CN1121850C - Use of unfermented honey as decolouring agent - Google Patents

Abstract

The invention relates to use of unfermented honey used in a cosmetic composition an agent for depigmenting and/or lightening the skin, body hair or head hair and/or for treating liver spots. The invention also relates to a beauty treating method for for depigmenting and/or lightening the skin, body hair or head hair, comprising using the composition including the unfermented honey on the skin, body hair or head hair.

Description

Use of unfermented honey as a depigmenting agent

The present invention relates to the use of unfermented honey in cosmetic compositions as a depigmenting and/or whitening agent for skin or hair and/or for the treatment of skin pigmentation, or as a depigmenting and/or brightening agent for skin or hair. Use in preparation of whitening agent and/or dermatological composition for treating skin pigmentation. The invention also relates to a cosmetic method of depigmentation and/or lightening of the skin or hair, which method comprises the application on the skin or hair of a composition comprising unfermented honey.

The color of human skin is related to various factors, especially season, race and gender, mainly determined by the nature and concentration of melanin produced by melanocytes. Additionally, at various times in human life, some individuals develop darker and/or darker pigmented spots on the skin, especially on the hands, which give the skin an uneven appearance. These spots are also due to high concentrations of melanin in the keratinocytes that line the surface of the skin.

Similarly, the color of the hair on the scalp or other parts of the body is also produced by melanin; when the hair color is heavy, some people want it to be lighter. This is especially meaningful for body hair, where lighter colors are less noticeable than heavier ones.

The mechanism of skin and hair pigment formation, i.e. the formation of melanin, is particularly complex and roughly includes the following main steps:

Tyrosine→dopa→dopabenzoquinone→dopa chromium→melanin

Tyrosinase (monophenolic dihydroxyphenylalanine: oxygen oxidoreductase EC 1.14.18.1) is an essential enzyme in this reaction sequence. In particular, it catalyzes the conversion of tyrosine to dopa (dihydroxyphenylalanine) by virtue of its hydroxylase activity and the conversion of dopa to dopabenzoquinone by virtue of its oxidase activity. This tyrosinase is only active under certain biological factors when it is in its mature state.

A substance if it directly affects the viability of melanin-producing epidermal melanocytes, and/or if it intervenes in melanin biogenesis by inhibiting an enzyme in melanogenesis or itself as a structural analogue of a compound in the melanin synthesis chain A step in the synthesis, blocking this reaction chain to produce decolorization, then it is considered a decolorization agent.

More particularly, hydroquinone and its derivatives, especially its ethers, such as hydroquinone monomethyl ether and monoethyl ether, are substances most commonly used as depigmenting agents. While these compounds have some efficacy, unfortunately they are not free from side effects due to toxicity and are therefore difficult or even dangerous to use. The reason for the toxicity is that it interferes with the main mechanism of melanogenesis by killing cells, which may disturb their biological environment and subsequently force the skin to clear them, thus producing toxicity.

Thus, hydroquinone is a highly irritating and cytotoxic compound to melanocytes, and many have investigated its full or partial alternatives.

There has therefore been a search for substances that do not interfere with the melanogenesis mechanism but act upstream of tyrosinase by preventing tyrosinase activation so that the toxicity is greatly reduced.

For the treatment of localized hyperpigmentation due to hyperactivity of melanocytes, such as spontaneous melanomas ("gravid spots" or melasma) arising during pregnancy or estrone/progestin contraception, due to benign melanocyte hyperplasia and localized hyperpigmentation due to hyperactivity, such as age spots called actinic pigmentation, accidental hyperpigmentation or depigmentation that may result from photosensitization or scarring after injury, and certain vitiligo conditions such as vitiligo, In particular, look for highly effective, non-toxic topical depigmenting substances. In the latter cases (scarring that may give the skin a pale appearance, and leukoplakia), it is not possible to repigment the damaged skin, so the remaining areas of normal skin are depigmented so that the entire skin appears Uniform white.

Therefore, there is a need for a new whitening agent for human skin and hair whose activity is as effective as existing agents without the disadvantages of existing agents, i.e., non-irritating to the skin, non-toxic and/or or non-allergenic and stable in composition.

The present applicants have unexpectedly found that unfermented honey has depigmentation activity even at low concentrations without exhibiting cytotoxicity.

Honey is commonly used for its moisturizing and antiseptic properties, or to treat wounds, sores, or burns. Honey is also known from FR-A-2 751 537 as a keratolytic, especially for increasing the radiance of the complexion and for treating wrinkles. However, it has never been suggested that honey may have depigmenting activity through a direct effect on melanogenesis.

The present invention thus provides the use of unfermented honey in a cosmetic composition as a depigmenting and/or whitening agent for the skin or hair and/or for the treatment of skin pigmentation.

The present invention also provides the use of unfermented honey in the preparation of a dermatological composition for depigmentation and/or whitening of skin or hair and/or treatment of skin pigmentation.

For the purposes of the present invention, unfermented honey is a honey that does not contain hydroxy acids, as distinct from honey extracts that are fermented products and that contain hydroxy acids.

The honey used in the present invention consists of a mixture of glucose, fructose, dextrin, sucrose, protein and water. The amounts of these various components vary according to the source of the honey. Typically, honey will contain a mixture of 72-75% glucose and fructose, 15% water, 10% dextrin, 2.5% sucrose and 1% protein.

Honey from various sources can be used. In particular it may be acacia honey, grapefruit honey, alpine honey, heather honey, or honey obtained from orange blossom or any other flower. However, in the present invention it is preferred to use acacia honey.

For example, the amount of honey used in the present invention is 0.1-10%, preferably 2-5%, of the total weight of the composition.

The invention also relates to a method of depigmentation and/or whitening of the skin or hair, and/or treatment of skin pigmentation, which comprises applying to the skin or hair a composition comprising unfermented honey.

Cosmetic or dermatological compositions containing honey are suitable for topical use and thus contain a cosmetically or dermatologically acceptable medium, ie a medium compatible with the skin or hair. It can be in various pharmaceutical forms commonly used for topical application, in particular aqueous or aqueous-alcoholic solutions, oil-in-water or water-in-oil or multiphase emulsions, aqueous gels, liquid, pasty or solid anhydrous products, by means of Oil dispersed in an aqueous phase in spherical structures, which may be polymeric nanoparticles such as nanospheres and nanocapsules, or more preferably ionic and/or non-ionic lipid vesicles.

The compositions can be more or less runny and have a white or colored cream, grease, milk, lotion, serum, paste or mousse-like appearance. It can be used in aerosol form on the skin or hair. Solid forms such as sticks are also possible. It can also be used as a grooming and/or makeup supply. It can also be in shampoo or conditioner, powder or pencil form.

In general, the composition of the present invention may also contain auxiliaries customary in the field of cosmetics and dermatology, such as hydrophilic or lipophilic gelling agents, hydrophilic or lipophilic active ingredients, preservatives, antioxidants, solvents, fragrances, Fillers, filters, pigments, odor absorbers and colorants. The amount of various additives is the usual amount in this field, for example, it can be 0.01-20% of the total weight of the composition. Depending on their nature, these auxiliaries can be incorporated into the fatty phase, the aqueous phase, lipid vesicles and/or nanoparticles.

Those of skill in the art should carefully select these optional active or inactive additional compounds and/or their amounts so that the beneficial properties of the honey are not or substantially not adversely affected by these intended additives.

When the composition of the present invention is an emulsion, the proportion of the fatty phase may be 0.5-80%, preferably 5-50%, of the total weight of the composition. The oils, emulsifiers and co-emulsifiers used in the compositions in emulsion form may be selected from those generally used in the art. The proportion of emulsifier and co-emulsifier in the composition is 0.3-30%, preferably 0.5-20%, of the total weight of the composition.

The oil used in the present invention can be mineral oil (liquid petroleum), vegetable oil (avocado oil, soybean oil), animal oil (lanolin), synthetic oil (perhydrogenated codlivene), silicone oil (cyclomethicone) and fluorine Carburetion (perfluoropolyether). Fatty substances used may also be fatty alcohols (cetyl alcohol), fatty acids and waxes (carnauba wax, ozokerite).

Emulsifiers and co-emulsifiers that can be used in the present invention may be, for example, fatty acid polyethylene glycol esters such as polyethylene glycol-20 stearate, and fatty acid glycerides such as glyceryl stearate.

Hydrophilic gelling agents can especially be selected from carboxyvinyl polymers (carboxyvinyl formulations), acrylic acid copolymers such as acrylate/alkyl acrylate copolymers, polyacrylamides, polysaccharides, natural gums and clays; lipophilic gelling agents The agent may be a modified clay such as organobentonite, metal salts of fatty acids, hydrophobic silica and polyethylene.

As active ingredients polyols, vitamins, keratolytics and/or exfoliants, anti-inflammatory agents, sedatives and mixtures thereof can be used, among others. Additionally, while unfermented honey alone has depigmenting activity, making it useful as the sole depigmenting active ingredient in whitening compositions, other depigmenting agents such as kojic acid or hydroquinone and Its derivatives, so that the latter can be used in low doses. In fact, a synergistic effect has been observed when unfermented honey is used in combination with kojic acid. In the case of incompatibility, at least some of the active ingredients can be incorporated into microspheres, especially ionic or non-ionic vesicles and/or nanoparticles (nanocapsules and/or nanospheres), so that the mutual Incompatible active ingredients are separated from each other in the composition.

In these compositions, lipophilic or hydrophilic UV filters can also be used, such as benzene-1,4-di(3-methylene-10-camphorsulfo) acid, 2-ethylhexyl α- Cyano-β,β-diphenylacrylate or octocrylene, butylmethoxydibenzoylmethane, octylmethoxycinnamate and/or titanium dioxide and zinc oxide.

These compositions may in particular constitute protective, therapeutic or cosmetic creams for the face, hands or body, protective or cosmetic milks for the body, emulsions, gels or mousses for skin care or treatment, cleansing emulsions or antiseptic lotions, Bath compositions, foundations and tinted creams. In the latter case, the composition contains pigments.

The invention is now illustrated with the aid of the following non-limiting examples.

Embodiment 1: honey decolorization activity experiment

The depigmentation activity of unfermented acacia honey was demonstrated by biological experiments carried out in aqueous solutions with a concentration of 0.1-1-10%.

This experiment corresponds to that described in the applicant's patent FR2734825 and in the article written by R. Schmidt, P. Krien and M. Regnier in "Analytical Biochemistry", Volume 235, No. 2, Page 113-18, 1996. It is performed on co-cultures of keratinocytes and melanocytes.

result

The advantage of honey is that it does not show cytotoxicity to keratinocytes and melanocytes, which is the main disadvantage of existing depigmenting agents.

At a concentration of 0.1-10%, it was further observed that the depigmentation effect of honey was independent of the concentration and comparable to that of a class 2 depigmentation agent (30-60% inhibition of melanocyte production compared to the control group).

Example 2: Honey-Based Compositions

Concentrations are given in percent by weight.

depigmenting lotion

Add appropriate amount of water to 100%

Glycerin 3%

Unfermented Acacia Honey 2%

Preservatives 0.4%

whitening cream

Add appropriate amount of water to 100%

Glycerin 3%

Unfermented Acacia Honey 5%

Preservatives 0.4%

Liquid Petroleum 15%

Sorbitan tristearate 0.9%

Polyethylene glycol stearate 2%

Cetyl Alcohol 4%

Glyceryl Stearate, Potassium Stearate 8%

Sodium Stearate 2%

Since honey is very easy to formulate, the above lotions and creams can be prepared in a conventional manner.

Claims (5)

1. unfermented honey is as the purposes in the cosmetic composition of the depigmenting agent of skin or hair and/or brightening agent and/or treatment skin splash.

2. unfermented honey is used for the decolouring of skin or hair and/or brightens and/or treat the purposes of the dermatosis compositions of skin splash in preparation.

3. purposes according to claim 1 and 2, the concentration that it is characterized in that Mel is the 0.1-10% of composition total weight.

4. purposes according to claim 3, the concentration that it is characterized in that Mel is the 2-5% of composition total weight.

5. skin or hair decolouring and/or brighten and/or treat the beauty method of skin splash is characterized in that it is included in to use the compositions that contains unfermented honey on skin or the hair.