Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
  • A61K36/18—Magnoliophyta (angiosperms)
  • A61K36/185—Magnoliopsida (dicotyledons)
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
  • A61K8/14—Liposomes; Vesicles
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
  • A61K8/34—Alcohols
  • A61K8/347—Phenols
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
  • A61K8/36—Carboxylic acids; Salts or anhydrides thereof
  • A61K8/365—Hydroxycarboxylic acids; Ketocarboxylic acids
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
  • A61K8/37—Esters of carboxylic acids
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
  • A61K8/44—Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
  • A61K8/4973—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/63—Steroids; Derivatives thereof
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/64—Proteins; Peptides; Derivatives or degradation products thereof
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/67—Vitamins
  • A61K8/671—Vitamin A; Derivatives thereof, e.g. ester of vitamin A acid, ester of retinol, retinol, retinal
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/67—Vitamins
  • A61K8/676—Ascorbic acid, i.e. vitamin C
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
  • A61K8/73—Polysaccharides
  • A61K8/735—Mucopolysaccharides, e.g. hyaluronic acid; Derivatives thereof
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
  • A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
  • A61K8/9783—Angiosperms [Magnoliophyta]
  • A61K8/9789—Magnoliopsida [dicotyledons]
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P17/00—Drugs for dermatological disorders
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q19/00—Preparations for care of the skin
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q19/00—Preparations for care of the skin
  • A61Q19/02—Preparations for care of the skin for chemically bleaching or whitening the skin
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q19/00—Preparations for care of the skin
  • A61Q19/08—Anti-ageing preparations
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q5/00—Preparations for care of the hair
• • C—CHEMISTRY; METALLURGY
  • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
  • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
  • C12N5/00—Undifferentiated human, animal or plant cells, e.g. cell lines; Tissues; Cultivation or maintenance thereof; Culture media therefor
  • C12N5/06—Animal cells or tissues; Human cells or tissues
  • C12N5/0602—Vertebrate cells
  • C12N5/0625—Epidermal cells, skin cells; Cells of the oral mucosa
  • C12N5/0629—Keratinocytes; Whole skin
• • C—CHEMISTRY; METALLURGY
  • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
  • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
  • C12N2500/00—Specific components of cell culture medium
  • C12N2500/70—Undefined extracts
  • C12N2500/76—Undefined extracts from plants

Definitions

• the present invention essentially relates to the use of an extract of Simaba for the manufacture of a cosmetic or pharmaceutical composition, in particular dermatological, having in particular a depigmenting activity and an activity promoting the differentiation of keratinocytes, and intended in particular for attenuation skin pigmentation spots, especially spots of senescence, in the treatment of vitiligo, in strengthening the protective function of the skin, or in improving the appearance of the hair; or for the preparation of a culture medium for skin cells, and composition thus obtained.
• the invention relates to the use of an extract of Simaba for the manufacture of a cosmetic or pharmaceutical composition, in particular dermatological, having in particular a depigmenting activity as well as an activity promoting the differentiation of keratinocytes, and intended for particular to treat skin pigment spots, especially spots of senescence, to treat vitiligo, skin disorders accompanied by dysregulations of the differentiation of keratinocytes, such as psoriasis, to restore, preserve and / or reinforce protective function of the skin, in particular the water barrier function, as well as the cohesion of the cells of the epidermis or even improving the quality of the hair; or for the preparation of a cell or tissue culture medium, in particular for the mass culture of skin cells, in particular of keratinocytes.
• the Simaba plant is a plant from the Simaroubaceae family.
• Simaba cedron Plantchon
• Simaba cuspidata Sprucc
• Simaba moretii Simaba multiflora
• Simaba multiflora Adr. Juss.
• Simaba guyanensis Align Engl.
• Simaba cedron (Planch.) Is a tree from the forests of Central America, especially Guyana.
• the natives use the roots of this tree as a dewormer or as an antimalarial remedy. They use also the bark in decoction for the preparation of baths intended to treat rashes of various origins.
• the seeds of this tree have been used for a long time as a remedy against snake bites, both in local applications on the wound and in ingestion.
• the inventors of the present invention have been able to observe that the Simaba extracts are particularly active at the melanocyte level with regard to the inhibition of elanogenesis, this activity having been able to be demonstrated by in vitro tests on cultures. of melanocytes, which will be described later.
• the extracts of -Simaba are also particularly active in promoting the differentiation of keratinocytes and can thus be used to treat skin disorders accompanied by dysregulation of the differentiation of keratinocytes.
• This differentiation is reflected in particular, at the level of the epidermis, by greater cell cohesion, by regulation of the transformation of keratinocytes into comeocytes by loss of the nucleus and increase in cellular corneification, by an increase in the number of layers of comeocytes forming the stratum corneum, all of these phenomena contributing to the strengthening of the protective function of the skin vis-à-vis the external environment and to the strengthening of the water barrier preventing excessive loss of water by the epidemic; and, at the level of the hair follicle, a regulation of the processes of synthesis of keratins by keratinocytes, these proteins being the main constituent of the hair shaft and the quality of which is essential for a hair in good condition.
• the inventors have observed that these extracts make it possible to promote
• the present invention aims to solve the new technical problem consisting in the supply of a new formulation of cosmetic or pharmaceutical compositions, in particular dermatological compositions having good depigmentation efficiency, thereby making it possible to use it for the treatment of pigment spots.
• skin in particular spots of senescence, as well as, in the treatment of vitiligo, the attenuation of the contrast between the areas affected by vitiligo and their surroundings.
• the spots of senescence result from complex phenomena, generally comprising local hypercoloration linked to hyperpigmentation and sometimes accompanied by localized hyperkeratosis.
• the main object of the present invention is also to solve the technical problem consisting in the supply of a new formulation of cosmetic or pharmaceutical composition, especially dermatological, having an activity promoting the differentiation of keratinocytes and intended in particular for treat skin disorders accompanied by dysregulation of the differentiation of keratinocytes, such as psoriasis, to restore, preserve and / or strengthen the protective function of the skin, in particular the water barrier function, thus leading to a hydrating effect, by in particular by preventing excessive loss of water from the epidermis, an advantageous application of which is the treatment of ichthyotic skin as well as the treatment of psoriatic skin, and of improving the quality of the hair, thus enhancing the appearance of the hair .
• the main object of the present invention is also to solve the new technical problem consisting in providing a solution making it possible to promote, accelerate and improve the differentiation of skin cells, in particular keratinocytes, in culture.
• the present invention solves these technical problems satisfactorily for the first time and can be used on an industrial scale for the preparation of cosmetic or dermatological compositions, or for the preparation of culture media, in particular in mass of skin cells.
• the present invention relates to the use of an extract of Simaba for the manufacture of a cosmetic or pharmaceutical composition, in particular dermatological, having in particular a depigmenting activity, and intended in particular for treating spots skin pigments, especially age spots, to treat vitiligo, skin disorders accompanied by dysregulation of the differentiation of keratinocytes, such as psoriasis, to restore, preserve and / or strengthen the protective function of the skin, in particular the water barrier function, as well as the cohesion of the cells of the epidermis or to improve the quality of the hair; or for the preparation of a cell or tissue culture medium, in particular for the mass culture of skin cells, in particular of keratinocytes.
• the abovementioned extract is obtained from Simaba cedron (Planchon), Simaba cuspidata (Spruce), Simaba moretii, Simaba multiflora (Adr. Juss.), Simaba guyanensis (Aublet Engl.), In particular from bark of trunks, stems or roots of these plants.
• the abovementioned extract is an extract obtained by extraction with at least one polar solvent, such as water, a alcohol, preferably a lower alcohol, such as methanol or ethanol, a glycol, in particular propylene glycol, or a hydro-alcoholic mixture in any propor ⁇ tion.
• the above-mentioned extract is present in the composition at a concentration of between 0.001 and 5% by weight, expressed as dry extract, relative to the total weight of the composition, preferably between 0.01 and 1% and more preferably between 0.1 and 0.5% by weight.
• the aforementioned composition contains, in addition, an active agent chosen from the group consisting of kojic acid and its salts or esters, caffeic acid and its salts or esters, hydroquinone and its derivatives, a mulberry extract, tretinoin, vitamin A or its derivatives or esters, a carotenoid, in particular beta-carotene, vitamin C, a corticosteroid, glutathione, cysteine, parahydroxycinnamic acid or its salts or esters, salts, esters and derivatives of the abovementioned substances being chosen from those which are cosmetically or pharmaceutically acceptable.
• an active agent chosen from the group consisting of kojic acid and its salts or esters, caffeic acid and its salts or esters, hydroquinone and its derivatives, a mulberry extract, tretinoin, vitamin A or its derivatives or esters, a carotenoid, in particular beta-carotene, vitamin C, a corticosteroid,
• the aforementioned composition can also contain at least one moisturizing agent, such as hyaluronic acid.
• the abovementioned mulberry extract is present in a proportion by weight of between 0.001 and 5%, preferably between 0.01 and 1%, more preferably between 0.1 and 0.8% by weight. relative to the total weight of the composition.
• the kojic acid or its abovementioned salts or esters is present in the composition in a proportion by weight of between 0.001 and 5%, more preferably between 0.01 and 2%, by weight relative to the total weight of the composition.
• the aforementioned extract of Simaba is at least partly incorporated in hydrated lipidic lamellar phases or in liposomes, either alone or combined with at least one other active substance present in the composition.
• the preparation of liposomes containing at least part of the abovementioned Simaba extract can be carried out according to one of the known methods for incorporating active substances into liposomes.
• a process is used for atomizing the constituents of the lipid phase, making it possible to obtain a lipid powder easily dispersible in an aqueous solution. to form liposomes, for example according to the method described in document US-A-4,508,703.
• the suspension of liposomes thus obtained can be homogenized using ultrasound, or in the case of mass production, at by means of pressure homogenization, in accordance with the process described in US-A-4,621,023.
• the above-mentioned Simaba extract can be incorporated either in the lipid phase or in the aqueous phase of the liposomes in particular using the methods described above.
• the procedure can be as follows.
• the Simaba extract is dissolved with the constituents of the lipid phase, before atomization, in an organic solution containing at least one amphiphilic lipid, such as soy lecithin, optionally a hydrophobic liphophilic compound such as a stcrol, especially cholesterol or ⁇ -sitosterol.
• the solvent is chosen from dichloromethane, chloroform or methanol, or one of their mixtures.
• the organic solution can advantageously contain an antioxidant agent such as ⁇ -tocopherol.
• the lipid powder obtained is dispersed in a suitable aqueous medium, for example a PBS buffer solution, a glucose solution or a sodium chloride solution. A suspension of liposomes is thus obtained.
• a suitable aqueous medium for example a PBS buffer solution, a glucose solution or a sodium chloride solution.
• the liposome compositions are gelled by mixing with a gel, such as a vinyl polymer gel, in particular marketed under the trade name Carbopol® 940.
• a gel such as a vinyl polymer gel, in particular marketed under the trade name Carbopol® 940.
• This gelation procedure is also described in US-A-4,508,703, in particular in the examples.
• the concentration of the abovementioned Simaba extract is between 0.001 and 30% by weight, preferably between 0.01 and 10% by weight, of the lipid phase of said liposomes .
• the present invention also relates to a cosmetic, or pharmaceutical, in particular dermatological, composition preferably for topical application, having in particular a depigmenting activity, as well as an activity promoting the differentiation of keratinocytes, and intended in particular for treating skin pigment spots, in particular age spots, to treat vitiligo, skin disorders accompanied by dysregulation of the differentiation of keratinocytes, such as psoriasis, restore, preserve and / or strengthen the protective function of the skin, in particular the water barrier function, thus in particular making it possible to obtain a hydrating effect by preventing excessive loss of water by the epidermis, thus allowing use in particular for the treatment of dry skin, whatever the degree of dryness, including ichthyotic skin, and psoriatic skin, to improve
• a composition according to the invention described above containing an extract of Simaba, optionally in form at least partially incorporated in hydrated lipidic lamellar phases or in liposomes, can be in different forms usable in cosmetics or in dermatology.
• these compositions can be gels, creams, milks or lotions.
• compositions applied to the areas to be treated of the skin, or of the scalp, have the effect of regulating the differentiation of keratinocytes, thereby promoting the formation and restoration of good quality epidermis, in particular at the layer cornea, to reinforce the protective skin barrier function of the epidemic, in particular of water barrier, and to obtain an embellishment of the hair, as was explained above as regards the effects and the advantages of this differentiation .
• the cosmetic or dermatological composition according to the invention has a hydrating power, in particular by preventing excessive loss of water in the epidemic, and can be intended for the treatment of dry skin. , especially ichthyotic skins.
• the cosmetic or dermatological composition according to the invention makes it possible to restore the normal differentiation of keratinocytes during their transfomiation into comeocytes, accom- worsened by the loss of the nucleus and cellular comification.
• this composition can be intended for the treatment of psoriatic skin.
• the Simaba extract is incorporated into a cosmetically or dermatologically acceptable excipient.
• the Simaba extract can be incorporated into hydrated lipid lamellar phases or liposomes, as described for the first previous aspect.
• the present invention also relates to a cell or tissue culture medium, in particular for the culture of skin cells, in particular of keratinocytes, making it possible to promote, accelerate and improve their differentiation, characterized in that it includes an effective amount of a Simaba extract to achieve such differentiation.
• the invention also relates to a method for promoting, accelerating or improving the differentiation of skin cells, in particular keratinocytes, in particular in the context of a mass culture of skin cells, for the production of skin.
• a culture medium is used as defined in the preceding description, or in the following description taken as a whole.
• cell differentiation presents in particular a great industrial interest.
• the method of the invention being particularly advantageous in the case of self-grafts of burn victims, thanks to the time savings it provides in the preparation of artificial skin.
• the acceleration and improvement of the differentiation of keratinocytes results in the faster formation of a good quality horny layer;
• this culture method will generally comprise the preparation of a culture medium for the growth of human keratinocytes comprising a DMEM nutritive base medium (Gibco®), epidermal growth factor ("EGF”), 10% fetal calf serum, isoproterenol and / or forskolinc, as well as hydrocortisone.
• this medium also comprises an extract of Simaba as described in the preceding or following description, generally at a concentration of 0.01 to 0.5% by weight.
• a mass culture of skin cells is carried out by inoculating keratinocytes in order to immobilize them on supports such as hollow fibers, microbeads, or microporous matrices and this using the culture medium above.
• supports such as hollow fibers, microbeads, or microporous matrices and this using the culture medium above.
• the culture medium according to the invention can advantageously be used for the mass culture of skin cells, in particular keratinocytes, for the production of artificial skin or for the preparation of reconstituted skin models.
• the present invention also covers a cosmetic or dermatological treatment process for the phenomena of cutaneous hyperpigmentation, comprising in particular spots of senescence and other cutaneous pigment spots, characterized in that one applies, at least to the skin pigment spots to be treated, an effective amount of a Simaba extract to obtain their attenuation.
• this extract is obtained from the plant of Simaba cedron (Planch.), In particular from the bark. Particular extracts have been described in the preceding description.
• the present invention also relates to a cosmetic or dermatological treatment process for vitiligo, charac ⁇ terized in that it is applied, at least to the pigmented areas of the skin bordering those depigmented by vitiligo, an effective amount of a Simaba extract to obtain attenuation of the pigmentation of said pigmented areas, thereby attenuating the contrast between the pigmented areas affected by vitiligo and their surroundings, which improves the aesthetic appearance of the subject.
• the extract can be applied in the form of a composition containing a Simaba extract at a concentration of between 0.001 and 5%, expressed as dry extract, relative to the total weight of the composition, preferably between 0.01 and 1% and more preferably between 0.1 and 0.5% by weight.
• a concentration of between 0.001 and 5%, expressed as dry extract relative to the total weight of the composition, preferably between 0.01 and 1% and more preferably between 0.1 and 0.5% by weight.
• a complementary active principle in particular a hydrating agent such as hyaluronic acid.
• the composition when the composition is a cosmetic composition, the abovementioned Simaba extract can be advantageously incorporated in a cosmetically acceptable excipient.
• this composition is a pharmaceu ⁇ tic, in particular dermatological, composition
• the aforementioned Simaba extract can be incorporated in a pharmaceutically acceptable, in particular dermatologically, excipient.
• excipients are well known to those skilled in the art and also result from the description of several examples of compositions which will follow.
• the excipient of the cosmetic composition, or that of the pharmaceutical composition is at least partly made up of very small solid particles, in particular of the order of 0.05 ⁇ m to 100 ⁇ m , and the Simaba extract, as active substance, is distributed, at least in part, on the surface of said particles, as described in French patent application FR-A-2 685 635.
• Example 1 of the invention Aqueous extract of Simaba bark
• the removal of the solvent in this case water, can be continued until a dry extract is obtained, by evaporation under reduced pressure or by lyophilization.
• the depigmenting activity of the extracts according to the invention is determined at different non-cytotoxic concentrations on melanocyte cultures of the Cloudman S91 line originating from ATCC and bearing the reference CCL 53.1 clone M-3. Each concentration of extract is tested on three culture dishes.
• the culture dishes are prepared by introducing 200,000 S91 cells per dish into a culture medium consisting of complete EMEM medium containing 2% v / v of fetal calf serum and 0.08 ⁇ g / ml of mitomycinc C.
• the melano ⁇ cytes are counted with a counting device such as the "Counter Coulter®" and the melanin content of the cells is determined by measuring the absorbance at 405 nm then by transfoming this value in quantity of melanin by means of a standard curve established with synthetic melanin from the company Sigma which establishes a linear relationship between known quantities of melanin and the absorbance at 405 nm. The amount of melanin is then reduced to 10 ⁇ melano ⁇ cytes.
• a control culture of melanocytes was carried out in three dishes, with the same cell line and under the same culture conditions. Turkish, except that the renewal medium introduced 24 h after incubation contains no product to be tested according to the invention.
• the significance of the results is determined by the Student t statistical test with a threshold of 0.05, which compares the cultures treated with the products, to the control cultures, not treated.
• Depigmenting activity A is calculated as follows
• product II produces a depigmenting activity of at least 19% compared to the control, even at the very low dose of 1 ⁇ g / ml, this activity increasing up to 54% for a dose of l ⁇ g / ml.
• the product 12 provides a depigmenting activity of at least 24.3% at the low dose of 2.8 ⁇ g / ml.
• products II and 12 exhibit significant depigmenting activity.
• this culture medium can be constituted by an M199 medium supplemented with 2 mM of L-glutamine, 10% of fetal calf serum, cholera toxin, hydrocortisonc, as well as the epidermal growth factor EGF.
• the culture medium is renewed by an identical medium on 6 of the 12 wells which constitute untreated control wells, and, on the 6 remaining wells, constituting the treated wells are renewed with an identical medium, but in which 2.5 ⁇ g / ml of extract of Simaba cedron as obtained in Example 2, or product 12, have been dissolved and on which a sterilizing filtration is carried out on filter, for example at 0.22 ⁇ m.
• Sections of each of the resin blocks thus obtained are produced in the form of ultrafine sections, for example using a device known by the name of Microtome, and this is observed with a transmission electron microscope.
• the upper layers of the treated cultures exhibit regular comification with well-formed long comocytes and little intercellular space, while the upper layers of the control cultures generally have undifferentiated comocytes and non-uniform stratification;
• the desmosomes of the intermediate layers of the treated cultures are large and well differentiated, while the desmosomes of the control cultures are only at the beginning of a differentiation;
• the upper layers of the treated cultures have a density of keratin very much higher than the density of keratin observed in the same upper layers of the control cultures.
• Simaba cedron extracts to the preparation of cosmetic or pharmaceutical compositions, in particular dermatological compositions, in particular the following:
• compositions promoting the formation of a well-differentiated epidermis, thus giving "beautiful” skin with a pleasant texture and feel;
• compositions combating disorders of epidermal differentiation, occurring in particular during aging; - compositions reinforcing the skin barrier therefore protecting from external aggressions, for example by allergens or surfactants, on the one hand, and limiting the excessive loss of water by the epidemic, on the other hand;
• compositions making it possible to improve the quality of the hair, in particular by improving the quality of the keratin of the hair shaft originating from the activity of the keratinocytes of the follicles which differentiate from the base of the hair.
• compositions in particular demiatological compositions according to the invention, using an extract of Simaba are given below.
• Example 5 Cosmetic or dermatological depigmenting composition in the form of a gel
• This gel is used topically twice a day for 6 weeks on the areas of the skin to be depigmented.
• Example 6 Cosmetic or dermatological composition containing an extract of Simaba in liposomes, in the form of a gel
• Example 2 0.3 g of product 12 of Example 2 is taken, which is dissolved in 50 ml of a dichloromethane / methanol mixture 8-2 (v / v) to which 9 g of soy lecithin and 1 are added. g of cholesterol.
• the solution obtained can be treated to obtain a suspension of liposomes by the well-known rotary container evaporation process which consists in depositing a lipid layer in the flask of the rotary evaporator by evaporation of the solvent, then adding water or a suitable aqueous solution containing preservatives, well known to those skilled in the art, to obtain 100 g of aqueous suspension of liposomes.
• This suspension can be homogenized by means of ultrasound at the power of 150 W for 10 min at 4 * C.
• the homogenized liposome suspension obtained is then gelled by addition of an equivalent weight of 2% Carbopol 940® gel, neutralized with triethanolamine.
• a gelled composition is thus obtained containing 0.15% by weight of product 12 incorporated at least in part into the lipid bilayer of the liposomes, relative to the total weight of the composition.
• This composition can be applied locally, for example once a day for 4 weeks, in order to reduce age spots.
• This gel is used in local applications on stains.
• HELIOCAROTTE® is in the form of an oil titrated at 0.05% in ⁇ -carotene. It is commercially available from BERTIN, Courbevoie - France.
• This milk is used in application after the shower on the parts of the body to be treated, once a day by cures of two to three weeks.
• the components are mixed in a conventional manner to obtain a treating emulsion applied morning and evening by lightly massaging the areas to be treated. This emulsion is used as a day and / or night cream.
• Example 12 Dermatological composition for the treatment of psoriatic skin
• the Simaba Cedron extract is introduced into the aqueous excipient to disperse it, then the Carbopol gel is added so as to obtain a gelled composition which is applied locally to the lesions for 6 weeks.
• This composition makes it possible in particular to reinforce the skin water barrier function of the epidemic by improving the epidermal inter-cellular cohesion. It thus allows the skin to maintain a satisfactory state of hydration.
• EXAMPLE 14 Liposomal Cosmetic Composition for Balancing the Exfoliation of the Corneal Layer of the Epidemic and Giving a Smooth Epidemic
• an aqueous suspension of liposomes is prepared encapsulating the methanolic extract of Simaba cedron of Example 2 in the lipid phase of said liposomes.
• 0.1 g of the methanolic extract of Simaba cedron from Example 2 2 g of soy lecithin and 0.2 g of ⁇ -sitosterol are dissolved in 50 ml of a 4: 1 mixture of dichloromethane and methanol . This solution is evaporated under reduced pressure (200 mm Hg approximately) in a rotary flask heated at 45 ° C.
• the lipid film obtained is taken up in 25 ml of an aqueous solution of monopotassium phosphate and 0.2 g 1 phosphate disodium at 1.44 g / 1, with stirring for 1 h.
• the cream can be applied daily to the face in the event of rough skin flaking off.
• This composition strengthens the cohesion of the stratum corneum and regulates the detachment of dead cells.
• Example 15 Cosmetic composition containing an extract of Simaba cedron. intended for the preventive treatment of dry skin
• the methanolic extract of Simaba cedron of Example 2 is conventionally incorporated into the cream emulsion excipient, to obtain the cream according to the invention.
• the aqueous extract of Simaba cedron obtained in Example 1, as well as glycerol and hvaluronic acid, is conventionally incorporated into the cream emulsion excipient to obtain the cream according to the invention.
• an optimal culture medium for the growth of human keratinocytes comprising a nutritive base medium DMEM (Gibco®), growth factor EGF, 10% fetal calf serum, isoproterenol and / or forskolin, as well as hydrocortisonc.
• This medium will comprise an extract of Simaba according to the invention, preferably at a concentration of 0.01 to 0.5% by weight of extract of Simaba relative to the total weight of the final culture medium.
• a culture based on skin cells is carried out by inoculating keratinocytes in order to immobilize them on supports such as hollow fibers, microbeads, or microporous matrices and this using the culture medium described above.
• An infusion in a medium in an infusion system of the type described by Sylvie GUICHARD-BALESTR1NI in the journal Biofutur, supplement no.56, April 1987, pages 2 to 14, will be provided in order to have an adequate contribution to the growth and differentiation even when the biomass is large.
• the substances secreted by the keratinocytes are recovered, containing mainly lipids, sources of raw material for the formulation of cosmetic or pharmaceutical compositions for topical application to the epidemic or the scalp.
• the product of the invention it is possible to treat reconstituted skin cultures, in particular cultures of keratinocytes or other epidermal cells cultivated on an appropriate support, such as a collagen support (containing or not containing fibroblasts). , for example described in the document La Diego, (1987), n ⁇ 185 . pages 149-159 and in Br. J. Dermatol. (1986), 114. pages 91-101, or a support constituted by half excised.
• composition according to the invention Thanks to the use of the composition according to the invention, a faster and more complete epidermization will be obtained. This will allow in a shorter time to provide doctors with reconstituted skin, a kind of biological dressing for autografts, for example in the case of extensive burns.
• the invention will also allow industrial and competitive production of reconstituted skins of good quality to carry out penetration or tolerance tests.
• the invention naturally includes all the means constituting the technical equivalents of the means described as well as their various combinations.
• the invention also covers any characteristic which appears to be new with respect to any prior art, from the present description taken as a whole.

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• 1993
  • 1993-08-02 FR FR9309493A patent/FR2699081B1/fr not_active Expired - Fee Related
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