SK173699A3 - Cosmetic composition containing a whitening agent and an exfoliant - Google Patents

Abstract

The present invention is a stabilized cosmetic composition useful in the lightening or whitening of skin. The composition contains a stabilized active ingredient for whitening along with an alpha hydroxy acid. The present invention is also a method of improving skin tone, moisturization and skin firmness through the use of the stabilized cosmetic composition and a moisture source.

Description

Technical field

The present invention relates to cosmetic compositions comprising delivery systems that provide novel methods of delivering dermatologically active agents to cosmetically important areas of the stratum comeum. The compositions of the invention are particularly, but not only, useful as skin lightening agents. The present invention also includes a stabilized anhydrous delivery system for water-soluble acids. and finally, the present invention relates to a method for improving skin tone, moisturizing and skin firmness.

BACKGROUND OF THE INVENTION

Many skin lightening and whitening agents are used to reduce skin pigmentation and improve skin tone. Such agents include kojic acid and derivatives thereof.

There are many other chemicals that have a severe physiological effect on the skin. One group of these dermatologically active compounds are alpha-hydroxycarboxylic acids with (relatively) low molecular weight, for example having 10 or less carbon atoms. These acids, popularly called "alpha-hydroxy acids", are known to have a number of beneficial effects on the skin. Alpha-hydroxy acids, hereinafter referred to as AHA, can moisturize dry skin and ameliorate various diseases including acne, psoriasis and other skin anomalies. AHAs are also effective in revitalizing the skin. Depending on concentration and length of application

I can cause or stimulate peeling, which is the removal of the outer corrugated or cornered tissue layers, and stimulate the renewal of new skin layers, thereby achieving a significant improvement in skin appearance.

Some of the AHAs used to achieve these beneficial effects are the simplest alpha-hydroxy acids, particularly lactic acid, as well as glycolic acid, citric acid and malic acid. These acids are known as "fruit acids" because they occur in fruit and, in the case of glycolic acid, in sugar cane.

There are many other AHAs or the corresponding alpha-keto acids and similar acids that are known to be used or have been designed for use in revitalizing the skin or that otherwise provide useful dermatological functions to the skin. Some beta-hydroxy acids, such as salicylic acid, also have useful dermatological properties. Some such "skin acids" are disclosed in Yu et al., U.S. Pat. No. 5,091,171, the disclosure of which is incorporated herein by reference.

The AHAs of interest are usually fairly hydrophilic, readily soluble in water, and in the case of lactic acid, are liquid at temperatures near room temperature (about 16.8 ° C). Such hydrophilicity is usually incompatible with conventional hydrophobic cosmetic compositions. The anhydrous nature of these cosmetic compositions means that small amounts of active hydrophilic agents, such as AHA, may either lose their efficacy due to chemical or physical-chemical interactions or fail to deliver them to the skin surface in an appropriately hydrophilic or aqueous environment in which they would be effective. .

In addition, preferred environments for these agents are significantly acidic environments, a condition that is difficult to achieve on the surface of the skin that is treated with anhydrous or substantially hydrophobic cosmetic compositions. For products intended for daily use, it is of particular importance to avoid skin irritation.

It has been found that when a bleaching agent such as kojic acid is combined with a peeling agent such as an alpha-hydroxy acid, more specifically lactic acid, the bleaching results are improved.

SUMMARY OF THE INVENTION

Other features of the invention will be set forth in part in the description that follows, and in part will be obvious from the description, or can be learned from the practice of the invention. The characteristics of the invention can be understood and obtained by means of the tools and combinations thereof, as particularly pointed out in the appended claims.

In accordance with the object of the invention in one of its aspects, which is contained and described in detail herein, it is described herein:

topically applied cosmetic composition, characterized in that it comprises:

(a) a bleaching agent selected from the group consisting of kojic acid and its derivatives, ascorbic acid and its derivatives, including ascorbic acid magnesium salt, hydroquinone, liquorice extract, liquorice extract, mulberry extract, arbutin and mixtures thereof;

(b) a peeling agent selected from the group consisting of lactic acid, glycolic acid, malic acid, citric acid and salicylic acid;

(c) sufficient adsorbent or particulate absorbent carrier to transport the peeling agent; and

d) a cosmetic base, said base having a sufficient amount of a film-forming agent to produce the desired cosmetic film when the cosmetic composition is applied to the skin.

Here is described:

A stabilized bleaching composition comprising a bleaching agent selected from kojic acid and derivatives thereof, ascorbic acid and derivatives thereof, including ascorbic acid magnesium salt, hydroquinone, liquorice extract, liquorice extract, mulberry extract, arbutin and mixtures thereof, and gelling agents Reagent selected from castor oil derivatives, silicone polymers, silicone rubbers, bentonite clays and block copolymers of styrene, ethylene and propylene.

Yet it is described here:

a method of whitening the skin, characterized in that a source of water is applied to the surface of the skin, followed by applying to said skin a bleaching cosmetic composition comprising:

(a) a bleaching agent selected from the group consisting of kojic acid and its derivatives, ascorbic acid and its derivatives, including magnesium salt of ascorbic acid, hydroquinone, bearberry extract, liquorice extract, mulberry extract, arbutin and mixtures thereof;

(b) a peeling agent selected from the group consisting of lactic acid, glycolic acid, malic acid, citric acid and salicylic acid;

(c) sufficient adsorbent or absorbent particulate carrier to transport the peeling agent; and

d) a cosmetic base, said base having a sufficient amount of a film-forming agent to produce the desired cosmetic film when the cosmetic composition is applied to the skin.

Finally, it is described here:

a topically applied hydrophobic, substantially anhydrous cosmetic composition, comprising:

(a) a bleaching agent selected from the group consisting of kojic acid, ascorbic acid and mixtures thereof;

(b) a peeling agent which is lactic acid

(c) an anti-aging agent selected from vitamin a and retinol palmitate and its derivatives;

(d) a sufficient quantity of adsorbent or particulate absorbent carrier to transport the peeling agent; and

e) a cosmetic base, said base having a sufficient amount of a film-forming agent to produce the desired cosmetic film when the cosmetic composition is applied to the skin.

Other aspects of the invention will be set forth in part in the description that follows, and in part will be apparent from the description or can be learned from the practice of the invention. The objects and characteristics of the invention can be understood and attained by means of the tools and combinations thereof, particularly pointed out in the appended claims.

Detailed Description of the Preferred Embodiment

Various embodiments of the invention and one or more methods for practicing the invention will now be described in more detail. Illustrative, but not limiting, examples of preferred embodiments of the invention will also be described.

Preferred embodiments of the invention relate to novel cosmetic compositions comprising a stabilized bleaching agent, a peeling agent and an anti-aging agent to improve skin whitening.

Bleaching agents include, but are not limited to, kojic acid and derivatives thereof, ascorbic acid and derivatives thereof, including ascorbic acid magnesium salt, hydroquinone, bearberry extract, liquorice extract, mulberry extract, arbutin and mixtures thereof.

Other bleaching agents will be apparent to the formulator. Preferred bleaching agents for use in the present invention are kojic acid and derivatives thereof and ascorbic acid and derivatives thereof.

The bleaching agent of the present invention is preferably stabilized with an anhydrous gelling agent. Such anhydrous gelling agents of the present invention include, but are not limited to, castor oil derivatives such as trihydroxystearin, silicone polymers, silicone gums, bentonite clays, and styrene, ethylene, and propylene block copolymers. If the gelling agent contains metal ions, it should first be reacted with a suitable chelating agent to avoid reaction between the metal ions and the active ingredients. Suitable chelating agents are well known to those skilled in the art of cosmetic compositions.

The use of a gelling agent allows stabilization of the water-soluble acids when incorporated into the anhydrous delivery system of the present invention.

The bleaching agent of the present invention is preferably present in the cosmetic composition of the present invention in an amount of from about 0.10 to about 10% by weight, more preferably from about 0.50 to about 5.0% by weight, and most preferably from about 1.0 to about 10% by weight. 3.0% by weight. The bleaching agent may be mixed with the gelling agent before being combined with the cosmetic base, or the bleaching agent and the gelling agent may be incorporated in the cosmetic load sequentially.

A peeling agent is also used in the composition of the present invention. The peeling agent not only improves the whitening / lightening properties of the bleaching agent, but also improves the overall appearance and skin feel.

Any peeling agent such as an alpha-hydroxy acid, in particular lactic acid, as well as glycolic acid, citric acid and malic acid may be used in the cosmetic composition of the present invention. There are many others

AHA or the corresponding alpha-keto acids and similar substituted acids are known, including some beta-hydroxy acids, for example salicylic acid, and which can also be used in accordance with the present invention. A preferred peeling agent for use in the present invention is lactic acid.

An absorbent carrier may be used in the context of the present invention. In accordance with the invention, a variety of materials may be used as carriers for the transport of a dermatologically active ingredient or agent, for example a peeling agent such as an alpha-hydroxy acid, to the skin in the form of an active agent, the active ingredient being protected from other cosmetic ingredients that inactivate. Suitable carrier materials include, but are not limited to, polymeric organic microspheres and inorganic particles. Some commercially available microsphere powders useful in preparing the cosmetic materials of the present invention include organic polymeric materials such as polyethylene, polypropylene and copolymers thereof, polyurethane, polyesters, polyamides, polymethylmethacrylate, nylon, ethylene-acrylate copolymers, and polyvinylidene copolymers.

In principle, any nontoxic, non-irritating, cosmetically compatible organic polymeric materials that can be prepared in a satisfactory adsorbent or satisfactory absorbent form and which are compatible with the anhydrous diluent can be used for the purposes of the present invention.

Some examples of inorganic particles include talc, clays, organic modified clays, kaolin, mica, calcium salicylate, and various carbonates of various metals such as calcium and magnesium.

While the carrier can function effectively in larger sizes, the carrier particles should not be too large or their presence as components of the composition should not be obvious to the user. These particles should not give the cosmetic composition a rough or sandy appearance, but rather a smooth feel. Therefore, at least eighty percent of the particles should preferably not be greater than 50 microns (pm) and more preferably should not exceed 20 microns (pm). The particles should be neither too small nor absorbed in fat follicles, which is undesirable, although acceptable, and should not have too little storage volume for the passing dermatologically active agent.

Within the limits of providing a satisfactory cosmetic sensation after attrition, the carrier particles should be relatively large to be able to release the active ingredient from either the surface or even

through openings on the surface from internal particle volumes. Preferably, at least eighty percent of the carrier particles have a diameter greater than 10 microns (pm). A particularly preferred range for at least eighty percent of the particles is from 10 to 20 microns (pm), more preferably from 10 to 15 microns (pm). A useful average particle size is from 12 to 20 microns (pm).

Porous carrier particles are particularly preferred when the liquid phase absorbed in the particle occupies, for example, from 10 to 90 percent of the particle volume, rather than simply being retained on the surface of the particle.

The absorbent matrix powder that serves as a carrier for the local delivery of a dermatologically active agent or dermatologically active solution may comprise a porous synthetic organic polymer microsphere, for example, a cosmetically acceptable polyamide such as nylon 12 in an amount of about 0.1 to about 40.0 percent preferably from about 5.0 to about 20.0 percent, and more preferably from about 6.5 to about 10.0 percent by weight of the cosmetic composition. In addition to bearing AHA or other dermatologically active hydrophilic agents, the organic polymeric microspheres can also provide desirable sensory properties to the consumer, such as creaminess, dustiness and silkiness, and thus improve the light-scattering properties of the composition. When AHA or other dermatologically active agents are consumed, organic polymer microspheres are capable of absorbing skin fat, helping to regulate the penetration of fat.

Examples of suitable dermatologically active agents that can be delivered to the skin in the compositions of the invention include, but are not limited to:

anesthetics, for example benzyl alcohol, lidocaine and menthol, astringents, for example hrabolist, benzoic and aluminum or aluminum-zirconium salts, keratolytics, for example resorcinol, salicylic acid, ascorbic acid and acetic acid, peeling agents, for example lactic acid and other alpha or beta-hydroxy acids, vasoconstrictors such as phenylepinefin hydrogen chloride, external analgesics such as tripolonamine hydrogen chloride and camphor, anti-inflammatory agents such as salts of sweetweed, alpha-bisabolol, salicylate derivatives and ibuprofen, anti-inflammatory agents, trimethylglycine, glycine, ascorbic acid, ferulic acid and sodium lactate, bleaching agents such as magnesium ascorbyl phosphate, hydrogen peroxide, kojic acid and hydroquinone, lipolytic agents such as caffeine, aminophyll and other xanthine bases, pigmentation enhancers such as dihydroxyacetone, solar filters such as diethanolamine, (E) -3- (paramoxyphenyl) -2-propenoate, glyceryl aminobenzoate,

2-hydroxy-4-methoxybenzophenone-5-sulfonic acid and 2-phenylbenzimidazolesulfonic acid, wetting and wetting agents such as panthenol-lactam iodopropyltrimonium chloride; glycerin, polyglyceryl polymers, mono-, di-, tri- or polysaccharides or reduced mono-, di-, tri- or polysaccharides or derivatives thereof, propylene glycol, polypropylene glycol having molecular weights from about 100 to about 10,000 Daltons, hygroscopic amino acids, peptides and polypeptides or derivatives thereof, glycosaminoglycans, amides or esters of alpha or beta-hydroxy acids, ethoxylated glycerin derivatives, propylene glycol, butanol or pentanol, inositol and choline chloride, and nutrients such as vitamin C, vitamin B, folic acid and minerals such as calcium, magnesium, iron, zinc, manganese, selenium and phosphorus.

When wetting agents are added directly to the skin lightening composition, they are most preferably added in the carrier particles to prevent oxidation of the active acidic whitening agents. Equivalents to the foregoing examples and further guidance contained herein will suggest other dermatologically active agents suitable for incorporation into the composition of the invention. Lists of some of these agents are set forth in OTC monographs and the Physician's Desk Reference, which are incorporated herein by reference. Some of these agents and other agents are disclosed in Schaefer et al., U.S. Pat. U.S. Pat. No. 5,292,512, which is also incorporated herein by reference.

The most preferred dermatologically active agents for use in the present invention are peeling agents such as alpha-hydroxy acids, especially lactic acid.

One or more dermatologically active agents, including peeling agents, are present in the cosmetic composition of the present invention in an amount of from about 0.01 to about 20.0 percent by weight of the composition and can be incorporated into preferred embodiments of the present composition. More preferably, these agents can be added in an amount of from about 0.5 to about 8.0 percent, and even more preferably from about 1.0 to about 5.0 percent. Other active agents may be used in equivalent amounts depending on their potency.

While some dermatologically active agents have properties that allow them to be absorbed or adsorbed directly to or within the carrier matrix, for example a sufficiently low melting point, others are in crystalline form at room temperature and are preferably dissolved in a hydrophilic solvent system. suitable for the active ingredient. The solvent system should also preferably have little or no affinity for a substantially anhydrous base. This is important to maintain the solvent and the dermatolgically active agent dissolved therein in or on the carrier and to protect the intended function of the dermatologically active agent. In addition, the solvent should be suitably viscous to further help slow the migration of the dermatologically active agent from the carrier. As regards the impact on the functionality of the dermatologically active agent, the solvent should also be inert or inactive, or at least not be adversely affected.

Some groups of liquid hydrophilic solvents or dispersion phase media that may be used as adjuvants to assist the deposition of the dermatologically active agent or agents on or into the appropriate carrier, alone or in combination, are, inter alia, water, alcohols, and ethers.

A suitable group of alcohols contains mono-, di-, tri- or polyhydroxy alcohols of the general formula (OH)

R- (CH) - (C) - (CH _{2) z} -R.

(OH) (CH) wherein R = H, CH 3 or any saturated, unsaturated, cyclic or branched alkyl radical of 1 to 20 carbon atoms, X = 0 to 1 000 000, Y = 0 to 100, Z = 0 to 100 and R ¹ = H , CH ₃ , O-CH ₃ , O-CH ₂ CH ₃ .

Suitable examples of these compounds are glycerin, propylene glycol, dipropylene glycol, propanol, isopropanol, butanol, isobutanol, pentanol, isopentanol, neopentanol, diglycerol, polyglycerol, sorbitol, polyethylene glycerol and polyol.

Suitable ethers are unsubstituted and substituted ethers, for example UCON® liquid from Union Carbide Corp. or DOWANOL® liquids from the Dow Chemical Company or solvents CARBITOL® and CELLOSOLVE® from Union Carbide.

In principle, suitable viscous, hydrophilic solvents or solvent mixtures may be used with the dermatologically active agent in a ratio of from about 99: 1 to about 1:99. However, preferred ratios are chosen so as to utilize the physical or physicochemical properties of the solvent to deliver the dermatologically active agent in an active form in the liquid phase for capture by the absorbent carrier particles. Here, although smaller solvent fractions may be beneficial in some circumstances, larger solvent ratios are preferred. Examples of preferred ratios are ratios from about 1: 1 to about 1:20 parts by weight of reagent to solvent. While these ratios may be effective for intracellular agents, more effectively intracellular agents, e.g., hydrophilic or water-soluble hormones, such as corticosteroids, may be present in relatively smaller ratios, e.g., from about 1:99 to 1:20 parts of agent to solvent. A preferred solvent for a dermatologically active agent, such as alpha-hydroxy acid (AHA), is glycerin. The viscosity of the solvent helps to maintain AHA inside or on the carrier particles, while its hydrophilicity allows the skin moisture to withdraw dissolved AHA from the microparticle.

The composition preferably also contains an anti-aging agent such as vitamin palmitate and / or retinol derivatives, in particular retinoic acid. The anti-aging agent improves skin elasticity and minimizes wrinkles. The anti-aging agent is present in the cosmetic composition of the present invention in an amount of from about 0.20 to about 10.0 weight percent, more preferably from about 1.0 to about 6.0 weight percent, and most preferably from about 1.5 to about 2 weight percent. 5 percent by weight.

The cosmetic base may be aqueous or anhydrous. Suitable cosmetic base materials are well known to the skilled artisan. Although an aqueous base may be used, the preferred base is an anhydrous hydrophobic base. If an aqueous base is used, the skilled artisan should minimize (to the maximum extent possible) the contact between the water base and the active agents that may be degraded by oxidation.

A preferred substantially or almost totally anhydrous base may provide an environment or diluent for dispersing the active agent, wherein the environment may be liquid or semi-solid, for example, a dispersing agent or solvent for other cosmetic ingredients imparting desired cosmetic properties to the composition. Thus, the anhydrous base may comprise a more or less volatile hydrophobic cosmetic solvent in which the gelling agent is optionally dispersed to achieve the desired consistency.

The bleaching cosmetic composition of the present invention is best used in conjunction with a water source, most often a moisturizer. The humectant is preferably applied to the skin surface before the bleaching cosmetic composition is applied. However, this is not necessary.

The bleaching cosmetic composition of the present invention may contain, in addition to the active ingredients, a variety of products or adjuvants. The addition of these materials is readily understood by the skilled artisan, and although the various ingredients are described below, this description does not claim to be exhaustive.

Advantageously, the invention provides a film-forming agent which aids adhesion of the carrier particles to the skin and thus helps to form an occlusive barrier to increase water access to or near the skin surface. By film-forming it is meant that a substantially continuous layer of product is formed on the skin surface. By occlusive, it is meant that the barrier placed on the skin surface substantially blocks or slows the loss of volatile substances from the skin surface and allows them to penetrate the upper layers of the skin. For the purposes of the present invention, the barrier film is preferably hydrophobic.

Some groups of suitable film-forming cosmetic agents that can be used alone or in combination are, among others, metal element soaps, waxes and film-forming emollients. Some examples of each of these classes of film-forming cosmetic agents will now be described, but are not exhaustive. Others are known to those skilled in the art.

Metal element soaps are useful substances that aid adhesion and promote the formation of a hydrophobic film. The gelling agent based on the metal element soap may be alkaline earth metal salts or aluminum salts of saturated carboxylic acids of six to twenty carbon atoms, for example calcium, magnesium, zinc, aluminum or lithium salts of lauric, oleic or stearic acid, or mixtures thereof . The metal element cosmetic soap, for example zinc laurate, may be used in an amount of from about 1.0 to about 5.0 percent, preferably about 3.0 percent by weight of the composition.

The metal element soap functions as an ionic gelling agent that aids adhesion and formation of a hydrophobic film.

Other agents useful in film formation are waxes. Many waxes are well known in the cosmetic art and can function as suitable film-forming agents in the compositions of the present invention. These compounds typically have the general formula RX in which R is a long saturated, unsaturated, cyclic or branched alkyl radical of 8 to 10,000,000 carbon atoms and X is -H, -OR ¹ or -C-OR ¹¹ , wherein R ¹ is H or a saturated, unsaturated, cyclic or branched alkyl radical of 1 to 24 carbon atoms and R ¹¹ is H or a moiety of a mono-, di-, tri- or polyhydroxy compound capable of forming a mono-, di-, tri- or polyester.

Preferred waxes have melting points that are above 38 ° C (100 ° F). Substances such as glyceryl wax esters, beeswax, ceresin wax, kamauba wax, candelilla wax and other cosmetically acceptable waxes may be used.

A total wax content of from 0 to 10.0 percent is adequate for the preparation of satisfactory cosmetic compositions of the present invention. Preferably the total wax content does not exceed 5.0 percent and more preferably does not exceed 3.0 percent. Suitable waxes are, for example, glycyl-tribehenate, ceresin wax and microcrystalline wax, which are used in amounts of from about 0.00 to about 5.00 percent, preferably from about 0.1 to

1.5 percent. More preferably, from about 0.25 to 0.5 percent wax, such as glyceryl tribehenate, and a slightly higher amount from about 1 to 2 percent ceresin wax are used.

The low wax content achieved in the cosmetic compositions of the present invention has the advantage of achieving low tensile strength and increasing removability. Useful wax functions are adhesion, creamy product impression, film formation and viscosity enhancement.

Other useful film-forming agents are plasticizers. These substances are usually liquid at temperatures between 0 ° C (32 ° F) and 38 ° C (100 ° F). Emollients useful in the present invention include emollients of the following formula C _n H (2iw-2-x)> wherein n is an integer from 0 to more than one million and x is 0 or even an integer not greater than n, and may contain saturated, unsaturated, branched and cyclic hydrocarbon chains. Examples are mineral oil, petrolatum, PERMETHYL® liquids and polybutylenes.

Other useful film-forming plasticizers are mono-, di-, tri- or polybranched, cyclic, saturated or unsaturated alkyl esters or alkyl ethers or di-, tri-, or polyhydroxy compounds, for example ethylene glycol, propylene glycol, glycerin, sorbitol or polyol. Examples of such emollients include, but are not limited to, vegetable oils such as soybean oil, Atalea palm oil, castor oil, cottonseed oil, Chinese tallow oil, Crambe L. oil, perilla oil, rape oil, rice bran oil , palm oil, palm oil, olive oil, linseed oil, coconut oil, sunflower oil, safflower oil, peanut oil and corn oil. Preferred saturated and unsaturated vegetable oils are those whose fatty acids have 6 to 24 carbon atoms.

Other suitable film-forming emollients include esters of the general formula

C-OR ₂ or R 1! O ¹ : (Ch ₂ ) "c D ABOUT

wherein R 1 and R ₂ are saturated, unsaturated, branched or cyclic alkyl radicals having 2 to 24 carbon atoms and n is an integer from 0 to about 20.

The novel cosmetic compositions of the present invention may also contain a silicone material that imparts some degree of film-forming ability. Suitable silicone materials are preferably water insoluble and include cyclomethicone polyalkyl siloxanes, polyaxyl siloxanes, polyalkylalkyl siloxanes, polysiloxane gums, amine functional polysiloxanes and polyether siloxane copolymers. Descriptions relating to other suitable silicone materials can be found in U.S. Pat. U.S. Pat. No. 4,788,006, U.S. Pat. U.S. Pat. No. 4,341,799, U.S. Pat. U.S. Pat. No. 4 152416, U.S. Pat. U.S. Pat. No. 3,964,500, U.S. Pat. U.S. Pat. No. 3,208,911, U.S. Pat. U.S. Pat. No. 4,364,837 and U.S. Pat. U.S. Pat. No. 4,465,619, all of which are incorporated herein by reference.

in

Another group of suitable film-forming agents comprises substances produced by polymerizing alkylene oxide monomers of the general formula / ° K

H (CH ₂ ) _n -HC-CH ₂ in which n is an integer from 0 to about 3.

These materials can be either a homopolymer or a copolymer of two or more monomers. Examples of homopolymers are polypropylene oxide and polybutylene oxide. The molecular weights of these materials are generally between 100 and 10,000 Daltons. These materials can be further condensed with mono- or polyhydroxyalkylalcohol such as UCON® liquids from Union Carbide Corp.

The film-forming agents may be used alone or in combination with other film-forming agents to achieve the desired aesthetic properties of the finished composition. A preferred range of amount of film-forming agents is from 1 to 99%, more preferably from about 1 to 50% by weight of the composition.

Suitable non-curing film-forming agents, for example dimethicone, may be used in amounts of from about 0.5 to about 5.0 percent, preferably from about 0.6 to about 5.0 percent.

1.5 percent, more preferably about 1.0 percent. Preferred functions are film formation, skin protection or water barrier, lubricant and silk softener function.

Film enhancing agents, such as mica treated with an aluminum salt of myristic acid, may be used in an amount of from about 4.0 to about 20.0 percent by weight of the composition, preferably about 5.0 to 8.0 percent, more preferably 6.5 percent. Advantageous functions of film enhancers include skin adhesion, imparting a creamy and silky appearance to the composition, and enhancing the formation of a hydrophobic film.

Although strong adhesive properties can be introduced into anhydrous cosmetic formulations by incorporating film-forming waxing agents, too high a wax content will cause contraction and an undesirable sticky feeling when the cosmetic composition is applied, and this may make the cosmetic composition difficult to remove.

To solve this problem, the present invention also provides a novel film-forming system comprising relatively high proportions of a particulate inorganic gelling agent, for example a gelling agent based on bentonite clays, and a metal element soap gelling agent, such as zinc laurate, using only a small proportion of wax, if any.

When this film system is used in cosmetic compositions containing microspheres, a good anhydrous film can be obtained with excellent extensibility and no stickiness or contraction. These desirable properties appear to derive from a unique combination of the metal element soap properties - adherence to the skin - and the properties of the microspheres - ball-transfer lubrication.

In one practical embodiment of the invention, loading the carrier with some AHA, e.g. is achieved by dissolving AHA in glycerine and absorbing the AHA dissolved in glycerine into porous microspheres or fine polymer particles. This system is intended for use in a hydrophobic environment where AHAs remain stored in porous microspheres. When applied to the skin, the cosmetic composition is coated on or rubbed into the skin and the microspheres spread along the skin surface to come into contact with moisture that releases the hydrophilic AHA-glycerin system from microporous polymer particles.

Once the microspheres have been emptied, the hollow microspheres are now capable of absorbing fats, thereby adjusting the tendency of fat penetration.

The AHAs are preferably filled into carrier particles, for example porous nylon particles in a liquid medium, which should be sufficiently viscous to keep them in the pores of the particles during manufacture of the composition. Lactic acid melts at 16.8 ° C and can be absorbed into porous carrier particles at temperatures above this melting point without the need for any adjuvant by mixing appropriate ratios of microspheres and lactic acid, for example around a 1: 1 weight ratio until lactic acid is absorbed. . Similarly, the carrier particles may be filled with other acids, for example a mixture of fruit acids, by stirring, i. by mixing fine powders with a sufficiently small particle size to fit into the pores of the carrier.

The beneficial effects of lightening or whitening of the skin resulting from the bleaching cosmetic composition can only be apparent after long-term regular, e.g. daily, use of the cosmetic composition of the present invention over a period of weeks, e.g., four or six or more weeks.

A preferred hydrophobic diluent for the microsphere particles loaded with the active agent is a silicone gel, which is preferably prepared using a volatile silicone solvent such as dimethicone. A preferred gelling agent is trihydroxystearin.

The volatile solvent, for example cyclomethicone, preferably in the form of a pentamer, may be used as a hydrophobic diluent, for example, for a "cream to powder" composition. Suitable amounts are from about 20.0 to about 70.0 percent by weight of the composition, preferably about 30 to 40 percent, and more preferably about 33.0 percent. Volatile solvents act as wetting agents and evaporate rapidly after application. Some alternative or other volatile silicone solvents are described below.

A gelling agent suitable for a volatile solvent, for example quatium-18 bentonite, is present in an amount of from about 1.0 to about 15.0 percent, more preferably from about 3 to 10 percent, and more preferably from about 5.0 to 6.0 percent. The gelling agent physically stabilizes the composition and functions as a diluent for the dye suspension, if dyes are present, and can also absorb fat and reduce shine.

In some compositions, a wetting agent may be used. When a wetting agent such as sorbitan isostearate is used, it is present in an amount of from about 1.0 to about 10.0 percent by weight of the composition, preferably about 3.5 to 4.5 percent, and more preferably about 4.0 percent can be used. Preferred wetting agents allow the capacity of the solid material to be increased and cause the formation of a hydrophobic film.

Synthetic polymeric microspheres may be used in the cosmetic compositions in question, in addition to an AHA powder carrier such as polymethyl methacrylate, in an amount of from about 8.0 to about 20.0 percent by weight of the composition, preferably about 10.0 to 15.0 percent, and more preferably 12, 0 percent. These other polymeric microspheres act as enhancers of sensation, providing a "bead transfer" feel and a silky, dry feel upon application and evaporation of the solvent upon application. Other features are light scattering and giving the product a powder feel.

Any oily, low volatility, solvent ester such as isononyl isononanoate is useful for controlling the volatility and molecular weight of the solvent system in an amount of from about 1.0 to about 10.0 percent by weight, preferably from about 4.0 to 6.0 percent and more preferably about 5.0 percent solvent. Preferred solvents also function as lipophilic plasticizers, aid in the solubilization of the ingredients, and are miscible with the volatile solvent of the carrier (e.g., dimethicone).

One or more fat-soluble moisturizing agents, for example lauryl-PCA, may be used in an amount of about 0.4 to about 0.4 to improve wetting.

2.5 percent, preferably about 0.5 percent, or cetyl dimethicone in an amount of from about 1.0 to about 5.0 percent by weight of the composition. Cetyl-dimethicone provides a light, dry feel and aids in film formation.

A humectant may be incorporated into the cosmetic composition of the present invention, but if incorporated, it is preferably filled into porous microspheres and dispersed in the composition. As an alternative to incorporating the moisturizing agent, or together with incorporating the moisturizing agent, the moisturizing agent may be applied to the skin prior to application of the bleaching cosmetic composition of the present invention.

The bleaching cosmetic composition of the present invention works best in the presence of a water source. The water source aims to hydrate the skin. Suitable hydration sources are liquid water added specifically to hydrate the skin or accidentally, such as directly after bath or after shower. Hydration can also be achieved by applying a humectant or other agent in the aqueous phase.

Kaolin or other fat absorbents may be used in an amount of from about 0.50 to about 3.0 percent by weight of the composition, preferably about 0.7 to 1.5 percent, and more preferably 1.0 percent. The function of the preferred fat absorbers is the absorption of excess skin fats, skin adhesion, light diffusion and turbidity.

A opacifying agent, such as titanium dioxide, may be used in an amount of from about 0.10 to about 5.0 percent by weight of the composition, preferably about 0.3 to 1.0 percent, and more preferably 0.50 percent, to cover the skin and her masks were disguised.

The volatile polar activator solvent for the gelling agent, for example hexylene glycol, may be used in an amount of from about 0.75 to about 3.0 percent by weight of the composition, preferably less than about 2.0 percent, more preferably no more than about 1.0 percent. This will act as a binder softening agent, a solvent, and a softening agent that provides resistance to moisture and oxidation.

Preservatives, such as methylparaben or propylparaben, may be used in amounts of, for example, 0.2 to 0.3 weight percent, as known to those skilled in the art.

Other ingredients, including dyes and fragrances, may also be used, as is known to the skilled artisan. Some other optional ingredients are: Vitamin E linoleate, at about 0.10 percent as an additional humectant, Vitamin E acetate at about 0.10 percent to act as a free radical scavenger and as an antioxidant, retinyl palmitate, at about 0.10 percent 0.1 percent, which functions as a retinoic acid derivative to reduce fine lines, ceramides at less than 0.3 percent, which act as skin firming agents, and sphingolipids at less than about 0.3 percent, which act as skin firming agents. Sphingolipids also function to improve the skin barrier, thereby increasing moisturizing and reducing the penetration of irritants.

A group of cyclomethicone compounds which is preferred for use in the cosmetic compositions of the present invention is illustrated by compounds of the general formula - [R 1 R ₂ SiO] _n - wherein both R ₁ and R ₂ are both shorter alkyls of one to four carbon atoms, with or without a substituent selected from the group consisting of halogen atoms, hydroxyl, carboxyl or methoxy, and n is from 3 to 6, wherein the compounds are cyclized. The volatile cyclomethicone solvent used may be one of the foregoing compounds or a mixture thereof. The compound or compounds may be a homopolymer in which all n monomer units are the same or a heteropolymer in which the units are different. Some preferred cyclomethicones are dimethicones, especially homopolymers, in which n is the number 4 or 5 and R 1 is the same. R ₂ is both methyl, such as octamethylcyclotetrasiloxane and decamethylcyclopentasiloxane.

Depending on the nature of the composition of the finished product, for example a washing solution, powder, cream, bar, other optional ingredients may be used, as known to those skilled in the art, in amounts known to those skilled in the art. Such ingredients include, but are not limited to, fragrances, dyes, colorants, preservatives, wetting agents, fat absorbents, opacifying agents, and antioxidants.

The following examples are provided to illustrate the invention. Since these examples are provided for illustrative purposes only, the present invention should not be limited by these examples.

DETAILED DESCRIPTION OF THE INVENTION

Example 1

A dry mixture of ascorbic acid was prepared by mixing the following substances in the following weight ratios.

weight. % ascorbic acid 3.00 zinc laurate 3.00 kaolin 1.00 silicon dioxide 0.20 sulphate 3.80 Example 2 11.00%

Using a dry ascorbic acid mixture of Example 1, a cosmetic composition was prepared by mixing the ingredients below in the indicated amounts. This composition was applied to the skin and caused increased skin tone and lightening.

dimethicone 350 Vise. weight. % 1.00 sorbitan isostearate 1.00 isononyl izononaoát 5.00 lauryl PCA 0.50 cetyl dimethicone 2.13 Glyceryl tribehenate 0.32 Ceresin wax 1.43 microcrystalline 0.32 propyl 0.10 methylparaben 0.30 cyclomethicone 33.50 nylon-12 / lactic acid (30%) 3.33 dry mixture of ascorbic acid 11,00 Nylon-12 6.67 PMMA beads 12,00 Thixogel RCM (trihydroxystearine) 16,00 tocopherol linoleate 0.50 tocopherol acetate 0.50 retinyl palmitate 0.10 ParsolMCX 0.50 lavender 0.30 hydrophobic sfmgolipids 0.50 Example 3 100%

A dry mixture of kojic acid was prepared by mixing the following substances in the following weight ratios.

zinc laurate weight. % 1.00 Cabosil 0.41 barium sulphate 2.07 EDTA disodium salt 0.10 FD&C June 40 0.01 FD & Cžltáč. 5 0.02 titanium dioxide 1.00 methylparaben 0.30 prodylparabén 0.10 sodium lactate, 100% 1.05 kojic acid 1.00 Example 4 7.06%

Using a dry kojic acid mixture of Example 3, a cosmetic composition was prepared by mixing the ingredients below in the indicated amounts. This composition was applied to the skin of the hand and caused increased skin tone and lightening.

dimethicone weight. % 5,00 cetyl dimethicone 10.00 Glyceryl tribehenate 0.38 paraffin wax 1.72 microcrystalline wax 0.38 cyclomethicone 17.37 dry mixture of kojic acid 7.05 Lactic acid / glycerin / nylon 10.00 Nylon-12 4.00 PMMA beads 11,00 trihydroxystearin (5.45%) / cyclomethicone 31,00 tocopherol 0.20 tocopherol acetate 0.50 retinyl palmitate ₍ 0.10 ethylhexyl (£) -3- (p-methoxyphenyl) -2-propenoate 0.50 lavender 0.30 hydrophobic sfmgolipids 0.50 100%

Example 5

The bleaching effect of the compositions of the present invention was tested using three sets of 20 women each. Women were 35-60 years old and had to fall into grades I to III of Fitzpatrick's skin classification. Women in grades I or IV of the modified Glogau classification were excluded.

Fitzpatrick skin classification:

I always burn easily, never brown

Π always burns easily, minimally brown

III slightly burned, brown gradually

At least IV burns, brown always good

They rarely get burned, very brown

VI never burns, richly pigmented.

Modified Glogau classification:

Even gentle: no keratoses or scarring, small wrinkles

II moderate: frequent actin keratoses - soft yellow skin, discoloration, frequent wrinkles parallel line of laughter

III advanced: actin keratoses - bright yellow skin, discolouration with teleangiectasis and wrinkles - present at rest, moderate acne scarring

IV strong: actin keratoses, skin cancer, wrinkles - deeply flabby skin of actin, gravitational and dynamic origin, strong acne scarring.

The test lasted 13 weeks. During this period, each of the three sets used one of the following:

I

I Visible Action Skin Revealing Lotion®

II the anhydrous cosmetic composition of the present invention together with the Visible Action Skin Revealing Lotion®

III Anhydrous cosmetic composition according to the present invention together with a washing solution that moisturizes the skin

Visible Action Skin Revealing Lotion®

Visible Action Skin Revealing Lotion is a moisturizing agent made as a combination of the following ingredients in the indicated amounts expressed as a percentage by weight:

2.0% acetylated lanolin 4.0% stearyl alcohol and ceteareth 20

2.5% stearyl alcohol 5.0% butyl ether PPG-14 1.0% cetyl acetate, acetylate 0.25% dimethicone

70.5% water

3.0% methyl-Gluceth-10

0.25% xanthan gum

3.0% water

3.0% 88% lactic acid

3.0% sodium lactate 0.20% iodopropylbutylcarbamate 0.20% nyaantoin DMDM 0.08% Japanese green tea actiphylte 0.20% wheat-barley-soya-millet 0.50% retinyl palmitate 0.25% 0.06% bisabolol

Anhydrous cosmetic composition according to the present invention

The anhydrous cosmetic composition of the present invention is a skin whitening or lightening composition. This anhydrous composition contains the following components in weight percent:

5.0% dimethicone

10.0% cetyl dimethicone 0.38% glyceryl tribehenate 1.72% paraffin wax 0.38% microcrystalline wax · 10.4% cyclomethicone

6.97% cyclomethicone

I, 05% sodium lactate

6.0% dry mixture of kojic acid

10.0% lactic acid mixture

4.0% nylon-12

II, 0% PMMA beads 31.0% thixogel RCM

0.2% tocopherol

0.5% tocopherol acetate

0.1% retinyl palmitate

0.5% ethylhexyl β-methoxynamate

0.3% lavender

0.5% hydrophobic sphingolipids

The compositions of the present invention have resulted in a 20-35% improvement in skin tone regularity, a 30-35% increase in skin elasticity, a 50-60% improvement in skin firmness, a 30-80% reduction in wrinkle appearance, a 30-40% improvement in skin clarity, 30- 40% reduction in fine lines, 40 to 50% reduction in skin roughness and 20 to 30% improvement in overall skin condition.

While the illustrative embodiments of the invention that have been described above have been described, it is to be understood that various modifications will be apparent to those skilled in the art.

Claims (17)

PATENT CLAIMS A topically applied cosmetic composition comprising: (a) a bleaching agent selected from the group consisting of kojic acid and its derivatives, ascorbic acid and its derivatives, including ascorbic acid magnesium salt, hydroquinone, liquorice extract, liquorice extract, mulberry extract, arbutin and mixtures thereof; (b) a peeling agent selected from the group consisting of lactic acid, glycolic acid, malic acid, citric acid and salicylic acid; (c) a sufficient amount of adsorbent or absorbent particulate carrier to carry said peeling agent; and d) a cosmetic base, said base having a sufficient amount of a film forming agent to produce the desired cosmetic film when said cosmetic composition is applied to the skin. The cosmetic composition of claim 1, wherein said cosmetic base is a hydrophobic, substantially anhydrous cosmetic base. The cosmetic composition of claim 1, further comprising an anti-aging agent selected from the group consisting of vitamin 4 palmitate and retinol and derivatives thereof. The cosmetic composition of claim 2, wherein said composition further comprises an anhydrous gelling agent. The cosmetic composition of claim 4, wherein said anhydrous gelling agent is selected from castor oil derivatives, silicone polymers, silicone rubbers, bentonite clays, and styrene / ethylene / popylene block copolymers. The cosmetic composition of claim 5, wherein said anhydrous gelling agent is trihydroxystearin. Cosmetic composition according to claim 2, characterized in that said hydrophobic phase of the cosmetic base comprises one or more solvents selected from glycerin polar solvent, silicone solvent and mixtures thereof. 8. A stabilized bleaching composition comprising: (a) a bleaching agent selected from kojic acid and derivatives thereof, ascorbic acid and derivatives thereof, including ascorbic acid magnesium salt, hydroquinone, liquorice extract, liquorice extract, mulberry extract, arbutin and mixtures thereof; and b) a gelling agent selected from castor oil derivatives, silicone polymers, silicone gums, bentonite clays, and styrene / ethylene-propylene block copolymers. The bleaching composition of claim 8, wherein the bleaching agent is selected from kojic acid, ascorbic acid, and mixtures thereof, and wherein the gelling agent is selected from trihydroxystearin. 10. A method of lightening the skin comprising applying a water source to the skin surface followed by applying to said skin a bleaching cosmetic composition comprising: (a) a bleaching agent selected from the group consisting of kojic acid and its derivatives, ascorbic acid and its derivatives, including ascorbic acid magnesium salt, hydroquinone, liquorice extract, liquorice extract, mulberry extract, arbutin and mixtures thereof; (b) a peeling agent selected from the group consisting of lactic acid, glycolic acid, malic acid, citric acid and salicylic acid; (c) a sufficient amount of adsorbent or absorbent particulate carrier to carry said peeling agent; and d) a cosmetic base, said base having a sufficient amount of film-forming agent to form the desired cosmetic film, when the said ^one cosmetic composition applied to the skin. The method of claim 10, wherein said cosmetic base is a hydrophobic, substantially anhydrous cosmetic base. The method of claim 10, wherein said bleaching cosmetic composition further comprises an anti-aging agent selected from the group consisting of vitamin 4 palmitate and retinol and derivatives thereof. The method of claim 11, wherein said bleaching composition further comprises an anhydrous gelling agent. The method of claim 13, wherein said anhydrous gelling agent is selected from castor oil derivatives, silicone polymers, silicone gums, bentonite clays, and styrene / ethylene / propylene block copolymers. 15. The cosmetic composition of claim 14, wherein said anhydrous gelling agent is trihydroxystearin. The method of claim 11, wherein said hydrophobic phase of the cosmetic base comprises one or more solvents selected from glycerin polar solvent, silicone solvent, and mixtures thereof. 17. A topically applied hydrophobic, substantially anhydrous cosmetic composition, comprising: (a) a bleaching agent selected from the group consisting of kojic acid, ascorbic acid and mixtures thereof; (b) a peeling agent which is lactic acid; (c) an anti-aging agent selected from the group consisting of vitamin 4 palmitate and retinol and derivatives thereof; (d) sufficient adsorbent or absorbent particulate carrier to transfer the peeling agent; and e) a substantially anhydrous, hydrophobic cosmetic base, said base having a sufficient amount of a film-forming agent to produce the desired cosmetic film when said cosmetic composition is applied to the skin. / * OoiiuUilA