EA041056B1 - STABILIZED EMULSIONS WITH ACID AGENTS - Google Patents

Description

Cross-reference to related applications

This application claims priority of U.S. Patent Application No. 16/439,509, filed June 12, 2019, which claims priority of U.S. Patent Application No. 62/683,960, filed June 12, 2018, which is incorporated herein by reference in its entirety .

The field of technology to which the invention belongs

The invention relates to emulsion compositions containing certain active ingredients. These emulsion compositions are typically of the glycerol-in-oil type and contain hydroxy acids. The combination of polyols with certain active ingredients has been found to inhibit the potential irritant properties of the active ingredients. When applied to the lips, the combination may provide therapeutic and/or cosmetic benefits, including smoother lips, increased hydration, reduced moisture loss, and combinations thereof. Methods for preparing these emulsions are also presented.

Prerequisites for the invention

The skin on the lips is structurally different from the skin on other parts of the human body. Lips have a thinner stratum corneum and less lipids than non-lip or normal skin. This allows water to easily pass through the lips and evaporate from them. In fact, the loss of water through the lips is 10 times greater than the loss of water through normal skin. This makes the lips more prone to dryness and more damage over time. The stratum corneum of the lips also has a high turnover rate, which means that the corneocytes are constantly being shed. As part of the exfoliation process, dead skin cells accumulate into scales on the surface of the lips. If the lips are dry, then these scales become more visible. Due to differences in the skin of the lips compared to the rest of the body, the thinner stratum corneum, together with a higher cell turnover rate, makes the lips more susceptible to environmental, mechanical and chemical influences. These factors lead to the feeling of dry, chapped lips and the visual scaling that occurs when the lips are damaged beyond the skin's natural ability to heal itself.

Accordingly, consumers are in need of effective lip care that hydrates, heals and smoothes the vulnerable and delicate surface of the lips. Most lip products on the market are made up of occlusive oils or waxes that limit the amount of moisture leaving the lips. These systems ultimately rely on the skin's natural ability to heal itself. These products do not address any cause of dryness, but only prevent further drying. Some products also contain moisturizing ingredients and healing ingredients. The effectiveness of such products is in a wide range.

Typically, lipstick products are anhydrous systems. These systems consist of a combination of builders, emollients and pigment materials. Lipsticks may also contain 0.05 to 3% of a humectant such as glycerin. There have also been cases where lipsticks, which are an emulsion, usually consisted of at least two phases, which partially or completely did not mix with each other. Glycerol-in-oil type emulsions are of particular interest in the lip and skin areas as they can provide moisture above and beyond the levels achievable in single phase oil based systems. It is generally known that emulsions using glycerol instead of water, either in continuous or discontinuous phases, produce higher levels of moisture than can be achieved with water alone.

However, these emulsion lipsticks often suffer from stability issues. To minimize the thermodynamically unfavorable interaction between the phases due to the immiscibility of the phases in the emulsion, there is a tendency for the phases to separate over time. As is known, emulsions undergo phase separation due to destabilizing processes such as separation, flocculation, coalescence, and Ostwald ripening.

Emulsifiers can be used to combat destabilization of the emulsion. For example, the emulsifier may be selected specifically for the type of emulsion being used. For systems with low pH in the aqueous phase (or apparent pH where applicable), several common emulsifiers can be used, such as PEG-2 stearate and steareth-2. It is also known that the thickening of the outer phase relative to the inner phase increases the stability of the emulsion.

However, the inclusion in these systems of certain active substances, such as αhydroxy acids, leads to an increase in the concentration of electrolytes in the dispersed phase, which, in turn, affects the stabilizing mechanism provided by the emulsifier. For example, these electrolytes can destabilize emulsifiers/stabilizers based on electrostatic repulsion. However, for some active ingredients the required pH is too low for standard emulsion stabilization mechanisms.

In addition, α-hydroxy acids are generally not applied to the lips due to lip skin irritation due to low operating pH ranges. This irritation is enhanced for the lips compared to the skin due to the unique structural and morphological characteristics of the skin of the lips. Ingredients, content

- 1 041056 Aggressive α-hydroxy acids, such as glycolic and lactic acid, when applied to the face can cause significant discomfort in some people and symptoms of severe skin irritation in others.

Emulsions of the glycerin-in-oil type are particularly sensitive to these changes in the internal phase, where destabilization and syneresis of the internal glycerol phase on the surface can appear as lipstick bleeding. This instability can be exacerbated by exposure to extreme temperatures and high humidity due to the moisturizing properties of glycerin. In order to be commercially viable, the emulsion must exhibit sufficient stability to fluctuations in temperature and humidity. However, limitations regarding the stability of glycerol in oil have prevented any commercial viability.

Brief description of the invention

Thus, it is an object of the present invention to provide stable lipsticks based on an emulsion of the glycerin-in-oil type containing one or more α-hydroxy acids. These lipsticks overcome many of the problems previously found when applying certain active substances (eg, α-hydroxy acids) to the skin of the lips. It has been found that these pomades unexpectedly provide enhanced therapeutic and/or cosmetic effects compared to moisturizing pomades based solely on occlusive mechanisms of action or other active ingredients (eg vitamin E). Factors provided by combinations of polyols and certain acidic active ingredients (e.g. α-hydroxy acids, etc.) can combine to provide a smoother lip surface, increased water retention in the lips, improved barrier functions, thicker stratum corneum, increased hydration and their combinations. Moreover, the pomades of the present invention may have increased stability and therefore the ability to include a wider range of active ingredients (eg, α-hydroxy acids, etc.) that do not interfere with the emulsion stabilization mechanism described herein.

A method for providing a therapeutic and/or cosmetic effect on the lips is presented, involving the application of an emulsion composition for topical use containing glycerol and one or more α-hydroxy acids. In preferred embodiments, the emulsion contains one α-hydroxy acid and the apparent pH of the glycerol phase is close to the pK _{a of} the α-hydroxy acid. The amount of irritation (or the strength of the composition) can be controlled by changing the pH of the phases containing the acid, since at a pH value approaching the pK _a in an aqueous system, the acid equilibrium is established with approximately 50% acid and 50% of the corresponding salt of the acid. For example, if the α-hydroxy acid is lactic acid (pK _a = 3.86), then the apparent pH of the glycerol phase may be from 3.3 to 4.3 (for example, from 3.4 to 4.2, from 3.5 to 4.1, 3.6 to 4.0, 3.7 to 3.9, 3.7 to 4.0, etc.).

In some embodiments, the lip composition may be in the form of an emulsion containing a glycerol internal phase and one or more α-hydroxy acids. In some embodiments, the glycerol phase has a first normal stress difference (viscosity at volume expansion index) of less than 20 Pa (e.g., less than 15 Pa, less than 10 Pa, less than 8 Pa, etc.) at a shear stress of 100 Pa, and temperature 25°C.

Preferably, the lip composition is in the form of a glycerol-in-oil type emulsion containing one or more α-hydroxy acids.

Brief description of graphic materials

In FIG. 1 illustrates the differences in light refraction between healthy and unhealthy lips;

in fig. 2A shows the average percentage change in corneometer readings for each clinical study sample. * denotes statistically significant results with respect to lip measurement at baseline with p<0.05 significance, and x denotes those results with p<0.10 statistical significance;

in fig. 2B is the mean percentage change in TEWL measurements for each clinical study sample;

in fig. 2C is the average percentage change in barrier function for each clinical study sample.

Detailed description of the invention

This document discloses detailed embodiments of the present invention; however, it should be understood that the disclosed embodiments are merely illustrative of the present invention, which may be embodied in various forms. In addition, each of the examples given with respect to various embodiments of the invention is intended to be illustrative and not limiting.

It is assumed that all terms in this document are used in their usual meaning in the art, unless otherwise indicated. All concentration values are expressed as a percentage by weight of the indicated component relative to the total weight of the composition for topical application, unless indicated.

- 2 041056 other.

As used herein, the singular forms also include the plural. The singular forms used in this document with the word containing also include the plural. Used in this document, the term other means at least the second or more.

All ranges of numerical values used herein include the endpoints and all possible values disclosed between the disclosed values. The exact values of all half-integer numeric values are also considered to be specifically disclosed and as limits to all subsets of the disclosed range. For example, a range of 0.1 to 3% specifically discloses percentages of 0.1, 0.5, 1, 1.5, 2.0, 2.5, and 3%. In addition, the 0.1 to 3% range includes subsets of the original range, including 0.5 to 2.5%, 1 to 3%, 0.1 to 2.5%, and so on.

It should be understood that the sum of all wt.% of the individual components will not exceed 100%.

As used herein, the term oil is intended to include silicone oils unless otherwise noted. The term oil is intended to encompass volatile and/or non-volatile oils. It should be understood that the oil phases of the compositions may contain one or more silicone oils as a major or different component of the oil phase.

The terms internal and dispersed phase are synonymous, as are the terms external and continuous phase. The terms glycerol and glycerol are synonymous and are used interchangeably. It will also be appreciated that the aqueous phases of the compositions may contain one or more polyols (e.g., glycerol, etc.) as a component other than the base, and the phases of the polyol-based compositions (e.g., glycerol, etc.) may include water as a component other than the main one.

By close to pKa with respect to the pH of the phase is meant that the phase has a pH value approaching the specified pKa value. In some embodiments, the pH may be within 0.5 pH units relative to pKa (i.e. pH = pKa ± 0.5), 0.4 pH units relative to pKa (i.e. pH = pKa ± 0.4) , 0.4 pH units relative to pKa (i.e. pH = pKa ± 0.4), 0.3 pH units relative to pKa (i.e. pH = pKa ± 0.3), 0.2 pH units relative to pKa (i.e. pH = pKa ± 0.2), etc.

The compositions of the present invention are used for application to the skin, lips, nails, hair and other keratinized surfaces. As used herein, the term keratinized surface means the keratin-containing portions of the human integumentary system, which includes, without limitation, skin, lips, hair (including eyebrows and eyelashes), and nails (toenails, fingernails, supranails, etc.). e) mammals, preferably humans. Preferably the compositions are applied to the lips.

The compositions are in the form of an emulsion with a polyol-based phase and/or an aqueous phase. Typically, emulsions may contain water and/or glycerin. In some embodiments, the emulsions may be polyol-in-oil, oil-in-polyol, glycerin-in-oil, oil-in-glycerin, silicone-in-glycerin, glycerin-in-silicone, silicone-in-oil emulsions. polyol or polyol-in-silicone. In preferred embodiments, the emulsion is a polyol-in-oil or glycerol-in-oil emulsion. Emulsions may contain an anhydrous external phase (eg an oil phase, a silicone-based phase, etc.). In some embodiments, the implementation of the emulsion may contain an internal phase, which is an aqueous phase, a phase based on polyol or glycerin.

In certain embodiments, the composition is a polyol-in-oil type emulsion containing a discontinuous internal phase based on a polyol (e.g., glycerol, etc.) and one or more hydroxy acids (e.g., α-hydroxy acid, β-hydroxy acid, etc. ). In most embodiments, the composition is a glycerol-in-oil type emulsion. In certain embodiments, the implementation of the composition contains one α-hydroxy acid. In embodiments with a single α-hydroxy acid, the apparent pH of the polyol-based phase is close to the pKa of the α-hydroxy acid. The internal phase usually makes up from 1 to 65% by weight of the total emulsion. More often, the internal phase will comprise from 5 to 45% by weight of the total emulsion. The outer phase typically contains 25 to 95% (eg 55 to 85%) by weight of the total emulsion.

Suitable polyols for inclusion in emulsions include, without limitation, C ₂ _ ₆ polyols such as ethylene glycol, propylene glycol, butylene glycol, hexylene glycol, sorbitol, diethylene glycol and glycerin. In most embodiments, the internal phase contains glycerol. In some embodiments, the polyol-based phase will contain glycerol in combination with one or more additional C ₂ _ ₆ polyol components. In some embodiments, the implementation of the phase based on the polyol will additionally contain water, in addition to water, which is naturally absorbed by the phase based on the polyol due to its hygroscopicity.

The active ingredient may be an exfoliating agent. Suitable exfoliants include α-hydroxy acids, β-hydroxy acids, keto acids, retinoic acid, lactamides, C4 hydroxylated quaternary ammonium lactates. ₁₂ -carboxylic acids,

- 3 041056 salicylic acid and their various derivatives. Examples include glycolic acid, lactic acid, citric acid, malic acid, mandelic acid, tartronic acid, tartaric acid, glucuronic acid, pyruvic acid, 2-hydroxyalkanoic acid, 2-hydroxyisobutyric acid, 3-hydroxybutyric acid, and their derivatives (e.g., esters and reverse esters with alcohols containing from one to six carbon atoms, such as methyl pyruvate). Other active ingredients may include vitamin A2 (3,4-didehydroretinol), hepaxanthin (vitamin A epoxide; 5-6-epoxy-5,6-dihydroretinol), and additional compound derivatives. In certain embodiments, the compositions contain an α-hydroxy acid. In preferred embodiments, the compositions contain lactic acid. In some embodiments, one or more active agents are present in an amount of 0.1 to 20% by weight of the composition (eg, 0.5 to 10%, 0.5 to 5%, etc.).

Depending on the active ingredient, the apparent pH of the polyol-based phase or the pH of the aqueous phase can be modified to create less irritating materials based on the active ingredient (eg, hydroxy acid conjugate bases). For example, the addition of basic salts (eg, sodium hydroxide, potassium hydroxide, magnesium hydroxide) can be used to change the pH and balance the acid balance in the phase. Typically, the polyol is within 0.5 pH units (eg, within 0.4 pH, within 0.3 pH, within 0.2 pH) relative to the pK _{a of} the hydroxy acid. In some embodiments, the implementation of the basic salt is present in an amount of from 0.1 to 5 wt.% of the composition.

In some embodiments, the external (continuous) phase is an oil phase. For example, the continuous oil phase may contain any oils suitable for emulsions, including, without limitation, vegetable oils; esters of fatty acids; fatty alcohols; isoparaffins such as isododecane and isoeicosan; hydrocarbon oils such as mineral oil, liquid paraffin and polyisobutene; polyolefins and their hydrogenated analogs (eg hydrogenated polyisobutene); natural or synthetic waxes; silicone oils such as dimethicones, cyclic silicones and polysiloxanes, and the like.

Suitable ester oils include fatty acid esters. Specific mention can be made of those esters which are commonly used as emollients in cosmetic formulations. Such esters will generally be the esterification product of an acid as R^COOH)^ with an alcohol as R ₅ (OH) ₁₃ , where R ₄ and R ₅ are each independently a straight, branched or cyclic hydrocarbon group, optionally containing unsaturated bonds (for example, 1-6, or 1-3, or 1) and containing from 1 to 30 (for example, 6-30, or 8-30, or 12-30, or 16-30) carbon atoms, optionally substituted with one or several functional groups, including hydroxyl, oxa, oxo and the like. Preferably, at least one of R ₄ and R ₅ contains at least 8, or at least 10, or at least 12, or at least 16, or at least 18 carbon atoms, thus the ester contains at least one fatty acid chain. Esters as defined above will include, without limitation, esters of monobasic acids with monohydric alcohols, monobasic acids with diols and triols, dibasic acids with monohydric alcohols, and tribasic acids with monohydric alcohols.

Suitable fatty acid esters include, but are not limited to, butyl acetate, butyl isostearate, butyl oleate, butyl octyl oleate, cetyl palmitate, cetyl octanoate, cetyl laurate, cetyl lactate, cetyl isononanoate, cetyl stearate, diisostearyl fumarate, diisostearyl malate, neopentyl glycol dioctanoate, dibutyl sebacate, di-C ₁₂ . ₁₃ αлкилмалат, дицетеарил димер дилинолеат, дицетиладипат, диизоцетиладипат, диизонониладипат, диизопропилдимерат, триизостеарилтрилинолеат, октодецилстеароилстеарат, гексиллаурат, гексадецил-изостеарат, гексадециллаурат, гексилдецилоктаноат, гексилдецилолеат, гексилдецилпальмитат, гексилдецилстеарат, изононил-изононаноат, изостеарил-изононат, изогексилнеопентаноат, изогексадецилстеарат, изопропил-изостеарат , н-пропилмиристат, изопропилмиристат, нпропилпальмитат, изопропилпальмитат, гексакозанилпальмитат, лауриллактат, октакозанилпальмитат, пропиленгликольмонолаурат, триаконтанилпальмитат, дотриаконтанилпальмитат, тетратриаконтанилпальмитат, гексакозанилстеарат, октакозанилстеарат, триаконтанилстеарат, дотриаконтанилстеарат, стеариллактат, стеарилоктаноат, стеарилгептаноат, стеарилстеарат, тетратриаконтанилстеарат, триарахидин, трибутилцитрат, триизостеарилцитрат, три -C ₁₂ . ₁₃ alkyl citrate, tricaprylin, tricaprylyl citrate, tridecyl behenate, trioctyldodecyl citrate, tridecyl cocoate, tridecyl isononanoate, glyceryl monoricinoleate, 2-octyldecyl palmitate, 2-octyldodecyl myristate or lactate, di(2-ethylhexyl)succinate, tocopheryl acetate, and the like.

Other suitable esters include those in which R ₅ is a polyglycol of the form H-(O-CHR*-CHR*) _n - where R* is independently selected from hydrogen or C ₁ . ₁₂ straight chain α-alkyl, including methyl and ethyl, an example of which is polyethylene glycol monolaurate.

The oil may also include a volatile or non-volatile silicone oil. Suitable silicone oils include straight or cyclic silicones such as polyalkyl or polyarylsiloxanes, optionally containing alkyl or alkoxy groups, which contain from 1 to 10

- 4 041056 carbon atoms. Иллюстративные силиконовые масла включают, например, каприлилметикон, циклометикон, циклопентасилоксан декаметилциклопентасилоксан, декаметилтетрасилоксан, дифенилдиметикон, додекаметилциклогексасилоксан, додекаметилпентасилоксан, гептаметилгексилтрисилоксан, гептаметилоктилтрисилоксан, гексаметилдисилоксан, метикон, метил-фенилполисилоксан, октаметилциклотетрасилоксан, октаметилтрисилоксан, перфторнонилдиметикон, полидиметилсилоксаны и их комбинации. The silicone oil will have a viscosity, typically but not necessarily 5 to 3000 centistokes (cSt), preferably 50 to 1000 cSt, measured at 25°C.

In one embodiment, the silicone oil contains phenyl groups, as is the case for a silicone oil such as methylphenylpolysiloxane (INCI name diphenyldimethicone) commercially available from Shin Etsu Chemical Co. under the name including F-5W, KF-54 and KF-56 . Diphenyl dimethicones have good organic compatibility and can impart film-forming characteristics to the product. In addition, the presence of phenyl groups increases the refractive index of the silicone oil and thus, if desired, can contribute to a high gloss product. In one embodiment, the silicone oil will have a refractive index of at least 1.3, preferably at least 1.4, more preferably at least 1.45, and even more preferably at least 1.5 when measured at 25°C. Another suitable phenyl-functionalized silicone oil has the INCI name phenyl trimethicone and is commercially available under the trade name DC 556 from Dow Corning. DC 556 has a refractive index of 1.46. In one embodiment, the silicone oil is a fluorinated silicone, such as perfluorinated silicone (ie, fluorosilicones). The fluorosilicones are advantageously both hydrophobic and oleophobic and thereby endow the product with the desired glide and tactile characteristics. Fluorosilicones also impart properties that contribute to the long-lasting wear of a lip product. If necessary, the fluorosilicones can be thickened using behenyl behenate. One suitable fluorosilicone is a fluorinated organofunctional silicone fluid having the INCI name perfluoronyl dimethicone. Perfluoronyl dimethicone is commercially available from Phoenix Chemical under the trade name PECOSIL®. The compositions may contain from 5 to 75% silicone oil by weight of the composition (eg, from 10 to 60 wt.% of the composition, from 20 to 50 wt.% of the composition, from 25 to 45 wt.% of the composition, etc.).

The compositions may also contain hydrocarbon oils. Exemplary hydrocarbon oils are straight or branched chain paraffinic hydrocarbons containing 5 to 80 carbon atoms, typically 8 to 40 carbon atoms, and more typically 10 to 16 carbon atoms, including, but not limited to, pentane, hexane, heptane, octane , nonane, decane, undecane, dodecane, tetradecane, tridecane, and the like. Some useful hydrocarbon oils are highly branched aliphatic hydrocarbons, including C ₈ . ₉ isoparaffins, C ₉ . ₁₁ isoparaffins, C ₁₂ isoparaffins, C ₂₀ .4 ₀ isoparaffins and the like. Particular mention should be made of isoparaffins, which have such INCI names as isohexadecane, isoeicosan and isododecane.

Also suitable as hydrocarbon oils are poly-a-olefins containing, as a rule, more than 20 carbon atoms, including (optionally hydrogenated) C _{2 4.28} olefins, C ₃₀ .45 olefins, polyisobutene, hydrogenated polyisobutene, hydrogenated polydecene, polybutene , hydrogenated polycyclopentane, mineral oil, pentahydrosqualene, squalene and the like. The hydrocarbon oil may also include higher fatty alcohols such as oleyl alcohol, octyldodecanol and the like.

Other suitable oils include, but are not limited to, castor oil, C ₁₀ . ₁₈ Triglycerides, Caprylic/Capric/Triglycerides, Coconut Oil, Corn Oil, Cottonseed Oil, Flaxseed Oil, Mink Oil, Olive Oil, Palm Oil, Bassia Nut Oil, Canola Oil, Soybean Oil, Sunflower Oil, Walnut Oil, Avocado Oil , camellia oil, macadamia oil, turtle oil, mink oil, soybean oil, grape seed oil, sesame oil, maize oil, rapeseed oil, sunflower oil, cottonseed oil, jojoba oil, peanut oil, olive oil, and combinations thereof.

It is contemplated that any of the above ester oils, silicone oils, and hydrocarbon oils may be practiced in accordance with the present invention. Therefore, in one embodiment, the compositions contain at least one oil selected from the ester oils, silicone oils, and hydrocarbon oils described above. In another embodiment, the compositions contain two or more oils selected from the ester oils, silicone oils, and hydrocarbon oils described above. In yet another embodiment, the compositions will contain at least one ester oil, at least one silicone oil, and at least one hydrocarbon oil from the list above. Since the ester oils described herein function as emollients, it may be preferred that the compositions contain at least one ester oil, and they may optionally contain at least one additional oil selected from hydrocarbon materials.

- 5 041056 villages, silicone oils and their combinations. For example, in some embodiments, the compositions contain lanolin, stearyl dimethicone, myristyl lactate, and diphenyl dimethicone.

Waxes and/or fillers can also optionally be added (particularly in those embodiments where the composition is a shape-retaining solid at room temperature) in an amount ranging from 1 to 20%, inclusive, by weight of the composition, or in the range from 1 up to 10% inclusive by weight of the composition. Examples of fillers may include, without limitation, silica, PMMA, nylon, alumina, barium sulfate, or any other filler used in such compositions. Examples of waxes may include, but are not limited to, linear polyethylene, microcrystalline petroleum wax, carnauba wax, lignite wax, urikuri wax, rice bran wax, castor wax, building wax, stearon, Acrawax, waxwort, castor wax, sumac fruit wax, ozocerite, beeswax , candelilla wax, liquid paraffin, ceresin wax, cocoa butter, bassia nut oil, esparto wax, shellac wax, diesters or triesters of ethylene glycol and C ₁₈ - ₃₆ fatty acids, cetyl palmitate, hard fat, hard paraffin, lanolin, lanolin alcohol, cetyl alcohol, glyceryl monostearate, sugar cane wax, jojoba wax, stearyl alcohol, silicone waxes, and combinations thereof.

In some embodiments, the implementation of the oil phase may include one or more waxes. The wax can impart consistency to the emulsion so that the emulsion has the physical form of a semi-solid or solid. As used herein, the term solid is intended to mean a composition that retains shape and is suitable for molding into a shape-retaining stick (eg, lipstick). In some embodiments, the waxes are present in an amount sufficient to form the emulsion into a solid emulsion. For example, a solid emulsion may have a hardness of at least 30 g. The composition typically has a hardness of at least 40 g at room temperature. In one embodiment, the composition may have a significantly higher hardness, from 100 to 300 g. The hardness of the emulsion may be measured using a model QTS-25 texture analyzer equipped with a 4 mm stainless steel probe (TA-24) as described in the US Pat. No. 8580283 issued by Avon, the disclosure of which is incorporated herein by reference.

Waxes can be natural, mineral and/or synthetic. Natural waxes include animal-based waxes (eg, beeswax, spermaceti, lanolin, and shellac wax) and plant-based waxes (eg, carnauba, candelilla waxes, waxwort, and sugar cane wax). Mineral waxes include, but are not limited to, ozokerite, ceresin, montan wax, paraffin, microcrystalline, petroleum wax, and liquid paraffin. Synthetic waxes include, for example, polyethylene glycols such as PEG-18, PEG-20, PEG-32, PEG-75, PEG-90, PEG-100 and PEG-180, available on the market under the trade name CARBOWAX® (The Dow Chemical company). Mention should be made of the polyethylene glycol wax CARBOWAX 1000 which has a molecular weight in the range of 950 to 1050 and a melting point of 38°C, CARBOWAX 1450 which has a molecular weight in the range of 1305 to 1595 and a melting point of 56°C, CARBOWAX 3350 which has a molecular weight in the range of 3015 to 3685 and a melting point of 56°C, and CARBOWAX 8000 which has a molecular weight in the range of 7000 to 9000 and a melting point of 61°C.

Synthetic waxes also include Fischer-Tropsch (FT) waxes and polyolefin waxes such as ethylene homopolymers, ethylene-propylene copolymers, and ethylene-hexene copolymers. Exemplary ethylene homopolymer waxes are commercially available under the tradename POLYWAX® Polyethylene (Baker Hughes Incorporated) with melting points ranging from 80 to 132°C. Commercially available ethylene-a-olefin copolymer waxes include those commercially available under the tradename PETROLITE® Copolymers (Baker Hughes Incorporated) having melting points ranging from 95 to 115°C.

In one embodiment, the oil phase of the emulsion comprises at least one wax selected from Acrawax (K,K'-ethylene-bis-stearamide), microcrystalline wax, polyethylene-based linear wax, stearone (18-pentatriacontanone), castor wax, montan wax, lignite wax, urikuri wax, carnauba wax, rice bran wax, shellac wax, esparto wax, ozocerite wax, jojoba wax, candelilla wax, ceresin wax, beeswax, castor wax, sugar cane wax, stearyl alcohol, tallow, cetyl alcohol, liquid paraffin, glyceryl monostearate, sumac fruit wax, silicone wax, hard paraffin, lanolin wax, lanolin alcohol, cere wax, cetyl palmitate, bassia nut oil, cocoa butter, and di or triesters of ethylene glycol and C ₁₈ _ ₃₆ fatty acids.

The amount of wax, if present, may be less than 2% (eg 0.1-2%) by weight of the composition if the composition is a liquid or if transparency is required. The amount of wax, if present, will typically be greater than 10% (eg, 10-20%) by weight of the composition if the composition is semi-solid or solid, or if transparency is not the goal.

- 6 041056

In some embodiments, the implementation of the emulsion may contain wax in an amount of from 1 to 25%, or 120%, or 1-5%, or 1-10 wt.% of the composition, in particular in embodiments formulated as lipsticks.

The oil phase of the emulsion may also include one or more of thickeners/gelling agents and/or bulking agents that function as structure improvers. Such bulking agents include mica, barium sulfate, nylon, talc, starch, calcium carbonate, silica, and mixtures thereof. Bulking agents may be present in an amount of 0.01 to 5% by weight of the emulsion (eg, 0.1 to 5% by weight of the emulsion, 0.1 to 1% by weight of the emulsion, etc.).

Other thickeners can be used to thicken the internal or external phase of emulsions. For example, polysaccharide thickeners can be used to structure the phase of a polyol emulsion as described in US Patent Publication No. 2015/0164768, incorporated herein by reference in its entirety, and in particular with respect to polysaccharide builders and emulsifiers. However, since xanthan gum has been shown to increase viscosity upon volume expansion of the polyol-based phase (see example 2), in preferred embodiments, the composition does not contain xanthan gum or contains xanthan gum in such small amounts that the first normal stress difference polyol-based phase is not more than 20 Pa. In some embodiments, the implementation of the composition does not contain structure-forming agents in the external phase. In some embodiments, the internal phase may be structured with TiO ₂ qualification for attenuating radiation. The composition may contain 0.1 to 20% (eg, 0.1 to 10%, etc.) TiO ₂ qualification for attenuating radiation by weight of the composition. TiO ₂ radiation attenuation qualifications can be surface treated, for example with hydrophobic modifiers such as lauroyllysine, isopropyltitanium triisostearate (ITT), crosslinked copolymers of ITT and dimethicone (ITT/dimethicone), ITT and amino acids, crosslinked copolymer of ITT and triethoxycaprylylsilane, waxes (e.g., carnauba), fatty acids (e.g., stearates, etc.), HDI-trimethylolhexyl lactone crosslinked copolymer, PEG-8 triethoxysilane methyl ether, aloe extract, jojoba ester, lecithin, perfluoroalcohol phosphate, and magnesium myristate (MM ), to name but a few.

In one embodiment, the oil phase of the composition comprises 0.1-2%, or 2-5%, or 510%, or 10-15%, or 15-20% by weight of at least one wax (e.g., microcrystalline wax, ozocerite wax, wax based on polyethylene, solid paraffin, liquid paraffin, etc.). In one embodiment, the oil phase of the composition includes microcrystalline wax within the above amounts. In one embodiment, the oil phase of the composition includes ozocerite wax within the above amounts. In one embodiment, the oil phase of the composition comprises a polyethylene-based wax in the range of the above amounts. In one embodiment, the oil phase of the composition includes liquid paraffin in the range of the above amounts. In one embodiment, the oil phase of the composition includes solid paraffin within the above amounts.

Typically, the emulsions of the present invention additionally contain one or more emulsifiers. For example, one or more emulsifiers may be present in the general range of 0.01 to 20.0% by weight of the emulsion (eg, 0.1 to 15% by weight of the emulsion). In some embodiments, the implementation of the total amount of emulsifier is in the range from 0.1 to 6.0 wt.% or from 0.5 to 4.0 wt.% emulsions. Examples of emulsifiers include polyglyceryl compounds such as polyglyceryl-6 polyricinoleate, polyglyceryl pentaoleate, polyglyceryl isostearate and polyglyceryl-2-diisostearate; glycerol esters such as glycerol monostearate or glycerol monooleate; phospholipids and phosphate esters such as lecithin and trilaureth-4-phosphate (available under the tradename HOSTAPHAT®KL-340-D); sorbitan-containing esters (including SPAN® esters) such as sorbitan laurate, sorbitan oleate, sorbitan stearate, or sorbitan sesquioleate; polyoxyethylenephenols such as polyoxyethyleneoctylphenol; polyoxyethylene ethers such as polyoxyethylene cetyl ether and polyoxyethylene stearyl ether; polyethylene glycol emulsifiers such as PEG-30-polyhydroxystearate or alkyl polyethylene glycols; polypropylene glycol emulsifiers such as PPG-6-laureth-3; dimethicone polyols and emulsifiers based on polysiloxane; etc. Combinations of emulsifiers are contemplated, such as a combination of lecithin and sorbitan. Additional emulsifiers are listed in INCI Ingredient Dictionary and Handbook, 12th Edition (2008), the disclosure of which is incorporated herein by reference. In some embodiments, the lip composition contains one or more emulsifiers and/or one or more waxes. In preferred embodiments, the lip composition contains 1 to 20% emulsifiers and/or 1 to 20% waxes by weight of the composition.

In some embodiments, compositions may require enhanced stability not available with standard emulsification systems. Methods for improving the stability of polyol-in-oil emulsions are also presented, involving a decrease in viscosity at volumetric

- 7 041056 expansion of the glycerol phase of the specified emulsion. As an approximate indicator of the expansion viscosity, the first normal stress difference of the internal phase at a shear stress of 100 Pa and a temperature of 25°C can be determined. A higher first normal stress difference correlates with higher viscosity during volumetric expansion. It has been found that the stability of a polyol-in-oil type emulsion can be increased by decreasing the viscosity with volume expansion of the internal phase. In some embodiments, the polyol (e.g., glycerol)-based phase has a first normal stress difference of less than 20 Pa (e.g., less than 15 Pa, less than 10 Pa, less than 8 Pa, less than 7 Pa, less than 6 Pa) at a shear stress of 100 Pa and temperature 25°C.

Composite elastomer powders can be included to increase the stability of solid emulsions and to reduce syneresis during extended storage periods. Examples of elastomeric powders include silicone elastomers, which are cross-linked flexible silicones that can withstand large reversible deformations. In some embodiments, the expansion viscosity is reduced by adding a silicone elastomer to the discontinuous phase of the emulsion. The silicone elastomer may be, for example, a crosslinked elastomeric organopolysiloxane powder, including a crosslinked dimethicone copolymer. Such elastomers can be formed, for example, by platinum metal-catalyzed reactions between SiH-containing diorganopolysiloxanes and organopolysiloxanes having silicon-bound vinyl groups. Suitable silicone elastomers include cross-linked dimethicone-vinyl dimethicone copolymers, cross-linked vinyl dimethicone-methicone-silsesquioxane copolymers, and cross-linked dimethicone-phenyl vinyl dimethicone copolymers. Examples include Dow Coining 9040, 9041, and 9506, and Shin-Etsu KSG-15, 16, and 17, and Shin-Etsu KSP-100, 101, 102, 103, 104, 105, 200, and 300. Commercially available powders include Dow Powder Coining 9506 from Dow Corning (INCI name: Dimethicone-Vinyl Dimethicone Crosslinked Copolymer). In particular, the organopolysiloxane elastomer used in the present invention is selected from a crosslinked copolymer of dimethicone (INCI name), a crosslinked copolymer of dimethicone and optionally dimethicone, a crosslinked copolymer of vinyl dimethicone (INCI name), a crosslinked copolymer of dimethicone and vinyl dimethicone (INCI name), a crosslinked a dimethicone-3 copolymer (INCI name); and in particular a crosslinked copolymer of dimethicone and a crosslinked polymer of dimethicone(s) dimethicone.

Composite elastomeric powders can be formed by coating at least a portion of the elastomeric powder particles with an inorganic powder. Typically, the inorganic powder has an average particle size less than the average particle size of the uncoated elastomeric powder. Typically, the average particle size of the inorganic coating powder is less than one tenth the average particle size of the uncoated elastomeric powder. Examples of suitable inorganic powders for making the composite elastomeric powder include metal oxide powders such as silicon oxide, titanium oxide, alumina, zirconium oxide, antimony oxide; metal nitride powders such as boron nitride and aluminum nitride; metal hydroxide powders such as aluminum hydroxide, magnesium hydroxide; metal carbonate salts such as potassium carbonate; metals such as nickel, cobalt, iron, copper, gold and silver; sulfide powders and chloride powders. Preferred powders for coating elastomeric particles include fine powders of metal oxides and in particular silica. Suitable composite elastomeric particles include Dow Coining 9701 powder from Dow Corning (INCI name: Crosslinked Copolymer of Dimethicone and Vinyl Dimethicone (and) Silica).

Typically, the composite elastomeric particles may be coated with a component to impart hydrophilicity and dispersibility to the composite elastomeric particles. This is especially important in an emulsion of the glycerol-in-oil type, where the composite particles can be dispersed throughout the glycerol-in-oil phase. In some embodiments, the composite elastomeric particle contains a monohydric alcohol, such as methanol, ethanol, isodecyl alcohol, isotridecyl alcohol, and/or polyhydric alcohols, including glycols, such as 1,3-butanediol, 1,2-pentanediol, ethylene glycol, dipropylene glycol etc. In some embodiments, the implementation of the composite elastomeric particle is coated with butylene glycol. Such composite elastomeric particles are described in US Pat. No. 9,394,412, which is incorporated herein by reference in its entirety, and in particular with respect to composite cured silicone powders. In preferred embodiments, the composite elastomeric particles include a product commercially available from Dow Coining under the name EP-9801 Hydrocosmetic Powder (INCI name: Cross-linked copolymer of dimethicone and vinyl dimethicone (and) silicon dioxide (and) butylene glycol).

In some embodiments, the composition may be a polyol-in-oil (e.g., glycerol-in-oil) type emulsion and contain 1 to 45% polyol (e.g., 1 to 20%, 5 to 15%) by weight of the composition. , and 0.1 to 5% active ingredient (e.g. α-hydroxy acid such as lactic acid) and 25 to 95% (e.g. 40 to 60%) oil (e.g. lanolin, stearyl dimethicone, myristyl lactate, diphenyl dimethicone and their combinations) by weight of the composition. In some

In other embodiments, the composition further comprises a basic salt (eg sodium hydroxide) in an amount of 0.1 to 5% by weight of the composition.

As is customary in the field of cosmetics, for various functional purposes, you can include additional components in the composition, in particular in the internal phase of the emulsions, in the external phase of the emulsions or in the form of a dispersed phase. However, while additional ingredients suitable for formulating the above cosmetic compositions may be included, the inclusion of additional ingredients is limited to amounts of such ingredients that do not affect the formation or stability of the compositions (eg, emulsions, etc.).

Such components may be selected from the group consisting of film formers, pigments, waxes, emollients, humectants, preservatives, fragrances, antioxidants, botanicals, and mixtures thereof. Special mention should be made of highly purified plant extracts or synthetic agents that may have wound healing, anti-inflammatory or other beneficial effects for skin or lip treatments. Additional embodiments may include antioxidants such as tocopherol and/or α-hydroxy acids such as glycolic acid, lactic acid, etc. The compositions may include one or more film formers to increase the affinity of the product.

Film-forming agents, including film-forming polymers, may also be used. The term film-forming polymer can be understood as a term denoting a polymer that is capable, by itself or in the presence of at least one film-forming aid, of forming a continuous film that adheres to a surface and acts as a binder for the particulate material. Polymeric film-forming agents include, without limitation, acrylic polymers or copolymers, (meth)acrylates, alkyl(meth)acrylates, polyolefins, polyvinyls, polyacrylates, polyurethanes, silicones, polyamides, polyethers, polyesters, fluoropolymers, polyacetates, polycarbonates, polyamides, polyimides, rubbers, epoxy resins, formaldehyde resins, organosiloxanes, dimethicones, amodimethicones, dimethiconols, methicones, silicone acrylates, polyurethane-silicone copolymers, cellulosic polymers, polysaccharides, polyquaterniums, etc. Suitable film formers include those listed in the Cosmetic Ingredient Dictionary (INCI and Handbook, 12th Edition (2008)), the disclosure of which is incorporated herein by reference.

The composition may contain one or more preservatives or antimicrobial agents, such as methyl-, ethyl- or propylparaben, etc., in amounts ranging from 0.0001 to 5% by weight of the entire composition. The compositions may contain other ingredients such as one or more anesthetics, antiallergic, antifungal, anti-inflammatory, antimicrobial, antiseptic, chelating agents, emollients, emulsifiers, fragrances, humectants, lubricants, masking agents, drugs, humectants, pH adjusters, preservatives , protectants, soothing agents, stabilizers, sunscreens, surfactants, thickeners, viscosity enhancers, vitamins, or any combination thereof.

In one embodiment, the emulsions of the present invention are provided as lip products. Such lip products may include lip cream, lip balm, lip gloss, lip healer, lip moisturizer, lip cosmetic, lip sunscreen, and lip fragrance. In one embodiment, the lip product is a creamy, flowable lip product. In certain embodiments, the products of the present invention may have the consistency of a semi-viscous liquid or paste. In other embodiments, the product is a lipstick.

Application of these compositions to keratinized surfaces provides therapeutic and/or cosmetic effects. Also provided are methods for providing therapeutic and/or cosmetic effects to the lips only found when the polyols and exfoliating actives described herein are combined. In some embodiments, the therapeutic and/or cosmetic effect is selected from reduced water loss from said lips, smoother lip surface (compared to untreated lips), increased hydration of said lips (compared to untreated lips), increased barrier function of said lips (by compared to untreated lips), thickened stratum corneum of said lips (compared to untreated lips), and combinations thereof.

The amount of topical composition that is applied each time, the area to which it is applied, the duration of application and the frequency of application can vary greatly depending on the specific needs of the user. For example, the topical composition may be applied over a period of time of at least one month and at a frequency ranging from once a week to twice a week, or twice a week, or every other day, or once once a day, or twice a day (for example, once in the morning and once in the evening, etc.), or three times a day, or four times a day, or five times a day. In some embodiments, one form of composition (e.g., lipstick of the present invention) can be applied one or more

- 9 041056 times (for example, one, two, three, four, five, etc.) during the entire period, and another form of composition (for example, the balm of the present invention) can be applied and left during the night during sleep user.

In most embodiments, the compositions are packaged individually in an individual container. In one embodiment, each of the one or more compositions is contained in a separate container, and multiple containers for the same composition (eg, jars and dispensers) are commercially available and/or packaged together (eg, lipstick and balm). In another embodiment, several compositions (eg, lipstick, balm, cream, etc.) are combined in different containers in one package. In some embodiments, these different containers are not separable from each other.

Examples

The following examples illustrate specific aspects of this description. The examples should not be construed as limiting, as the example only provides a specific understanding and practical application of the embodiments and their various aspects.

Example 1 Measurement of moisture content and water loss on the lips through the epidermis.

Conducted an eight-week clinical study of various formulations applied to the lips. Women with rough lips aged 40-65 years and with skin type Ι-III on the Fitzpatrick scale applied a particular lipstick composition at least 3 times a day. Several groups were instructed to also apply the balm in the evening. Features of the compositions are presented in table. 1. As can be seen, Formulation 1 is a glycerin-in-oil type emulsion containing α-hydroxy acids, and Formulation 2 is a gel-like composition having a lower glycerol content and no α-hydroxy acid. In addition, another group of participants were instructed to apply oBoticario's commercially available Intense lipstick. This Intense lipstick moisturizes lips by preventing water evaporation using a combination of vitamin E and cupuaçu oil. Each group included 9 to 11 participants.

Table 1

Component Composition 1 (wt%) Composition 2 (wt%) Balm (wt%) Oil (e.g. lanolin, stearyl dimethicone, myristyl lactate, diphenyl dimethicone, squalene, diisostearyl fumarate, polybutene, or combinations thereof) 50.11 55.67 52.45 Glycerol 10.00 1.50 10.00 a-hydroxy acid (lactic acid) 2.00 - 2.00

- 10041056

Base (30% ammonium hydroxide) 0.35 - 0.35 Emulsifier (e.g. lauryl methicone copolyol, polyglyceryl-3-diisostearate and combinations thereof) 8.75 - 8.75 Cross-linked dimethicone-vinyl dimethicone copolymer, silicon dioxide and butylene glycol (EP-9801) 3.00 - 3.00 Other powders (e.g., 12 micron polyethylene, E603 acrylate copolymer, cross-linked lauryl methacrylate/glycol dimethacrylate polymer, colloidal silicon dioxide, mica, or combinations thereof) 2.63 2.83 2.63 preservative 0.50 0.50 0.50 Demineralized water 1.00 - 1.00 active ingredients (eg, sunscreen, sweetener, antioxidant, skin protectant, skin conditioner, protein, and combinations thereof) 7.91 13.70 7.91 gelling agent - 2.90 - Bulking agent (e.g. barium sulfate) - 0.40 2.66 Wax 8.75 13.40 8.75 Dyestuffs (e.g. pigments, varnishes, dyes, or combinations thereof) 5.00 9.10 -

For one (1) week, two (2) weeks, four (4) weeks, and eight (8) weeks, lip hydration and barrier function (without product) was assessed by measuring skin electrical capacitance and transepidermal water loss (TEWL). Lip health was also assessed by optical measurement of lip gloss. The images show that incident light on unhealthy lips with an increased number of skin scales and an uneven surface tends to create accentuated lines with shadows.

On healthy lips, the absence of these features suppresses the presence of such shadows. A diagram of the mechanism causing this difference between healthy and unhealthy lips is shown in FIG. 1. In addition, regression period measurements were performed after the eight-week study. At 24 and 72 hours after completion of the application phase of the study, skin capacitance and TEWL of the participants were measured again. During periods of regression, participants did not apply any lip products.

Corneometer (Courage & Khazaka) determines the moisture content of the lips by measuring the electrical capacitance at the surface of the lips. By measuring the electrical capacitance at the surface of the lips, the water content of the lips can be measured based on differences in the permittivity of water and other substances. Higher corneometer readings indicate higher moisture content in the lips. Measurements were taken on the lips without product on them. In FIG. 2A shows the corneometer measurements for each test population at various time points.

TEWL measurements made with a ventilated chamber pan (cyberDERM) reflected the loss of water from the epidermis of the lips at each time point. Measurements were taken on the lips without product on them. A broken barrier results in higher water loss, while lower TEWL values indicate water loss prevention. In FIG. 2B shows the results of TEWL measurements for each population tested at various time points on the inverted y-axis.

The amount of water lost by the lips is affected not only by the barrier, but also by the amount of moisture in the lips. A complete representation of the change in barrier function for the lips of each sample was calculated by subtracting the percentage change in TEWL of each subject from the percentage change in electrical capacitance of the skin. In FIG. 2C shows the change in the barrier function for each sample. In FIG. 2A-2C*

- 11 041056 means statistically significant results with respect to the lip measurement at baseline with p<0.05 significance (two-tailed distribution), and x means those results that approach the significance corresponding to p<0.10 (two-tailed distribution).

Optical measurements showed that in populations treated with glycerol and α-hydroxy acids, lips were healthier and smoother. Moreover, as seen in FIG. 2A-2C, treatment with formulations containing glycerol and α-hydroxy acids resulted in a significant increase in lip hydration and a statistically significant reduction in water loss on untreated skin. In fact, only those subjects who received treatment involving daily multiple treatments with glycerol and αhydroxy acid had significantly less water loss after three days of regression. Moreover, these results are not seen in the commercially available Intensive Moisture Pomade, which works by preventing evaporation using a combination of vitamin E and cupuaçu oil. The combination of α-hydroxy acid and glycerin uniquely provides a smoother lip surface, keeps lips moisturized and reduces water loss on the lips.

Example 2 Measurements of the first normal stress difference of phases based on glycerol with αhydroxy acids.

Before emulsification, the first normal stress difference of several glycerol-based phases (phase) was measured. The components of these phases based on glycerol are shown in table. 2.

_________________________________________________________Table 2

Phase A (d) Phase B (g) Phase C (g) PhaseO (g) Phase E (g) Glycerol 93.60 93.60 93.60 93.60 93.60 Lactic acid - 2.00 2.00 2.00 2.00 Demineralized water - - - 1.00 1.00 Ammonium hydroxide, 30% - - 0.40 0.40 0.40 Cross-linked copolymer of dimethicone and vinyl dimethicone / silicon dioxide / isocetetlO / BG / antiox. - - - - 3.00 xanthan gum 1.00 - - - - Total weight 94.60 95.60 96.00 97.00 100.00

An AR-G2 rheometer from TA Instruments was used to perform viscosity measurements for each of the A-E phases and the 100% glycerol phase using a 2° cone and plate geometry and a gap of 52 µm. The measurements were carried out at a shear stress of 100 Pa and 25°C (77°F). To understand the nature of the change in viscosity during volumetric expansion between the phases in table. 2, you can calculate the first normal stress difference using the formula

N1=2 x Je x η ² x V ² where J _e is the recoverable plasticity, η is the viscosity and V is the shear stress measured by the rheometer. The values of the first difference of normal stresses for each tested glycerol phase and 100% glycerol phase are shown in table. 3.

Table 3

Glycerin (100%) Phase A Phase B Phase C Phase D PhaseE The first difference in normal stresses (Ni \u003d 2 x J _e x η ² χ γ ² , Pa) 0 1315.9 164.0 0 29.6 5.7

A larger value of the first normal stress difference indicates a higher viscosity during volumetric expansion. As can be seen, 100% glycerin does not have a viscosity in volume expansion. However, the addition of various components to the glycerol phase, such as xanthan gum, lactic acid, ammonium hydroxide, and water, results in an increase in viscosity as the glycerol system expands. The incorporation of various silicone elastomers, such as crosslinked dimethicone-vinyl dimethicone/silica/butylene glycol (EP-9801, available from Dow Corning), can reduce the internal phase expansion viscosity.

Example 3 Stability measurements of glycerin-in-oil type emulsions.

Emulsions of the glycerol-in-oil type were prepared to illustrate the stability of emulsions made with various α-hydroxy acids and composite elastomeric polymers. In table. 4 shown

- 12 041056 components of formulations 3-7 tested in stability measurements. ________________________________________________________ Table 4

Composition 3 (wt%) Composition 4 (wt%) Composition 5 (wt%) Composition 6 (wt%) Composition 7 (wt%) Lactic acid 2.00 2.00 2.00 2.00 2.00 Base 0.35 0.40 0.40 0.35 0.35 Conditioner 1.00 1.00 1.00 1.00 1.00 Oil 51.32 54.92 52.57 53.32 48.62 Emulsifier 0.00 0.00 0.00 0.00 0.00 Glycerol 10.00 10.00 10.00 10.00 10.00 Water 1.00 1.00 1.00 1.00 1.00 Cellulose granules 5.00 0.00 0.00 0.00 0.00 Composite elastomeric particles (EP9801) 0.00 1.00 2.00 3.00 5.00 Wax 4.13 8.83 8.83 7.13 11.83 Additional Ingredients! 15.83 19.03 18.03 15.83 18.53

f Additional ingredients may include flavor oil, pigments, other powders, preservatives, sunscreen, sweetener, and combinations thereof.

As can be seen, formulations 3-7 were prepared without emulsifiers, which made it possible to demonstrate the stability effect provided by the composite elastomeric particle. The conditioning agent used in these formulations, a hybrid polymer containing silk protein, silicone and an alkyl group (Protosil LH available from SEPPIC) may provide some emulsion stability. However, Formulation 3, a composition without any composite elastomeric particles, was unstable as an emulsion and could not be subjected to further experimentation because the conditioning agent was not sufficient to stabilize the emulsion. Formulations 4-7 were allowed to solidify in stick form for further stability testing.

Pencils were placed in several environments (77, 40°F, alternating 40°F (12 h) and 110°F (12 h), 120°F and 120°F at 90% humidity) for four weeks. After four weeks, observed changes in the pencil were noted on each medium and scored from zero (0) to five (5) depending on the visible changes in the pencil (eg, syneresis). Zero means no observed change, and five means an observed critical change indicating compositional instability. In table. 5 summarizes the observed changes in each of the pencils after four weeks on each medium.

Table 5

Composition 4 Composition 5 Composition 6 Composition 7 % composite elastomeric particles 1.00 2.00 3.00 5.00 77°F 0 0 0 0 40°F 0 0 0 0 40°F/110°F 2 2 1 1 120°F 5 2 0 0 120°F (90% humidity) 5 5 3 1 Freeze/Thaw Cycles 0 0 0 0

As can be seen, increasing the amount of composite elastomeric particles in the compositions increases the stability of glycerin-in-oil type emulsions. The emulsions ranged from complete instability (formulation 3) to minimal syneresis observed even under severe conditions (formulations 6 and 7). For example, a glycerol-in-oil type emulsion with 5% elastomer powder was the most stable formulation at 120° F. (90% humidity) ambient temperature.

Similar stability measurements were performed for compositions with other α-hydroxy acids.

- 13 041056 lots drawn up in it. Glycerol-in-oil type emulsions were made with emulsifiers (polyglyceryl-3-diisostearate and lauryl methicone) and either 2% lactic acid by weight, 2.43% by weight glycolic acid, or 1.89% by weight trioxaundecanedioic acid. In an environment at 120°F (90% humidity), the lactic acid formulation had a stability score of 1 after four weeks, the glycolic acid formulation had a stability score of 3 with some stick discoloration, and the trioxaundecanedioic acid formulation was unable to retain the shape of a hard stick . As can be seen, the specific α-hydroxy acid used in a given emulsion affects the stability of the glycerol-in-oil emulsion. However, stable emulsions of the glycerol-in-oil type with various α-hydroxy acids other than lactic acid can be obtained by known methods, including the use of various emulsification systems, changing the viscosity of the internal phase, and so on. In addition, the inclusion of various amounts of composite elastomeric particles in these compositions can also improve the stability of the emulsions.

Specific Embodiments

Specific embodiments of the present invention are numbered below.

Specific Embodiment 1. A lip composition in the form of a glycerin-in-oil type emulsion containing one or more α-hydroxy acids.

Specific Embodiment 2 A composition according to Specific Embodiment 1, wherein said composition contains one α-hydroxy acid.

Particular Embodiment 3. The composition according to Particular Embodiment 1 or 2, wherein the glycerol-based phase of said emulsion has an apparent pH in the range of 0.5 pH units relative to the pK _a of said α-hydroxy acid.

Particular Embodiment 4. A composition according to any one of Particular Embodiments 1-3, wherein said composition is capable of being in the form of a hard stick for at least four weeks after curing at 120°F and 90% humidity.

Specific Embodiment 5 A composition according to any of Specific Embodiments 1-4, wherein said α-hydroxy acid is lactic acid.

Specific Embodiment 6. A composition according to any of Specific Embodiments 1 to 5 further comprising a composite elastomeric powder.

Specific Embodiment 7. The composition according to Specific Embodiment 6, wherein said elastomeric powder is a silicone elastomeric powder.

Particular Embodiment 8. The composition according to Particular Embodiment 6, wherein said elastomeric powder comprises a crosslinked copolymer of dimethicone and vinyl dimethicone.

Specific Embodiment 9. A composition according to any of Specific Embodiments 6-8, wherein said composite elastomeric powder is surface coated with inorganic particles and/or one or more alcohols (e.g., monohydric alcohols, polyhydric alcohols, glycols, etc.). ).

Particular Embodiment 10. The composition according to Particular Embodiment 6, wherein said composite elastomeric powder is a crosslinked copolymer of dimethicone and vinyl dimethicone (and) silica (and) butylene glycol.

Particular Embodiment 11. A lip composition according to any one of Particular Embodiments 6-10, wherein said composite elastomeric powder is present in an amount of 0.1-10% by weight of the composition.

Particular Embodiment 12. A lip composition according to any one of Particular Embodiments 6-10, wherein said composite elastomeric powder is present in an amount of 1% to 5% by weight of the composition.

Specific Embodiment 13. A lip composition according to any of Specific Embodiments 1-12, wherein said composition comprises:

(a) from 1 to 45% glycerol by weight of the composition;

(b) 40 to 95% oil by weight of the composition;

(c) 1 to 10% α-hydroxy acid by weight of the composition; and (d) 1 to 10% elastomeric powder by weight of the composition.

Specific Embodiment 14. A method of providing a therapeutic and/or cosmetic effect to lips in need thereof, comprising applying a lip composition according to any of Specific Embodiments 1-13.

Particular Embodiment 15. The method according to Particular Embodiment 14, wherein said therapeutic and/or cosmetic effect is selected from reduced water loss from said lips, smoother lip surface (compared to untreated lips), increased hydration of said lips (compared to with untreated lips), increased barrier function of said lips (compared to untreated lips), thickened stratum corneum

Claims (15)

specified lips (compared to untreated lips) and their combinations. Particular Embodiment 16. The method according to Particular Embodiment 14 or 15, wherein said composition is applied one or more times per day. Since various changes can be made to the subject matter described above without departing from the scope and spirit of the present invention, it is intended that all matters contained in the foregoing description or defined in the appended claims should be interpreted as descriptive and illustrative of the present invention. In view of the above provisions, the present invention may have many modifications and variations. Accordingly, the present description is intended to cover all such changes, modifications, and omissions that fall within the scope of the appended claims. CLAIM 1. A lip composition in the form of a glycerol-in-oil type emulsion containing one or more α-hydroxy acids and a composite elastomeric powder. 2. The composition of claim 1, wherein said composition contains one α-hydroxy acid. 3. A composition according to any one of claims 1 or 2, wherein said composition is capable of being in the form of a hard stick for at least four weeks after curing at 49°C (120°F) and 90% humidity. 4. A composition according to any one of claims 1 to 3, wherein said α-hydroxy acid is lactic acid. 5. A composition according to claim 4, wherein the glycerol-based phase of said emulsion has an apparent pH of 3.3 to 4.3. 6. The composition of claim 1, wherein said elastomeric powder is a silicone elastomeric powder. 7. The composition of claim 1, wherein said elastomeric powder comprises a crosslinked copolymer of dimethicone and vinyl dimethicone. 8. A composition according to any one of claims 1 to 7, wherein said composite elastomeric powder is coated on the surface with inorganic particles and/or one or more alcohols, such as monohydric alcohols, polyhydric alcohols, glycols, etc. 9. The composition of claim 1, wherein said composite elastomeric powder contains a crosslinked copolymer of dimethicone and vinyl dimethicone and silica and butylene glycol. 10. A lip composition according to any one of claims 1-9, wherein said composite elastomeric powder is present in an amount of 0.1-10% by weight of the composition. 11. A lip composition according to any one of claims 1 to 9, wherein said composite elastomeric powder is present in an amount of 1 to 5% by weight of the composition. 12. A lip composition according to any one of claims 1 to 11, wherein said composition comprises: (a) from 1 to 45% glycerol by weight of the composition; (b) 40 to 95% oil by weight of the composition; (c) 1 to 10% α-hydroxy acid by weight of the composition; and (d) 1 to 10% elastomeric powder by weight of the composition. 13. A method of providing a cosmetic effect to lips in need thereof, comprising applying a lip composition according to any one of claims 1 to 12. 14. The method of claim 13, wherein said cosmetic effect is selected from reduced water loss from said lips, smoother lip surface compared to untreated lips, increased hydration of said lips compared to untreated lips, increased barrier function of said lips compared to untreated lips. lips, thickened stratum corneum of said lips compared to untreated lips, and combinations thereof. 15. The method according to claim 13 or 14, where the specified composition is applied one or more times a day. -