cellulose, or cationic hydrophobically modified hydroxyethyl cellulose.
[0053] In some embodiments, the thickening polymer is a dispersion polymer. The term "dispersion" polymer means that compositions having such polymers exhibit a yield stress. [As used herein, the term "yield value" means that the elastic modulus of the composition must be higher than the viscous modulus in the low strain / stress plateau region of the amplitude sweep. The yield stress is then considered to be the stress at the crossover where G' = G", and is expressed in Pascals (Pa). In one or more embodiments, the compositions of the present invention exhibit a yield value of about 0.1 Pa or greater, or about 0.5 Pa or greater, or about 1.0 Pa or greater, or about 2.0 Pa or greater.
[0054] In some embodiments, the pH of the composition ranges from about 3, 3.1, 3.2, 3.3, 3.4, 3.5, 3.6, 3.7, 3.8, or 3.9 to about 3.8, 3.9, 4, 4.1, 4.2, 4.3, 4.4, 4.5, 4.6, 4.7, 4.8, 4.9, or 5. In some embodiments, the pH of the composition ranges from about 3 to about 5, or from about 3.5 to about 4.5. Compositions below these pH ranges are considered too acidic for the skin and generally function as chemical peels. Chemical peels may also have higher acid concentrations (e.g., as much as 50%) than the embodiments described herein and may have a water-like viscosity.
[0055] Any suitable method of applying the composition to skin in need may be used. For example, the composition may be applied directly from the package to the skin in need, manually applied to the skin in need, or transferred from a substrate such as a wipe or mask, or a combination of two or more of these. In other embodiments, the composition may be applied via a dropper, tube, roller, spray, patch, or added to water that is to be used in a bath or otherwise applied to the skin. The composition may be applied in various ways / forms, including, but not limited to, a leave-on cream, a mask, and / or a serum. In one or more embodiments, the composition is left on the skin after application. The composition may be left for a period of at least 1, 5, 10, 24, or 48 hours.
[0056] Exemplary Compositions Any of the embodiments described herein can be combined in various combinations. Another aspect of the present invention relates to compositions suitable for treating acne. In one or more embodiments, the composition comprises: a. about 0.1% by weight to about 7.5% by weight of glycolic acid; b. about 0.1% to about 5% by weight of gluconolactone; c. about 0.1% to about 5% by weight of mandelic acid; d. glycol, e. salt-tolerant thickening and / or dispersing polymers; wherein the total amount of glycolic acid, gluconolactone, and mandelic acid is less than about 15% by weight of the total composition.
[0057] In another aspect, the present invention provides a composition for treating acne, comprising: a. about 2.5% by weight to about 7.5% by weight of glycolic acid; b. about 1% to about 5% by weight of gluconolactone; c. about 1% to about 5% by weight of mandelic acid; d. about 2.5% to about 7.5% by weight of propylene glycol; e. about 0.5% to about 2% by weight of polyacrylate crosspolymer-6; f. about 0.5% to about 2% by weight of hydroxyethyl acrylate / sodium acryloyldimethyltaurate copolymer; wherein the total amount of glycolic acid, gluconolactone, and mandelic acid is less than about 12% by weight of the total composition.
[0058] Other additives Various other materials may also be present in compositions used in accordance with the principles of the present invention. In certain embodiments, the compositions include one or more topically applied ingredients selected from the group consisting of surfactants, chelating agents, emollients, moisturizers, conditioners, preservatives, opacifiers, fragrances, and the like.
[0059] Emollient refers to the compound that helps maintain the soft, smooth and supple appearance of skin (for example, by remaining on the surface or stratum corneum of skin to act as lubricant).Suitable examples of emollient include those that can be found in Handbook of Cosmetic Science and Technology (edited by A. Barel, M. Paye and H. Maibach, published in 2001, Marcel Dekker, Inc. New York, NY), Chapter 35, page 399-415 (Skin Feel Agents, written by G Zocchi), for example, include but are not limited to petrolatum, hexyldecyl stearate, dimethicone, neopentyl glycol diheptanoate, and vegetable, nut and plant oil (for example, macadamia nut oil, rice bran oil, grape seed oil, palm oil, primrose oil, hydrogenated peanut oil and avocado oil).
[0060] Moisturizing agent refers to the compound (for example, hygroscopic compound) that is intended to increase the moisture content of the uppermost layer of skin.Suitable moisturizing agent examples include those found in Handbook of Cosmetic Science and Technology (edited by A. Barel, M. Paye and H. Maibach, published in 2001, Marcel Dekker, Inc. (New York, NY)), Chapter 35, pages 399-415 (Skin Feel Agents, written by G Zocchi), including but not limited to glycerin, sorbitol or trehalose (for example, α,α-trehalose, β,β-trehalose, α,β-trehalose), or its salt or ester (for example, trehalose-6-phosphate).
[0061] Surfactant refers to a surface active agent intended for cleansing or emulsifying.Suitable examples of surfactants include those found in Chapter 37, pages 431-450 (Classification of surfactants, by L. Oldenhove de Guertechin) of Handbook of Cosmetic Science and Technology (edited by A. Barel, M. Paye and H. Maibach, published in 2001, Marcel Dekker, Inc. (New York, NY)), including, but not limited to, anionic surfactants such as sulfates, cationic surfactants such as betaines, amphoteric surfactants such as sodium cocoglycinate, and nonionic surfactants such as alkyl polyglucosides.
[0062] Examples of suitable chelating agents include those capable of protecting and preserving the compositions of the present invention. In certain embodiments, the chelating agent is ethylenediaminetetraacetic acid ("EDTA"), and in further embodiments, tetrasodium EDTA, available commercially under the trade name "Versene 100XL" from Dow Chemical Company, Midland, Michigan.
[0063] Suitable preservatives include, for example, parabens, quaternary ammonium species, phenoxyethanol, benzoates, DMDM hydantoin, organic acids, phenoxyethanol, and are present in the composition in an amount of about 0 to about 1%, or about 0.05% to about 0.5%, based on the total weight of the composition.
[0064] Any of a variety of commercially available pearlizing or opacifying agents are suitable for use in the composition. Examples of suitable pearlizing or opacifying agents include, but are not limited to, (a) a fatty acid having about 16 to about 22 carbon atoms and (b) a mono- or diester of either ethylene or propylene glycol; (a) a fatty acid having about 16 to about 22 carbon atoms, (b) a mono- or diester of a polyalkylene glycol of the formula: HO-(JO)aH, where J is an alkylene group having about 2 to about 3 carbon atoms and a is 2 or 3; aliphatic alcohols containing about 16 to about 22 carbon atoms; aliphatic esters of the formula: KCOOCH2L, where K and L independently contain about 15 to about 21 carbon atoms; inorganic solids insoluble in shampoo compositions, and mixtures thereof.
[0065] Any fragrance composition suitable for use on the skin may be used in accordance with the present invention.
[0066] Any suitable carrier may be used in the composition. In particular, the carrier is a cosmetically acceptable carrier. As will be appreciated by those skilled in the art, a cosmetically acceptable carrier includes a carrier suitable for use in contact with the body, particularly the skin, that is free from undue toxicity, incompatibility, instability, irritation, allergic reaction, etc. A safe and effective amount of the carrier is from about 50% to about 99.999%, particularly from about 80% to about 99.9%, more particularly from about 99.9% to about 95%, and most particularly from about 98% to about 99.8% of the composition.
[0067] The following are non-limiting examples of carriers. Other carriers may be formulated by those skilled in the art. In one embodiment, the carrier comprises water. In a further embodiment, the carrier may further comprise one or more aqueous or organic solvents. Examples of organic solvents include, but are not limited to, dimethyl isosorbide; isopropyl myristate; cationic, anionic, and nonionic surfactants; vegetable oils; mineral oils; waxes; gums; synthetic and natural gelling agents; alkanols; and polyols. Examples of alkanols include, but are not limited to, those having about 2 carbon atoms to about 12 carbon atoms (e.g., about 2 carbon atoms to about 4 carbon atoms), such as isopropanol and ethanol. Examples of polyols include, but are not limited to, those having about 2 carbon atoms to about 15 carbon atoms (e.g., about 2 carbon atoms to about 10 carbon atoms), such as propylene glycol. The organic solvent may be present in the carrier in an amount of about 1% to about 99.99% (e.g., about 20% to about 50%) based on the total weight of the carrier. Water may be present in the carrier (prior to use) in an amount of about 5% to about 95% (e.g., about 50% to about 90%) based on the total weight of the carrier. The solution can contain any suitable amount of solvent, including about 40% to about 99.99%. Particularly preferred solutions contain about 50% to about 99.9%, about 60% to about 99%, about 70% to about 99%, about 80% to about 99%, or about 90% to about 99% solvent.
[0068] Compositions used in accordance with the principles of the present invention may further comprise any of a variety of additional cosmetic active agents. Examples of suitable additional active agents include skin lightening agents, tanning agents, additional anti-aging agents, tropoelastin promoters, collagen promoters, anti-acne agents, sheen adjusting agents, antimicrobial agents (e.g., anti-yeast, anti-fungal, and anti-bacterial agents), anti-inflammatory agents, anti-parasitic agents, topical analgesics, sunscreens, photoprotective agents, antioxidants, keratolytic agents, detergents / surfactants, moisturizers, nutrients, vitamins, energy enhancers, antiperspirants, astringents, deodorants, hair removal agents, hair growth strengthening agents, hair growth retarding agents, stabilizers, hydration enhancers, efficacy enhancers, anti-callus agents, skin conditioning agents, anti-cellulite agents, malodor control agents (e.g., malodor masking agents), or pH modifying agents.
[0069] Examples of various suitable additional cosmetically acceptable active substances include benzoyl peroxide, D-panthenol; avobenzone (Parsol 1789), bisdisulizole disodium (Neo Heliopan AP), diethylaminohydroxybenzoyl hexylbenzoate (Uvinul A Plus), ecamsule (Mexoryl SX), methyl anthranilate, 4-aminobenzoic acid (PABA), cinoxate, ethylhexyl triazone (Uvinul T150), homosalate, 4-methylbenzylidene camphor (Parsol 5000), octyl methoxycinnamate (Octinoxate), octyl salicylate (Octisalate), padimate O (Escalol 507), phenylbenzimidazole sulfonic acid (Ensulizole), polysilicone-15 (Parsol SLX), trolamine salicylate, bemotrizinol (Tinosorb S), Benzophenone 1-12, Dioxybenzone, Drometrizole Trisiloxane (Mexoryl XL), Iscotrizinol (Uvasorb HEB), Octocrylene, Oxybenzone (Eusolex 4360), Sulisobenzone, Bisoctrizole (Tinosorb UV filters, such as, but not limited to, UV-filters, such as, but not limited to, UV-filters (e.g., UV-filters M), titanium dioxide, zinc oxide; carotenoids; free radical scavengers; spin traps; retinoids and retinoid precursors (e.g., (30) retinol, retinoic acid, and retinyl palmitate); ceramides; polyunsaturated fatty acids; essential fatty acids; enzymes; enzyme inhibitors; minerals; hormones (e.g., estrogen); steroids (e.g., hydrocortisone); 2-dimethylaminoethanol; copper salts (e.g., copper chloride); copper-containing peptides such as Cu: Gly-His-Lys, Coenzyme Q10; amino acids (e.g., proline); vitamins; lactobionic acid; acetyl-coenzyme A; niacin; riboflavin; thiamine; ribose; electron transporters (e.g., NADH and FADH2); and other plant extracts (e.g., extracts of oat, aloe vera, feverfew, soybean, and shiitake mushroom), and derivatives and mixtures thereof.
[0070] Product form and packaging The compositions can be made into a wide variety of product forms. For example, but not limited to, compositions in the form of emulsions, such as oil-in-water, water-in-oil, water-in-oil-in-water, and oil-in-water-in-silicone emulsions, are useful herein. These emulsions can cover a wide range of viscosities, for example, from about 100 cps to about 200,000 cps. In this application, two types of viscosity measurements are referred to: A) viscosity at 25°C in a rheometer at 20 s -1 A) "Rheometer viscosity," measured as a steady-state value at an applied shear rate of A, B) "Rheometer viscosity," measured as a steady-state value at an applied shear rate of A, C, and B) "Brookfield viscosity," measured at 5 or 10 RPM after 1 minute at 25° C. in a 4 oz. jar using spindle RV#4 or RV#5. Unless otherwise specified, the viscosity referred to is the rheometer viscosity.
[0071] Examples of suitable forms include solutions, suspensions, lotions, creams, serums, essences, gels, toners, sticks, sprays, ointments, cleansing solutions and bar soaps, shampoos, hair conditioners, pastes, foams, mousses, powders, shaving creams, wipes, patches, strips, powered patches, microneedle patches, bandages, hydrogels, film-forming products, facial and skin masks, make-up, liquid drops, and the like.
[0072] In one or more embodiments, the compositions described herein are in the form of a serum or lotion. As used herein, the term "serum" or "lotion" refers to a primarily water-containing topical formulation with a viscosity of about 1,000 cPs to 4,000 cPs, a light texture, and a fresh, watery feel. A lotion or serum typically contains at least one emollient in addition to a solvent. A lotion / serum may contain about 1% to about 20% (e.g., about 5% to about 10%) of emollient(s) and about 50% to about 90% (e.g., about 60% to about 80%) water.
[0073] In some embodiments, the compositions described herein are in the form of a cream. As used herein, the term "cream" refers to a topical formulation containing a thick, predominantly water-based solution having a viscosity of about 2,000 cPs to 8,000 cPs. Creams typically contain about 5% to about 50% (e.g., about 10% to about 20%) of emollient(s) and about 45% to about 85% (e.g., about 50% to about 75%) of water.
[0074] In one or more embodiments, the compositions described herein are in the form of an ointment. As used herein, the term "ointment" refers to a topical formulation containing primarily oil and having a thick texture with a viscosity of about 10,000 cPs to about 40,000 cPs. The ointment may contain a simple base of animal, vegetable, or synthetic oil, or a semi-solid 10-carbon hydrocarbon. The ointment may contain about 2% to about 10% of an emollient(s) and about 0.1% to about 2% of a thickener(s).
[0075] The compositions useful in the present invention can also be formulated as emulsions. When the carrier is an emulsion, about 1% to about 10% (e.g., about 2% to about 5%) of the carrier contains an emulsifier(s). The emulsifier may be nonionic, anionic, or cationic.
[0076] Lotions and creams can be formulated as emulsions. Such lotions typically contain 0.5% to about 5% emulsifier(s), and such creams typically contain about 1% to about 20% (e.g., about 5% to about 10%) emollient(s), about 20% to about 80% (e.g., about 30% to about 70%) water, and about 1% to about 10% (e.g., about 2% to about 5%) emulsifier(s).
[0077] Single-phase emulsion skin care preparations, such as lotions and creams, of the oil-in-water and water-in-oil types, are well known in the art and are useful in the present invention. Multiphase emulsion compositions, such as water-in-oil-in-water or oil-in-water-in-oil types, are also useful in the present invention. Generally, such single-phase or multiphase emulsions contain water, emollients, and emulsifiers as essential ingredients.
[0078] The compositions of the present invention can also be formulated as gels. As used herein, the term "gel" refers to a topical formulation containing a dispersed polymer and having a thick, predominantly water-based texture, exhibiting a yield value of about 0.1 Pa or greater. Gels may contain a gelling agent. Such gels typically contain about 0.1% to 5% by weight of such a gelling agent.
[0079] The compositions of the present invention can also be formulated into solid preparations (e.g., wax-based sticks, bar soap compositions, powders, or wipes). The compositions of the present invention may be combined with solid, semi-solid, or soluble substrates (e.g., wipes, masks, pads, gloves, or strips).
[0080] The compositions described herein can be provided to the consumer in a container, such as a bottle, tube, etc. Individual packets containing measured portions of the composition can also be used. A pump, squeezable valve, or removable screw cap can be used to dispense the composition from the bottle. [Example]
[0081] Examples 1A-C: Compositions and Properties Several compositions were prepared and evaluated as described below. Viscosity values shown in the results of the Examples section are Brookfield viscosities and were measured using a Brookfield Viscometer DV-II+PRO. For E1-3, values were taken after 1 minute using RVT spindle #4 at 5 rpm. For E4-E22, values were taken after 1 minute using RVT spindle #5 at 5 rpm. All measurements were made at 22°C in 4 oz. glass jars.
[0082] E1-3 were prepared according to the following protocol: Premix A: Add 10% water, propylene glycol, glycolic acid, gluconolactone, mandelic acid, and salicylic acid (if included). Mix for a minimum of 1.5 hours. Adjust the pH of this premix to 3.8 with 20% sodium hydroxide solution. Main Phase: Add water, chelating agent, hydroxyethyl acrylate / sodium acryloyldimethyl taurate copolymer, polyacrylate crosspolymer-6. Start the homogenizer and add the other ingredients. Homogenize until the formulation is uniform, there are no undissolved particles, and a suitable emulsion is formed.
[0083] Compositions E4-E17 were prepared according to the following protocol: Acid Premix: Add 10% water, propylene glycol, glycolic acid, gluconolactone, mandelic acid, and salicylic acid (if included). Mix for a minimum of 1.5 hours. Adjust the pH of this premix to 3.5-3.8 with 20% sodium hydroxide solution. Main Phase: Add water and polymer(s) (hydroxyethyl acrylate / sodium acryloyldimethyltaurate copolymer and polyacrylate crosspolymer-6, or ammonium acryloyldimethyltaurate / carboxyethyl acrylate crosspolymer, or sodium acryloyldimethyltaurate / VP crosspolymer, or hydroxyethyl cellulose). For E15, which used hydroxyethyl cellulose, add 1,3-butene glycol to the main phase and mix until the polymer is completely dissolved. oHeat to C. Homogenize with a homogenizer until the formulation is uniform and free of undissolved particles. Add the acid(s) premix and mix for 15 minutes. Add the other ingredients. Homogenize until the formulation is uniform, free of undissolved particles, and a proper emulsion is formed. Adjust the pH to 3.4-4.0 using 20% sodium hydroxide solution. For E1-3, adjust the pH of the formulation to 3.8.
[0084] [Table 2] 1.Sepimax Zen(trademark) 2.Sepinov(TM) EMT 10 3. A blend of Xiameter™ PMX-200 silicone fluid, Dow Corning® Q7-9120 silicone fluid, and Dowsil™ 9041 silicone elastomer blend.
[0085] As can be seen from the table above, compositions E1-12 containing up to about 10.5 weight percent total acid of AHA, PHA, and (optionally) BHA in combination with various levels of salt-tolerant thickening polymer resulted in different formulation forms: lotion or serum (E1-E3), lotion (E4-E6), cream (E5, E6), or ointment (E7-12). All viscosities were measured by the method described above.
[0086] Example 1B: Effect of Polymer Type on Viscosity Five compositions were prepared according to the table below and the viscosities were measured.
[0087] [Table 3] 1.Sepimax Zen(trademark) 2.Sepinov(TM) EMT 10 3. Aristoflex® AVC 4. Aristoflex® AVS
[0088] As can be seen from the table above, polymers of different properties were used to increase viscosity depending on the desired product form. Compositions containing acrylate-based crosspolymers such as acryloyldimethyltaurate / VP copolymer (E16, E17), combinations of polyacrylate crosspolymer-6 and hydroxyethyl acrylate / sodium acryloyldimethyltaurate copolymer (E13, E14), and cellulose-based polymers such as hydroxyethyl cellulose (E15) were prepared and their viscosities measured. Furthermore, compositions formulated with sodium acryloyldimethyltaurate / VP crosspolymer (E16) exhibited higher viscosities than compositions formulated with ammonium acryloyldimethyltaurate / carboxyethyl acrylate at the same polymer concentration, thus making sodium acryloyldimethyltaurate / VP crosspolymer a more potent viscosity enhancer.
[0089] Example 1C: Effect of Acid Addition on Viscosity Five samples were prepared according to the table below.
[0090] [Table 4] 1.Sepimax Zen(trademark) 2.Sepinov(TM) EMT 10
[0091] E18-22 were prepared according to the following protocol: Acid Premix: Add 10% water, propylene glycol, glycolic acid and / or gluconolactone and / or mandelic acid. Mix for a minimum of 1.5 hours. Adjust the pH of this premix to 3.5-3.8 with 20% sodium hydroxide solution. Main Phase: Add water, hydroxyethyl acrylate / sodium acryloyldimethyl taurate copolymer, polyacrylate crosspolymer-6. Homogenize with a homogenizer until the formulation is uniform and free of undissolved particles. Add the acid(s) premix, mix for 15 minutes, and adjust the pH to 3.4-4.0 with 20% sodium hydroxide solution.
[0092] As can be seen from the table above, the addition of acid reduces viscosity compared to the acid-free formulation (E18). The addition of glycolic acid in E19 showed the greatest reduction in viscosity compared to gluconolactone in E20 or mandelic acid in E21. At the same acid concentration, the glycolic acid-containing composition required the greatest amount of sodium hydroxide to adjust the pH to the desired value compared to gluconolactone and / or mandelic acid. Thus, the glycolic acid example (E19) contains the greatest amount of salt, which provides the strongest effect on the polymer in reducing viscosity. Combining gluconolactone and mandelic acid in E22 exhibits an additive effect; therefore, an even greater reduction in viscosity requires more polymer to effectively increase viscosity.
[0093] Example 1D: Effect of Polymer Selection on Stability Thirteen samples (six comparative and seven inventive) having the ingredients shown in the table below were prepared and then evaluated for stability, rheometer viscosity and yield. Stability was determined by the presence of separation after one month at 50°C.
[0094] Samples were prepared according to the following protocol: Premix A: Add 10% water, propylene glycol, glycolic acid, gluconolactone, mandelic acid, and salicylic acid. Mix for a minimum of 1.5 hours. Adjust the pH of this premix to 3.8 using 20% sodium hydroxide solution. Main Phase: Add water, chelating agent, and polymer(s) and mix until uniform (heat to 80°C if necessary). Start the homogenizer and add the other ingredients. Homogenize until the formulation is uniform, there are no undissolved particles, and a suitable emulsion is formed. Adjust the pH to 3.6-4.0 using 20% sodium hydroxide solution. All formulations have a salt content greater than 2%.
[0095] [Table 5] 1. Carbopol® Aqua SF-1 2. Carbopol® Aqua SF-2 3. Carbopol® Ultrez 20 4. Carbopol® Ultrez 10 5.Avalure(TM) Flex-6 6. A blend of Xiameter™ PMX-200 silicone fluid, Dow Corning® Q7-9120 silicone fluid, and Dowsil™ 9041 silicone elastomer blend.
[0096] [Table 6]
[0097] [Table 7] 1.Sepimax Zen(trademark) 2.Sepinov(TM) EMT 10 3. Aristoflex® Silk 4. Aristoflex® HMB 5. Rheocare XGN 6. Benecel K200M 7. A blend of Xiameter™ PMX-200 silicone fluid, Dow Corning® Q7-9120 silicone fluid, and Dowsil™ 9041 silicone elastomer blend.
[0098] [Table 8]
[0099] As can be seen from the table above, comparative compositions E23-28 were all unstable, while inventive compositions E29-34 were all stable. Here, stable means that the samples passed accelerated stability testing at 50°C for one month, showed no visible changes such as phase separation, and showed no significant changes in pH or viscosity. Because the compositions were all similar except for variations in the polymer selection, the above data is informative regarding polymers that can be used to obtain stable formulations. While the inventive formulations all feature the use of salt-tolerant polymers, specifically either sulfonate-containing or cellulosic moieties, the comparative formulations do not.
[0100] As can be seen from the table above, compositions E29-34 containing various levels of salt-tolerant thickening polymer resulted in different formulation forms: lotion or serum (E31), cream (E32) or ointment (E29, E30, E33, E34). All viscosities were measured by the method described above.
[0101] As can be seen from the table above, compositions E29 to E33 are in the form of gels because they contain dispersed polymers, and exhibit yield values of about 0.1 Pa or greater.
[0102] Examples 2A-D: Clinical Study A 12-week, single-center, evaluator-blinded, randomized, controlled clinical trial was conducted to evaluate the efficacy and tolerability of the compositions of the present invention (E1 and E2) in improving acne and facial appearance in subjects with mild to moderate acne vulgaris.The breakdown of the composition ingredients is reproduced in the table below.E1 and E2 are identical except that E1 contains salicylic acid, and E2 contains water instead of salicylic acid.35 subjects completed treatment with E1, and 32 subjects completed treatment with E2.
[0103] [Table 9] 1.Sepinov(TM) EMT 10 2.Sepimax Zen(trademark) 3. A blend of Xiameter™ PMX-200 silicone fluid, Dow Corning® Q7-9120 silicone fluid, and Dowsil™ 9041 silicone elastomer blend.
[0104] Subjects used their assigned treatment once daily (evening) during the first week, followed by twice daily (morning and evening) for the remainder of the study. Study investigators assessed acne lesion counts, global acne assessment, and additional clinical tiered efficacy. Tolerability was assessed by the investigator and by self-assessment. Results are shown in the table below. Data show the total % of subjects who showed improvement in at least one subattribute in the greater benefit bucket between both treatments for various attributes.
[0105] [Table 10]
[0106] As can be seen from the results, the treatments provided a statistically and clinically significant reduction in total lesion counts (inflammatory and non-inflammatory) according to investigator grading over the 12-week clinical study, starting at week 2, with no statistically significant difference in total lesion counts between Treatments A and B at week 12. In addition, both treatments improved the redness of inflammatory lesions, skin surface roughness, and overall skin blemishes, with no statistically significant difference in grading at week 12. Both products were found to be well tolerated, with no statistically significant increase in any of the tolerance attributes evaluated. The degree to which the products were well tolerated was also surprising, considering the relatively high acid content of the products.
[0107] Examples 3A-C: Microbiology Studies Two compositions of the present invention were tested against two placebo compositions to evaluate their effectiveness against P. acnes in both planktonic and biofilm states. The two compositions of the present invention are the same E1 and E2 described above. E1 and E2 are identical except that E1 contains salicylic acid, while E2 contains water instead of salicylic acid. The two placebo compositions correspond to E1 and E2 except that the placebo compositions do not contain propylene glycol or any acid. Placebo 1 has a pH of 4.5, which corresponds to the pH obtained when the ingredients are removed without additional pH adjustment. Placebo 2 was pH-adjusted to 3.8, the pH of E1 and E2, to account for any pH effects. The components of the compositions are listed in the table below.
[0108] [Table 11] 1.Sepinov(TM) EMT 10 2.Sepimax Zen(trademark) 3. A blend of Xiameter™ PMX-200 silicone fluid, Dow Corning® Q7-9120 silicone fluid, and Dowsil™ 9041 silicone elastomer blend.
[0109] Placebo 1 was prepared by adding water, a chelating agent, hydroxyethyl acrylate / sodium acryloyldimethyl taurate copolymer, and polyacrylate crosspolymer-6. The mixture was then homogenized in a homogenizer, followed by the addition of the other ingredients. The mixture was homogenized until the formulation was uniform, free of undissolved particles, and a suitable emulsion was formed. Placebo 2 was prepared identically to Placebo 1, except that the pH was adjusted to 3.8 using citric acid solution.
[0110] Example 3A: Effect on planktonic bacteria Planktonic bacteria were treated with E1-2 and placebo 1-2 and evaluated for efficacy. The protocol used is described below.
[0111] Assay: C. acnes microbial kill time assay (standard plankton test method) Test organism: Propionibacterium acnes ATCC 11827 Testing Procedure: Organism Preparation: Prepare organism inoculum by making a direct suspension of isolated colonies from the agar plate in sterile saline. a. Using a spectrophotometer, target an approximate 1.0 OD600 on the spectrophotometer for a suspension of approximately 108-109 CFU / mL. Further dilute to 107 CFU / mL and 105 CFU / mL in saline. 1:50 Neutralizer Validation: Weigh 0.2 grams of test sample and dilute 1:50 in 9.8 mL of neutralizer. b. Prepare a control tube containing 9.8 mL of neutralizer and 0.2 mL of saline. Add 100 μL of inoculum (10 CFU / mL of the standardized inoculum above) to all neutralized and control tubes to obtain 10-100 CFU / mL. After 10 minutes, 0.1 mL aliquots were made and plates were spread in duplicate on RCA. Incubate anaerobically at 35 ± 2.5°C for 5-7 days. Count colonies and calculate the average CFU / mL. Recovery of less than 50% CFU / mL of neutralizer vs. inoculated control CFU / mL indicates toxicity.
[0112] Microbial death time test Weigh 5 grams of each test sample into a sterile sample cup. Inoculate each sample cup with 50 μL of inoculum (10 CFU / mL). Start the timer and mix thoroughly. Sample at 10 minutes. After the time has elapsed, transfer 0.2 grams of the inoculated test sample to 9.8 mL of neutralizer. Run a saline blank sample in the same manner.
[0113] Dilution and plating: After the initial 1:50 dilution, make another 1:50 dilution in saline. Aliquot 0.1 mL from the initial 1:50 dilution and spread the plates in duplicate on the RCA. Prepare all plates after the initial 1:50 dilution as spot plates. Divide the agar plate into quadrants with markers on the bottom of the plate. Prepare duplicate plates for each sample. Each plate will receive up to five dilutions of one sample. Use a multi-dispensing pipettor to draw up 100 μL of sample. Dispense five spots of 10 μL each onto one quadrant of the plate. Dispense the next five spots of 10 μL onto one quadrant of the replicate plate. Continue with each dilution required for each sample.
[0114] After the liquid is absorbed, invert the plates and incubate them in an anaerobic chamber at 35 ± 2 °C for 5-7 days until clear colonies are observed. Count the colonies using an automated colony counter and calculate the CFU / mL of sample.
[0115] result
[0116] [Table 12]
[0117] As can be seen from the table above, both Placebo 1 and Placebo 2 showed approximately the same bacterial counts as the untreated control. In contrast, the bacterial counts of E1 and E2 of the present invention were below the detection limit. This indicates that E1 and E2 are effective in killing planktonic C. acnes bacteria. Furthermore, because E2 does not contain salicylic acid yet still showed a high mortality rate, the presence of glycolic acid, gluconolactone, and mandelic acid alone is surprisingly effective in killing planktonic C. acnes bacteria.
[0118] Example 3B: Effect on biofilms Biofilm-grown bacteria were treated with E1-2 and placebo 1-2 to evaluate their effectiveness. The protocol used was in accordance with ASTM E2647-13: "Standard Test Method for Quantification of Pseudomonas aeruginosa Biofilm Grown Using Drip Flow Biofilm Reactor with Low Shear and Continuous Flow," and is also described below.
[0119] Preparation of C. acnes biofilms A standard C. acnes ATCC 11827 culture grown in Reinforced Clostridial Media (RCM) (Remel, Lenexa, KS) was used as the seed culture for biofilm formation. Biofilms were grown on half of a soda-lime glass microscope slide (VistaVision™, VWR International) in a growth medium of RCM supplemented with olive oil, oleic acid, and squalene. Biofilms were incubated anaerobically at 32.5 ± 2.5 °C for 72 ± 0.5 h.
[0120] Treatment of C. acnes biofilms with clear skin preparations: After 72 ± 0.5 hours, the biofilms were removed from the anaerobic conditions and treated with 1 gram of test product for 10 minutes. Untreated biofilms served as negative controls in each test. After treatment, the biofilms and test products were immediately scraped from half of the slides and collected in neutralizing broth (TAT Broth, Remel) according to ASTM E2647-13 (a procedure modified for C. acnes biofilms). After collection of the biofilms and test products in neutralizing broth (considered a 100-fold dilution), serial dilutions were made in 0.85% saline and plated onto reinforced clostridial agar (RCA). The plates were incubated anaerobically at 32.5 ± 2.5°C for 5–7 days. After incubation, colonies on the plates were counted, and the average CFU / cm2 was calculated (representing the viability).
[0121] result
[0122] [Table 13]
[0123] [Table 14]
[0124] As can be seen from the table above, both placebos 1 and 2 showed nearly the same bacterial counts as the untreated control. In contrast, the bacterial counts of E1 and E2 of the present invention were much lower. This demonstrates that E1 and E2 are effective at killing C. acnes bacteria in a biofilm state. These results are surprising, as bacteria are known to be more difficult to kill in a biofilm. Furthermore, because E2 does not contain salicylic acid yet still showed a high mortality rate, the presence of glycolic acid, gluconolactone, and mandelic acid alone is effective at killing C. acnes bacteria in a biofilm state.
[0125] Example 3C: Biofilm disruption test The disruptive efficacy of formulations according to one or more embodiments of the present invention was investigated against the biofilm-state organism C. acnes ATCC 11827. The inventive composition (E1') was tested alongside a placebo composition (Placebo 2, same as above) and a sterile water control treatment. All were evaluated for efficacy against biofilm-state C. acnes. Placebo 2 is similar to E1', except that the placebo composition does not contain propylene glycol or any acid. Both the inventive composition (E1') and the placebo composition (Placebo 2) were pH-adjusted to 3.8 to account for any pH effects. The components of the compositions are listed in the table below.
[0126] [Table 15]
[0127] Biofilm-forming Propionactium acnes bacteria were treated with E1', placebo 2, and a sterile water control and evaluated for biofilm disruption efficacy. The assay used was developed according to Holmberg, A. et al., "Biofilm Formation by Propionacterium acnes is a Characteristic of Invasive Isolates. Clin Microbiol Infect 2009;15:787-795." and is described below.
[0128] Preparation of C. acnes biofilms Standard C. acnes ATCC 11827 cultures grown in enriched clostridial medium (RCM) (Remel, Lenexa, KS) were used as seed cultures for biofilm formation. Biofilms were grown in CoStar 96-well tissue culture-treated plates (Corning, Fisher Scientific, Pittsburgh, PA) in RCM growth medium supplemented with olive oil, oleic acid, and squalene. Biofilms were incubated at 32.5±2.5°C in a 5% CO atmosphere for 72±0.5 hours.
[0129] Treatment of C. acnes biofilms with test compositions: After 72 ± 0.5 hours, the biofilms were removed from the 5% CO2 atmosphere and treated with 200 μL of the test composition (E1' and Placebo 2, respectively) diluted 1:5 with sterile water for 30 seconds at room temperature. Biofilms treated with sterile water alone served as negative controls in each test. After treatment, the biofilms and test composition were gently aspirated from the wells, and the wells were then gently washed with 0.1% peptone water and allowed to dry ("fixed") for 60 minutes. After fixation, the biofilms were stained with 1.0% crystal violet solution at room temperature for 15-20 minutes. After staining, excess crystal violet solution was decanted, and each well was gently rinsed with sterile water. A solvent (ethanol) was then added to each well for 30 minutes. The solubilized dye was then dispensed into a new 96-well plate, and the mean optical density at 595 nm (OD ) was measured. 595nm ) represents the biomass, and the optical density at 595 nm (OD 595nm The absorbance at 1000 kJ / min was measured.
[0130] result
[0131] [Table 16]
[0132] As can be seen from the table above, the control (sterile water) and placebo 2 exhibited mean optical densities (indicating mean biomass) of 0.902 and 0.792, respectively. In contrast, E1' of the present invention exhibited a much lower mean biomass of 0.678. This demonstrates that E1' is effective in destroying C. acnes bacteria in a biofilm state. These results are surprising because biofilm structures are often difficult to disrupt.
[0133] While various aspects of the present disclosure have been illustrated and described by way of example, it will be understood that the invention claimed herein is not limited thereto and may be variously embodied in accordance with the claims presented herein and / or any derivative patent application.
[0134] [Embodiment] (1) A composition for treating acne, comprising: a. about 0.1% by weight to about 7.5% by weight of glycolic acid; b. about 0.1% to about 5% by weight of gluconolactone; c. about 0.1% to about 5% by weight of mandelic acid; d. glycol, e. a salt-tolerant thickening polymer; wherein the total amount of glycolic acid, gluconolactone, and mandelic acid is less than about 15% by weight of the total composition. (2) The composition of embodiment 1, wherein the total amount of glycolic acid, gluconolactone, and mandelic acid is at least about 2% by weight of the total composition. (3) The composition of any one of the preceding claims, wherein the glycol is selected from the group consisting of glycerin, propylene glycol, butylene glycol, pentylene glycol, hexylene glycol, polyethylene glycol, polypropylene glycol, diethylene glycol, triethylene glycol, caprylyl glycol, glycerol, butanediol, and hexanetriol, and copolymers and combinations thereof. (4) The composition according to any one of embodiments 1 to 3, which is in the form of a lotion. (5) The composition of any one of embodiments 1 to 4, having a rheometer viscosity at 22°C of about 2,000 to about 18,000 cPs.
[0135] (6) The composition of any one of embodiments 1 to 5, having a rheometer viscosity of about 8,000 to about 10,000 cPs at 22°C. (7) The composition according to any one of embodiments 1 to 6, having a pH of about 3 to about 5. (8) The composition of any one of embodiments 1 to 7, further comprising about 0.5% to about 5% by weight of salicylic acid. (9) The composition of any one of embodiments 1 to 7, which is substantially free of salicylic acid. (10) The composition according to any one of embodiments 1 to 9, which is substantially free of lactic acid.
[0136] (11) The composition of any one of the preceding claims, wherein the salt-tolerant thickening polymer comprises a naturally derived polymer, or the salt-tolerant thickening polymer comprises sulfonate groups. (12) The composition of any one of the preceding claims, wherein the salt-tolerant thickening polymer is selected from the group consisting of polyacrylate crosspolymer-6, hydroxyethyl acrylate / sodium acryloyldimethyltaurate copolymer, and combinations thereof. (13) The composition of any one of the preceding claims, wherein the salt-tolerant thickening polymer comprises hydroxyethyl cellulose. (14) A composition for treating acne, comprising: a. about 2.5% by weight to about 7.5% by weight of glycolic acid; b. about 1% to about 5% by weight of gluconolactone; c. about 1% to about 5% by weight of mandelic acid; d. about 2.5% to about 7.5% by weight of propylene glycol; e. about 0.5% to about 2% by weight of polyacrylate crosspolymer-6; f. about 0.5% to about 2% by weight of hydroxyethyl acrylate / sodium acryloyldimethyltaurate copolymer; wherein the total amount of glycolic acid, gluconolactone, and mandelic acid is less than about 12% by weight of the total composition. (15) The composition according to embodiment 14, which is in the form of a lotion.
[0137] (16) The composition of any one of embodiments 14 to 15, having a rheometer viscosity of about 2,000 to about 18,000 cPs at 22°C. (17) The composition of any one of embodiments 14 to 16, having a rheometer viscosity of about 8,000 to about 10,000 cPs at 22°C. (18) The composition according to any one of embodiments 14 to 17, having a pH of about 3 to about 5. (19) The composition of any one of embodiments 14 to 18, further comprising about 0.5% to about 5% by weight of salicylic acid. (20) The composition according to any one of embodiments 14 to 18, which is substantially free of lactic acid.
[0138] (21) A method for treating acne, comprising: A method of treating acne comprising contacting skin in need of such treatment with a composition comprising a first alpha hydroxy acid, a second alpha hydroxy acid, and a polyhydroxy acid. 22. The method of claim 21, wherein the first alpha hydroxy acid comprises glycolic acid, the second hydroxy acid comprises mandelic acid, and the polyhydroxy acid comprises gluconolactone. (23) The method of any one of embodiments 21 to 22, wherein the total amount of glycolic acid, gluconolactone, and mandelic acid is less than about 15% by weight of the total composition. 24. The method of any one of claims 21 to 23, wherein the total amount of acid in the composition is less than about 15% by weight of the total composition. (25) The method according to any one of embodiments 21 to 24, wherein the composition is left on the skin.
[0139] (26) The method according to any one of embodiments 21 to 25, wherein the composition is in the form of a lotion. (27) The method of any one of embodiments 21 to 26, wherein the composition has a pH of about 3 to about 5. 28. The method of any one of claims 21 to 27, wherein the composition further comprises a glycol selected from the group consisting of glycerin, propylene glycol, butylene glycol, pentylene glycol, hexylene glycol, polyethylene glycol, polypropylene glycol, diethylene glycol, triethylene glycol, caprylyl glycol, glycerol, butanediol, and hexanetriol, and copolymers and combinations thereof. (29) The method of any one of embodiments 21 to 28, wherein the composition is substantially free of lactic acid. 30. The method of any one of claims 21 to 29, wherein the composition is substantially free of salicylic acid.
[0140] (31) A method for treating acne, comprising: treating skin in need of such treatment with a. about 0.1% by weight to about 7.5% by weight of glycolic acid; b. about 0.1% to about 5% by weight of gluconolactone; c. about 0.1% to about 5% by weight of mandelic acid; d. glycol, e. a salt-tolerant thickening polymer; wherein the total amount of glycolic acid, gluconolactone, and mandelic acid is less than about 15% by weight of the total composition. 32. The method of claim 31, wherein the total amount of acid in the composition is less than about 15% by weight of the total composition. (33) The method of any one of embodiments 31 and 32, wherein the composition is left on the skin. (34) The composition according to any one of embodiments 31 to 33, which is in the form of a lotion. (35) The composition of any one of embodiments 31 to 34, wherein the composition has a pH of about 3 to about 5.
[0141] 36. The composition of any one of embodiments 31 to 35, wherein the composition further comprises a glycol selected from the group consisting of glycerin, propylene glycol, butylene glycol, pentylene glycol, hexylene glycol, polyethylene glycol, polypropylene glycol, diethylene glycol, triethylene glycol, caprylyl glycol, glycerol, butanediol, and hexanetriol, and copolymers and combinations thereof. (37) The composition according to any one of embodiments 31 to 36, which is substantially free of lactic acid. (38) The composition of any one of embodiments 31 to 37, which is substantially free of salicylic acid. 39. The composition of any one of embodiments 31 to 38, wherein the salt-tolerant thickening polymer comprises a naturally derived polymer or the salt-tolerant thickening polymer comprises sulfonate groups. 40. The composition of any one of claims 31 to 39, wherein the salt-tolerant thickening polymer is selected from the group consisting of polyacrylate crosspolymer-6, hydroxyethyl acrylate / sodium acryloyldimethyltaurate copolymer, and combinations thereof.
[0142] (41) A method for disrupting a biofilm or killing bacteria contained in a biofilm, comprising applying to a surface having a biofilm a composition comprising a first alpha hydroxy acid, a second alpha hydroxy acid, and a polyhydroxy acid. (42) The method of embodiment 41, wherein the surface is a surface on the skin. (43) The method of embodiment 41 or 42, wherein the skin has acne. (44) The method according to any one of embodiments 41 to 43, wherein the biofilm contains Propionibacterium acnes bacteria. 45. The method of any one of embodiments 41-44, wherein the first alpha hydroxy acid comprises glycolic acid, the second hydroxy acid comprises mandelic acid, and the polyhydroxy acid comprises gluconolactone.
[0143] (46) The method of any one of embodiments 41 to 45, wherein the total amount of glycolic acid, gluconolactone, and mandelic acid is less than about 15% by weight of the total composition. 47. The method of any one of claims 41 to 46, wherein the total amount of acid in the composition is less than about 15% by weight of the total composition. (48) The method according to any one of embodiments 41 to 47, wherein the composition is in the form of a lotion. (49) The method of any one of embodiments 41 to 48, wherein the composition has a pH of about 3 to about 5. 50. The method of any one of embodiments 41 to 49, wherein the composition further comprises a glycol selected from the group consisting of glycerin, propylene glycol, butylene glycol, pentylene glycol, hexylene glycol, polyethylene glycol, polypropylene glycol, diethylene glycol, triethylene glycol, caprylyl glycol, glycerol, butanediol, and hexanetriol, and copolymers and combinations thereof.
[0144] (51) The method of any one of embodiments 41 to 50, wherein the composition is substantially free of lactic acid. 52. The method of any one of embodiments 41 to 51, wherein the composition is substantially free of salicylic acid. (53) A method for destroying a biofilm or killing bacteria contained in a biofilm, comprising applying to a surface having a biofilm: a. about 0.1% by weight to about 7.5% by weight of glycolic acid; b. about 0.1% to about 5% by weight of gluconolactone; c. about 0.1% to about 5% by weight of mandelic acid; d. glycol, e. a salt-tolerant thickening polymer; wherein the total amount of glycolic acid, gluconolactone, and mandelic acid is less than about 15% by weight of the total composition; the composition has a pH of about 3 to about 5; A method for disrupting a biofilm or killing bacteria contained in a biofilm, wherein the surface is a surface on the skin. (54) The method of embodiment 53, wherein the skin has acne. (55) The method of any one of embodiments 53 and 54, wherein the biofilm contains Propionibacterium acnes bacteria.
[0145] (56) The method of any one of embodiments 53 to 55, wherein the total amount of acid in the composition is less than about 15% by weight of the total composition. 57. The method of any one of embodiments 53 to 56, wherein the composition further comprises a glycol selected from the group consisting of glycerin, propylene glycol, butylene glycol, pentylene glycol, hexylene glycol, polyethylene glycol, polypropylene glycol, diethylene glycol, triethylene glycol, caprylyl glycol, glycerol, butanediol, and hexanetriol, and copolymers and combinations thereof. (58) The method of any one of embodiments 53 to 57, wherein the composition is substantially free of lactic acid. 59. The method of any one of embodiments 53 to 58, wherein the composition is substantially free of salicylic acid. 60. The method of any one of claims 53 to 59, wherein the salt-tolerant thickening polymer is selected from the group consisting of polyacrylate crosspolymer-6, hydroxyethyl acrylate / sodium acryloyldimethyltaurate copolymer, and combinations thereof.
Claims
1. 1. A composition for treating acne, comprising: a. about 0.1% to about 7.5% by weight of glycolic acid; b. about 0.1% to about 5% by weight of gluconolactone; c. about 0.1% to about 5% by weight of mandelic acid; d. glycol; e. a salt-tolerant thickening polymer; Including, the total amount of glycolic acid, gluconolactone, and mandelic acid is less than about 15% by weight of the total composition; A composition for treating acne that is free of lactic acid or contains less than 0.1% by weight of lactic acid.
2. 10. The composition of claim 1, wherein the total amount of glycolic acid, gluconolactone, and mandelic acid is at least about 2% by weight of the total composition.
3. 3. The composition of claim 1 or 2, wherein the glycol is selected from the group consisting of glycerin, propylene glycol, butylene glycol, pentylene glycol, hexylene glycol, polyethylene glycol, polypropylene glycol, diethylene glycol, triethylene glycol, caprylyl glycol, glycerol, butanediol, and hexanetriol, and copolymers and combinations thereof.
4. The composition according to any one of claims 1 to 3, which is in the form of a lotion.
5. The composition of any one of claims 1 to 4, having a rheometer viscosity of about 2,000 to about 18,000 cPs at 22°C.
6. The composition of any one of claims 1 to 5, having a rheometer viscosity of about 8,000 to about 10,000 cPs at 22°C.
7. The composition of any one of claims 1 to 6, having a pH of about 3 to about 5.
8. The composition of any one of claims 1 to 7, further comprising about 0.5% to about 5% by weight of salicylic acid.
9. A composition described in any one of claims 1 to 7, containing less than about 2% by weight of salicylic acid.
10. The composition of any one of claims 1 to 9, wherein the salt-tolerant thickening polymer comprises a naturally derived polymer or wherein the salt-tolerant thickening polymer comprises sulfonate groups.
11. 11. The composition of any one of claims 1 to 10, wherein the salt-tolerant thickening polymer is selected from the group consisting of polyacrylate crosspolymer-6, hydroxyethyl acrylate / sodium acryloyldimethyltaurate copolymer, and combinations thereof.
12. The composition of any one of claims 1 to 11, wherein the salt-tolerant thickening polymer comprises hydroxyethyl cellulose.
13. A composition comprising: a. about 2.5% to about 7.5% by weight of glycolic acid; and b. about 1% to about 5% by weight of gluconolactone; c. about 1% to about 5% by weight of mandelic acid; d. about 2.5% to about 7.5% by weight of propylene glycol; e. about 0.5% to about 2% by weight of polyacrylate crosspolymer-6; f. about 0.5% to about 2% by weight of hydroxyethyl acrylate / sodium acryloyldimethyltaurate copolymer; 2. The composition of claim 1, comprising:
14. 14. The composition of claim 13 in the form of a lotion.
15. 15. The composition of claim 13 or 14, having a rheometer viscosity of about 2,000 to about 18,000 cPs at 22°C.
16. The composition of any one of claims 13 to 15, having a rheometer viscosity of about 8,000 to about 10,000 cPs at 22°C.
17. The composition of any one of claims 13 to 16, having a pH of about 3 to about 5.
18. The composition of any one of claims 13 to 17, further comprising from about 0.5% to about 5% by weight of salicylic acid.
19. 1. A composition for use in a method of treating acne, said method comprising contacting skin in need of such treatment with the composition; The composition comprises: a. about 0.1% to about 7.5% by weight of glycolic acid; b. about 0.1% to about 5% by weight of gluconolactone; c. about 0.1% to about 5% by weight of mandelic acid; d. glycol; e. a salt-tolerant thickening polymer; Including, the total amount of glycolic acid, gluconolactone, and mandelic acid is less than about 15% by weight of the total composition; A composition for use in a method for treating acne, the composition being free of lactic acid or containing less than 0.1% by weight of lactic acid.
20. 20. The composition of claim 19, wherein the total amount of acid in the composition is less than about 15% by weight of the total composition.
21. 21. The composition of claim 19 or 20, wherein the composition is left on the skin.
22. The composition according to any one of claims 19 to 21, which is in the form of a lotion.
23. The composition of any one of claims 19 to 22, wherein the composition has a pH of from about 3 to about 5.
24. 24. The composition of any one of claims 19 to 23, wherein the glycol is selected from the group consisting of glycerin, propylene glycol, butylene glycol, pentylene glycol, hexylene glycol, polyethylene glycol, polypropylene glycol, diethylene glycol, triethylene glycol, caprylyl glycol, glycerol, butanediol, and hexanetriol, and copolymers and combinations thereof.
25. A composition according to any one of claims 19 to 24, comprising less than about 2% by weight of salicylic acid.
26. 26. The composition of any one of claims 19 to 25, wherein the salt-tolerant thickening polymer comprises a naturally derived polymer or wherein the salt-tolerant thickening polymer comprises sulfonate groups.
27. 27. The composition of any one of claims 19 to 26, wherein the salt-tolerant thickening polymer is selected from the group consisting of polyacrylate crosspolymer-6, hydroxyethyl acrylate / sodium acryloyldimethyltaurate copolymer, and combinations thereof.
Citation Information
Patent Citations
Anti-irritants in cosmetic compositions
CN1298292A
Therapeutic effect increasing method and therapeutic drug composition
JP1988166837A
Composition containing 2-hydroxycarboxylic acid and related compound and method for relieving symptoms of dermotological aging
JP1993139947A
Acid cosmetic, pharmaceutical and dermatological agents
JP2002205915A
Anti-irritation agent in cosmetic compositions
JP2002504504A