FR2788693A1 - Use of unfermented honey as an agent for depigmenting and/or lightening the skin, body hair or head hair and/or for treating liver spots - Google Patents

Abstract

Unfermented honey is used in a cosmetic or dermatological composition as an agent for depigmenting and/or lightening the skin, body hair or head hair and/or for treating liver spots.

Description

The present invention relates to the use of unfermented honey in a

  cosmetic composition, or for the manufacture of a dermatological composition, as a depigmenting and / or whitening agent for the skin,

  hair or hair and / or to treat pigmentation spots on the skin.

  The invention also relates to a cosmetic process for depigmentation and / or bleaching of the skin, hair or hair, consisting in applying to the skin, the hair or the hair a composition comprising unfermented honey. The color of human skin is a function of various factors, including the seasons of the year, race and sex, and is mainly determined by the nature and concentration of melanin produced by the melanocytes. In addition, at different periods of their life, some people see appear on the skin and more especially on the hands,

  darker and / or more colored spots, giving the skin heterogeneity.

  These spots are also due to a high concentration of melanin in the

  keratinocytes located on the surface of the skin.

  In the same way, the color of the hairs and the hair is due to the melanin, when the hairs or the hair are dark, some people wish to see their lighter. This is particularly interesting for

  hairs that are less visible when they are light than when they are dark.

  The mechanism of formation of the pigmentation of the skin, of the hairs and of the hair, that is to say of the formation of melanin, is particularly complex and schematically involves the following main stages Tyrosine -> Dopa --- > Dopaquinone ---> Dopachrome ---> Melanin

  Tyrosinase (monophenol dihydroxyl phenylalanine: oxygen oxydo-

  reductase EC 1.14.18.1) is the essential enzyme involved in this sequence of reactions. It catalyzes in particular the reaction of transformation of tyrosine into Dopa (dihydroxyphenylalanine) thanks to its hydroxylase activity and the reaction of transformation of Dopa into dopaquinone thanks to its oxidase activity. This tyrosinase only acts when it is in the maturation state under the action of certain

biological factors.

  A substance is recognized as depigmenting if it acts directly on the vitality of epidermal melanocytes where melanogenesis takes place and / or if it interferes with one of the stages of melanin biosynthesis either by inhibiting one of the enzymes involved in melanogenesis or by s intercalating as a structural analogue of one of the chemical compounds in the melanin synthesis chain, a chain which can then be blocked and thus

ensure depigmentation.

  The substances most used as depigmentants are more particularly hydroquinone and its derivatives, in particular its ethers such as the monomethyl ether and the monoethyl ether of hydroquinone. These compounds, although they have a certain effectiveness, are unfortunately not free from side effects due to their toxicity, which can make their use delicate, even dangerous. This toxicity comes from the fact that they intervene on fundamental mechanisms of melanogenesis by killing cells which then risk disturbing their biological environment and which consequently

  force the skin to evacuate them, producing toxins.

  Thus, hydroquinone is a particularly irritating and cytotoxic compound for the melanocyte, the replacement of which, total or partial, has been

envisioned by many authors.

  We thus sought substances which do not intervene in the mechanism of melanogenesis but which act upstream on tyrosinase in

  preventing its activation and are therefore much less toxic.

  The use of harmless topical depigmenting substances with good efficacy is particularly sought in order to treat regional hyperpigmentations by melanocytic hyperactivity such as idiopathic melasmas, occurring during pregnancy ("pregnancy mask" or chloasma) or estrogen-progestogen contraception, localized hyperpigmentations by hyperactivity and benign melanocytic proliferation, such as senile pigment spots called actinic lentigo, hyperpigmentations or accidental depigmentations, possibly due to photosensitization or post-lesional scarring, as well as certain leukoderma, such than vitiligo. For the latter (scarring which can lead to a scar giving the skin a whiter appearance and leukoderma), failing to be able to repigment the damaged skin, we finish depigmenting the areas of residual normal skin to give the whole of

  the skin a homogeneous white shade.

  Also, there remains the need for a new whitening agent for human skin, hair and / or hair with an action as effective as those known, but not having their drawbacks, that is to say which is not irritant, non-toxic

  and / or non-allergenic for the skin and stable in a composition.

  The Applicant has unexpectedly found that unfermented honey exhibits depigmenting activity, even at low concentrations,

without showing cytotoxicity.

  - Honey is commonly used for its moisturizing and bactericidal properties, or in the treatment of wounds, ulcers or burns. It is also known from FR-A-2 751 537 as a keratolytic agent, in particular for improving the radiance of the skin complexion and treating wrinkles. However, it has never been suggested that honey could have activity

  depigmenting by acting directly on melanogenesis.

  A subject of the present invention is therefore the use of unfermented honey in a cosmetic composition as a depigmenting and / or whitening agent for the skin, hair or hair and / or for treating pigmentary spots

skin.

  Another subject of the invention is the use of unfermented honey for the manufacture of a dermatological composition intended for depigmentation and / or bleaching of the skin, body hair or hair and / or for the treatment of

pigment spots on the skin.

  By "unfermented honey" is meant, in the present invention, a honey not containing hydroxy acids, unlike honey extract which is a

  fermentation product which contains hydroxy acids.

  The honey used in this invention consists of a mixture of glucose, levulose, dextrin, sucrose, proteins and water, the content of these various constituents being able to vary according to the origin of the honey. Conventionally, honey can comprise from 72 to 75% of the mixture of glucose and levulose, 15%

  water, 10% dextrin, 2.5% sucrose and 1% protein.

  Honey can come from any source. It can especially be acacia honey, lime blossom, mountain honey, gatinais, orange blossom or any other flower. In the present invention, however, it is preferred to use acacia honey. The amount of honey used according to the invention is for example between 0.1 and 10% by weight, and preferably between 2 and 5% by weight, relative

the total weight of the composition.

  The present invention also relates to a cosmetic process for depigmentation and / or bleaching of the skin, hair or hair and / or treatment of pigmented spots on the skin, comprising applying to the skin, hair or hair, a composition comprising unfermented honey. The cosmetic or dermatological composition containing honey is suitable for topical use and therefore it contains a cosmetically or dermatologically acceptable medium, that is to say compatible with the skin, body hair or hair. It can be in all dosage forms normally used for topical application, in particular in the form of an aqueous, hydroalcoholic solution, an oil-in-water or water-in-oil or multiple emulsion, an aqueous gel , a liquid, pasty or solid anhydrous product, an oil dispersion in an aqueous phase using spherules, these spherules possibly being polymeric nanoparticles such as nanospheres and nanocapsules or, better still, vesicles lipid

ionic and / or non-ionic type.

  This composition can be more or less fluid and have the appearance of a white or colored cream, an ointment, a milk, a lotion, a serum, a paste, a foam. . It can optionally be applied to the skin or to the hair in the form of an aerosol. It can also be in solid form, and for example in the form of a stick. It can be used as a care product and / or as a makeup product. It can also be

  in the form of a shampoo or conditioner, powder or pencil.

  In known manner, the composition according to the invention can also contain the adjuvants usual in the cosmetic and dermatological fields, such as hydrophilic or lipophilic gelling agents, hydrophilic or lipophilic active agents, preservatives, antioxidants, solvents, perfumes, fillers, filters, pigments, odor absorbers and coloring matter. The amounts of these various adjuvants are those conventionally used in the fields under consideration, and for example from 0.01 to% of the total weight of the composition. These adjuvants, depending on their nature, can be introduced into the fatty phase, into the aqueous phase, into the vesicles

  lipids and / or in nanoparticles.

  Of course, a person skilled in the art will take care to choose these possible additional compounds, active or non-active, and / or their quantity, in such a way that the advantageous properties of honey are not, or substantially

  not, altered by the planned addition.

  When the composition according to the invention is an emulsion, the proportion of the fatty phase can range from 0.5 to 80% by weight, and preferably from 5 to 50% by weight relative to the total weight of the composition. The oils, emulsifiers and coemulsifiers used in the composition in the form of an emulsion are chosen from those conventionally used in the field under consideration. The emulsifier and the coemulsifier are present in the composition in a proportion ranging from 0.3 to 30% by weight, and preferably from

  0.5 to 20% by weight relative to the total weight of the composition.

  As oils which can be used in the invention, mention may be made of mineral oils (petrolatum oil), oils of vegetable origin (avocado oil, soybean oil), oils of animal origin (lanolin), oils of synthesis (perhydrosqualene), silicone oils (cyclomethicone) and fluorinated oils (perfluoropolyethers). Alcohols can also be used as fats

  fatty (cetyl alcohol), fatty acids, waxes (carnauba wax, ozokerite).

  As emulsifiers and coemulsifiers which can be used in the invention, mention may, for example, be made of fatty acid and polyethylene glycol esters such as PEG-20 stearate, and fatty acid and glycerin esters such as stearate

glyceryl.

  As hydrophilic gelling agents, mention may in particular be made of carboxyvinyl polymers (carbomers), acrylic copolymers such as acrylate / alkyl acrylate copolymers, polyacrylamides, polysaccharides, natural gums and clays, and, as lipophilic gelling agents, cite modified clays such as bentones, metal salts of fatty acids,

  hydrophobic silica and polyethylenes.

  As active agents, polyols, vitamins, keratolytic and / or scaling agents, anti-inflammatory agents, soothing agents and their mixtures can be used in particular. In addition, although the unfermented honey alone has a depigmenting activity justifying its use as the only depigmenting active ingredient of a whitening composition, other depigmenting agents can also be added to the composition according to the invention, such as Kojic acid or hydroquinone and their derivatives, which allows the latter to be used in lower doses. There is even a synergistic effect when using a combination of unfermented honey and kojic acid. In the event of incompatibility, at least some of the active agents can be incorporated into spherules, in particular ionic or nonionic vesicles and / or nanoparticles (nanocapsules and / or nanospheres), so that the active agents

  incompatible with each other are isolated from each other in the composition.

  UV filters with property can also be used in these compositions

  lipophilic or hydrophilic, such as benzene 1,4-di (3-methylidene10-

  camphosulfonic), 2-ethylhexyl or octocrylene α-cyano- 3, -3-diphenylacrylate, butyl methoxydibenzoylmethane, octyl methoxycinnamate and / or

titanium and zinc oxides.

  These compositions constitute in particular protective, treatment or care creams for the face, for the hands or for the body, body protection or care milks, lotions, gels or foams for the care or treatment of the skin , cleansing or disinfecting lotions, bath compositions, foundations and tinted creams. In these

  last cases, the composition contains pigments.

  The invention will now be illustrated with the aid of the examples not

following limitations.

  EXAMPLE 1 Demonstration of the Depigmenting Activity of Honey A biological test has demonstrated the depigmenting activity of honey

  unfermented acacia, tested at concentrations of 0.1 - 1 - 10% in water.

  This test corresponds to that described in patent FR 2734825 filed by the Applicant, as well as in the article by R. Schmidt, P. Krien and M. Régnier, Anal. Biochem., 235 (2), 113-18, (1996). It is thus produced on coculture of

keratinocytes and melanocytes.

  Results: Honey has the advantage of not showing cytotoxicity towards

  keratinocytes and melanocytes, a major defect in existing depigmenters.

  For concentrations between 0.1 and 10%, it was further observed that the depigmenting effect of honey was independent of the concentration and corresponded to a class 2 depigmenting agent (30 to 60% inhibition of

  melanogenesis compared to the control).

  EXAMPLE 2 Compositions Based on Honey

  The concentrations are given as a percentage by weight.

  Depigmenting lotion Water qs 100% Glycerin 3% Unfermented acacia honey 2% Preservatives 0.4% Whitening cream Water qs 100% Glycerin 3% Unfermented acacia honey 5% Preservatives 0.4% Vaseline oil 15% Tristearate sorbitan 0.9% Polyethylene glycol stearate 2% Cetyl alcohol 4% Glyceryl stearate, potassium stearate 8% Sodium stearate 2% The above lotion and cream can be prepared

  classic, honey being very easy to formulate.

Claims (5)

  1. Use of unfermented honey in a cosmetic composition as a depigmenting and / or whitening agent for the skin, hair or hair and / or for treating pigmentary spots on the skin. 2. Use of unfermented honey for the manufacture of a dermatological composition intended for depigmentation and / or bleaching of the skin,   hair or hair and / or the treatment of pigmentation spots on the skin.   3. Use according to claim 1 or 2, characterized in that the honey is present in an amount ranging from 0.1 to 10% by weight relative to the weight total of the composition.   4. Use according to claim 3, characterized in that the honey is present in an amount ranging from 2 to 5% by weight relative to the total weight of the composition. 5. Cosmetic process for depigmentation and / or bleaching of the skin, body hair or hair and / or treatment of pigmented spots on the skin, characterized in that it consists in applying to the skin, body hair or hair   a composition comprising unfermented honey.