WO1998043608A1

WO1998043608A1 - Cosmetic compositions comprising at least one hyptis extract

Info

Publication number: WO1998043608A1
Application number: PCT/FR1998/000440
Authority: WO
Inventors: Daniel Greff
Original assignee: Sederma S.A.
Priority date: 1997-04-02
Filing date: 1998-03-05
Publication date: 1998-10-08
Also published as: FR2761604A1; AU6839398A; FR2761604B1

Abstract

Plants of the genus Hyptis (Labiatae family) are used for making extracts used in cosmetics for lightening the skin, eliminating freckles and improving and homogenising complexion. Inter alia, the H. pectinata, H. verticillata, H. capitata, H. mutabilis, H. suaveolens, H. spicigera species can be used. The extracts, obtained by the usual (maceration, decoction) or novel (microwaves, ultrasounds) methods can contain variable amounts of phenolic, flavonoid derivatives or hydroquinone derivatives.

Description

TITLE: COSMETIC COMPOSITIONS COMPRISING AT LEAST ONE HYPTIS EXTRACT

The pigmentation of the skin is due to the synthesis of melanin in specialized cells, as well as to the homogeneous distribution of this melanin in the keratinocytes of the epidermis. In healthy, perfect skin, this synthesis is well regulated, modulated by exposure to the sun and by the desquamation process.

It happens, however, in many cases that this complex process is disturbed: a lack of melanogenesis (either due to a genetic problem, or following a skin injury) is as possible as a localized overabundance of pigmentation : freckles, age spots, and diffuse spots (chloasma, pregnancy spots) are the most well-known phenomena.

Since these symptoms do not constitute real pathologies, being more of an aesthetic problem than of health, and since melanogenesis takes place within the epidermis, it is rather the cosmetic industry than the pharmaceutical which is interested in this problem.

Many molecules or substances have been proposed to treat hyperpigmentation of the skin, but few of them can be retained for a topical cosmetic application (problem of irritation, legislation, toxicity). Those that remain after this selection are generally not very effective.

The object of this patent is the discovery that plant extracts belonging to the genus Hyptis, also called Hiptis, (family of Labiatae) have a strong biological activity which makes it possible to use them advantageously in cosmetic compositions intended for depigmentation, therefore for lighten the skin, reduce freckles, dark spots, chloasma and other skin discolourations. The usable species of the genus Hyptis include among others the plants H. pectinata, H. verticillata, H. capitata, H. mutabilis, H. suaveolens, H. spicigera without this list being exhaustive. The advantage of the extracts of this plant lies in a favorable ratio of biological activity on dry matter (and associated color), which is often problematic in cosmetic herbal medicine. The extracts are stable, odorless and easy to use in any type of cosmetic product. The extraction solvents for the preparation of the extracts which are the subject of this patent can be chosen from water, propylene glycol, butylene glycol, glycerin, polyethylene glycols, methyl or ethyl ethers of diglycols, cyclic polyols, ethoxy or propoxylated diglycols or any mixture of these solvents.

The extracts can be obtained by maceration of the plant in the extraction solvent, for a more or less long period. Instead of simple maceration, one can use, for example, countercurrent techniques, decoction, leaching, extraction using ultrasound, microwaves.

For certain cosmetic applications it may prove useful to prepare a dry extract from the liquid extract. This can be achieved by conventional techniques of precipitation, drying, evaporation, atomization or delyophilization.

Other plants, like the bearberry (Uva ursi L.) contain derivatives of hydroquinone and are already used for skin depigmentation. A particular aspect of the discovery which is the subject of this patent is the fact that the combination of extracts of Egyptis spp. and d'Uva ursi L. (Bearberry) is particularly active in this application, more than the simple addition of the effects suggests.

Examples will illustrate the achievements of the patent: Example No. 1: preparation of an extract of Egyptis verticillata 100 g of dry plant (aerial parts) are finely ground, then mixed with the extraction solvent (glycerin / water 80 / 20) and extracted by rapid heating in the microwave. After separation of the plant from the solvent, the extract is discolored, possibly preserved and standardized. Example No. 2: Ethanolic extract of Egyptis spicigera 100 g of dry plant (aerial parts) are finely ground, then extracted to exhaustion with 1 I of ethanol at 55 ° C. After separation of the plant residues by filtration, the filtrate is filtered on charcoal, then concentrated by dry evaporation. It is then taken up in a propylene glycol-water mixture (50/50) at a concentration of 3%.

Example 3: depigmenting cream

Brij ^R 721 2.4

Brij ^R 72 2.6

Arlamol ^R E 8.0

Beeswax 0.5

Abil ^R ZP 2434 3.0

Propylene glycol 3.0

Carbopol "941 0.25

0.25 triethanolamine Liquid extract of Egyptis spicigera 7.0

(according to example n ° 2)

Water, preservatives, perfumes qs 100 g.

Example No. 4: Biochemical activity of the extract of Egyptis verticillata.

An extract prepared according to the extraction method described in Example 2 is subjected to the tyrosinase inhibitory activity test. Tyrosinase is the key enzyme in melanogenesis. It converts tyrosine to dopa and dopa to dopachrome. The enzymatic reaction can be followed by spectroscopy at 475 nm (appearance of dopachrome). A depigmenting action goes - most of the time - through an inhibition of this enzymatic reaction which prevents the synthesis of new melanin molecules in the skin.

The test, carried out according to standard enzymatic protocols (SIGMA phenolase and tyrosinase protocol), shows the high activity of the extract of Egyptis verticillata. The inhibition effect depends on the dose: at 0.025% the inhibition is

55%, at 0.05% it rises to 78%, at 0.75% it is 91% and at 0.1% it is 99.0%. In combination 3: 1 to 1: 3 (w / w) with a similar extract obtained from the bearberry, the active concentrations can be further reduced thanks to an obvious synergistic effect between the two extracts as shown in the following table:

Inhibition%

Extract from H. verticillata at 0.01% 0%

0.01% Uva ursi extract 2%

Extract from H. 0.005% verticillata in combination with 0.005% Uva ursi Extract 45%

Extracts from Egyptis spp. alone or in combination with extracts of Uva ursi L., subject matter of the patent can be used in cosmetic and dermopharmaceutical products of all kinds. Such compositions have regulatory activities for complexion, coloring of the skin, reduction of the intensity of brown spots (freckles), elimination or attenuation of the symptoms of chloasma.

Their main use is in specific skin care cosmetics (skin lightening) but the extracts can be incorporated into any cosmetic product since, in addition to the depigmenting activities of the substances contained in the extracts, it is found that these same extracts, especially in combination with bearberry extracts (Uva ursi L.) help restructure the epidermis, improve the appearance of the skin, reduce capillary microcirculation (anti-rosacea effect), give elasticity and firmness to tired skin.

Extracts from Egyptis spp. alone or in combination with extracts of Uva ursi L. subjects of the patent can also find application in the treatment of the scalp (anti-dandruff) or acne skin.

Extracts from Egyptis spp. alone or in combination with the extracts of Uva ursi L. subject of this patent can be used in any dosage form used in cosmetics: O / W and W / O emulsions, milks, lotions, gels, ointments, body oils, hair lotions, shampoos, soaps, sticks and pencils, sprays, without this list being exhaustive.

It is possible to incorporate extracts of Egyptis spp. alone or in combination with the extracts of Uva ursi L. described in cosmetic vectors such as liposomes, chylomicrons, macro-, micro- and nanoparticles as well as macro-, micro- and nanocapsules, to absorb them on polymers powdery organic, talcs, bentonites and other mineral supports.

The concentration of use of these extracts of Egyptis spp. alone or in combination with extracts of Uva ursi L. can vary between 0.01 and 90% (w / w), preferably between 0.5 and 10% in the finished product. Extracts from Egyptis spp. alone or in combination with extracts of Uva ursi L. can be combined in cosmetic compositions with any other ingredient usually used in cosmetics: extraction and / or synthetic lipids, gelling and viscosifying polymers, surfactants and emulsifiers, active ingredients water- or fat-soluble, extracts from other plants, tissue extracts, marine extracts.

Claims

1) Cosmetic or dermopharmaceutical compositions with depigmenting activity, inhibiting or regulating melanogenesis and coloring of the skin, acting against brown spots (freckles), chloasma or other abnormal colorings characterized in that they contain at least one plant extract of the genus Hyptis or Hiptis (family of Labiatae).

2) Cosmetic or dermopharmaceutical compositions according to claim 1, characterized in that the Egyptis extract is obtained from the whole plant, preferably from the aerial part of the plant (s) chosen from H. spicigera. , H. verticillata, H. pectinata ,, H. capitata, H. mutabilis, H. suaveolens.

3) Cosmetic or dermopharmaceutical compositions according to claim 1 characterized in that the extract of Egyptis is used in combination with an extract of Uva ursi L. (bearberry) for a synergistic effect.

4) Cosmetic or dermopharmaceutical compositions according to claims 1 to 3, characterized in that the extract of Egyptis alone or in combination with the extract of Uva ursi L. is obtained by extraction from the plants by maceration techniques, leaching, decoction, counter-current extraction, extraction using ultrasound or microwaves.

5) Cosmetic or dermopharmaceutical compositions according to any one of claims 1 to 4, characterized in that the extraction solvent is chosen from the group consisting of: water, propylene glycol, butylene glycol, glycerin, polyethylenes glycols, methyl or ethyl ethers of diglycols, cyclic polyols, ethoxylated or propoxylated diglycols or any mixture of these solvents. 6) Cosmetic or dermopharmaceutical compositions according to any one of claims 1 to 5, characterized in that the extract is used either in liquid form or in dry form obtained by precipitation, atomization, evaporation or lyophilization.

7) Cosmetic or dermopharmaceutical compositions according to one any one of claims 1 to 6 characterized in that the concentration of the extract of Egyptis alone or in combination with the extract of Uva ursi L. is between 0.01 and 90% (w / w), preferably between 0.5 and 10% by weight of the total composition.

8) Cosmetic or dermopharmaceutical compositions according to any one of claims 1 to 7, characterized in that the extract of Egyptis alone or in combination with the extract of Uva ursi L. is used in any galenic form used in cosmetics or dermopharmacy namely O / W and W / O emulsions, milks, lotions, gels, ointments, body oils, hair lotions, shampoos, soaps, sticks and pencils, sprays.

9) Cosmetic or dermopharmaceutical compositions according to any one of Claims 1 to 8, characterized in that the extract of Hyptis alone or in combination with the extract of Uva ursi L. is incorporated in cosmetic vectors such as liposomes, chylomicrons, macro-, micro- and nanoparticles as well as macro- micro- and nanocapsules, or absorbed on powdery organic polymers, talcs, bentonites and other mineral supports.

10) Cosmetic or dermopharmaceutical compositions according to any one of claims 1 to 9 characterized in that the extract of Egyptis alone or in combination with the extract of Uva ursi L. is combined in the cosmetic compositions with any other ingredient usually used in cosmetics: extraction and / or synthetic lipids, gelling and viscosifying polymers, surfactants and emulsifiers, water- or liposoluble active principles, plant extracts, tissue extracts, marine extracts.

1 1) Use of the cosmetic or dermopharmaceutical compositions according to any one of claims 1 to 10 in cosmetic applications for skin care, particularly the regulation of the complexion, the depigmentation, the elimination or the attenuation of brown spots ( freckles), symptoms of chloasma and other abnormal skin colors. 12) Use of the cosmetic or dermopharmaceutical compositions according to any one of claims 1 to 10 for restructuring the epidermis, improving the appearance of the skin, reducing capillary microcirculation (anti-rosacea effect), improving elasticity and firmness to tired skin.

13) Use of the cosmetic or dermopharmaceutical compositions according to any one of claims 1 to 10 for the treatment of the scalp, in particular anti-dandruff, or the treatment of acneic skin.