EP3765001A1 - Composition cosmétique pour le traitement d'altérations de l'hyperpigmentation de la peau - Google Patents

Composition cosmétique pour le traitement d'altérations de l'hyperpigmentation de la peau

Info

Publication number
EP3765001A1
EP3765001A1 EP19708581.4A EP19708581A EP3765001A1 EP 3765001 A1 EP3765001 A1 EP 3765001A1 EP 19708581 A EP19708581 A EP 19708581A EP 3765001 A1 EP3765001 A1 EP 3765001A1
Authority
EP
European Patent Office
Prior art keywords
weight
composition according
skin
concentration
varies
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Withdrawn
Application number
EP19708581.4A
Other languages
German (de)
English (en)
Inventor
Fabio BANFI
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Fb Dermo Srl
Original Assignee
Fb Dermo Srl
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Fb Dermo Srl filed Critical Fb Dermo Srl
Publication of EP3765001A1 publication Critical patent/EP3765001A1/fr
Withdrawn legal-status Critical Current

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • A61K31/05—Phenols
    • A61K31/055—Phenols the aromatic ring being substituted by halogen
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
    • A61K31/726—Glycosaminoglycans, i.e. mucopolysaccharides
    • 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
    • A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
    • A61K8/41—Amines
    • A61K8/411—Aromatic amines, i.e. where the amino group is directly linked to the aromatic nucleus
    • 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
    • A61K8/498—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom having 6-membered rings or their condensed derivatives, e.g. coumarin
    • 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
    • A61K8/673—Vitamin B group
    • 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
    • A61K8/9741—Pteridophyta [ferns]
    • A61K8/9749—Filicopsida or Pteridopsida
    • 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
    • A61Q19/02—Preparations for care of the skin for chemically bleaching or whitening the skin
    • F—MECHANICAL ENGINEERING; LIGHTING; HEATING; WEAPONS; BLASTING
    • F28—HEAT EXCHANGE IN GENERAL
    • F28D—HEAT-EXCHANGE APPARATUS, NOT PROVIDED FOR IN ANOTHER SUBCLASS, IN WHICH THE HEAT-EXCHANGE MEDIA DO NOT COME INTO DIRECT CONTACT
    • F28D21/00—Heat-exchange apparatus not covered by any of the groups F28D1/00 - F28D20/00
    • F28D2021/0019—Other heat exchangers for particular applications; Heat exchange systems not otherwise provided for
    • F28D2021/0035—Other heat exchangers for particular applications; Heat exchange systems not otherwise provided for for domestic or space heating, e.g. heating radiators
    • F28D2021/0036—Radiators for drying, e.g. towel radiators

Definitions

  • the present invention relates to a composition
  • a composition comprising tranexamic acid, at least one inhibitor or antagonist of the enzyme tyrosinase and at least one polyphenol source.
  • the invention also relates to the cosmetic use of the composition for the prevention and/or treatment of alterations of skin pigmentation, in particular of skin hyperpigmentation.
  • Melanocytes are highly specialized cells that have the function of protecting the epidermis from the damage of ultraviolet (UV) radiation by means of the production of melanin, through a process known as melanogenesis. Together with melanocytes, the epidermis is composed mainly of keratinocytes, which constitute up to 95% of the epidermis. During their differentiation, keratinocytes move progressively toward the more superficial layers of the skin and their nuclei are constantly exposed to high UV radiation levels. In order to protect the DNA of keratinocytes and therefore the integrity of the cells themselves, melanin is transferred from melanocytes to the surrounding keratinocytes by means of dendrites in response to exposure to UV radiation. By arranging themselves above the keratinocyte nuclei, melanin granules absorb UV radiation before it is able to reach the nucleus and damage the DNA.
  • UV radiation ultraviolet
  • Pigmentation disorders are conditions that have important aesthetic and psychological effects. When melanin production in human skin is altered, disorders such as vitiligo and melasma occur. Vitiligo is the most widespread pigmentation disorder (it affects 0.1-2% of world population) and is characterized by a loss of function of melanocytes, with consequent appearance of light patches on colored skin. Vice versa, the abnormal accumulation of melanin can lead to melasma, freckles and sun spots.
  • Skin pigmentation disorders are very frequent in all ethnic groups and cause medical problems (acceleration of the natural aging process) but most of all aesthetic and psychological problems, which affect the possibility to lead a normal life.
  • Skin pigmentation disorders are currently treated with nondefmitive methods based on invasive therapies which use laser, light or chemical peeling and on topical treatments that use creams based on active ingredients such as hydroquinone, azelaic acid, arbutin or kojic acid.
  • Hydroquinone is currently the most used and most effective active ingredient for the topical treatment of skin patches; however, it has some side effects, such as toxicity, allergic reactions, the development of skin contact dermatitis and also difficulty in preparing stable formulations.
  • active ingredients for topical use have been recently developed which have shown total or partial effectiveness in the treatment of hyperpigmentation in people of color; examples of these active ingredients are: soy extracts, licorice extracts, extracts from the leaves of Morus alba containing moracin M, 4-n-butylresorcinol, niacinamide (vitamin B3), ellagic acid, resveratrol, dioic acids and N-acetylglucosamine (Konda et al, New horizons in treating disorders of hyperpigmentation in skin of color, Sem Cutan Med and Sur, 31 : 133-139, 2012).
  • Active ingredients have also been developed recently which are effective for the treatment of hyperpigmentation of people of color and can be administered orally.
  • procyanidins tranexamic acid and extract of Polipodium Leucotomos (Konda et al., New horizons in treating disorders of hyperpigmentation in skin of color, Sem Cutan Med and Sur, 31 : 133-139, 2012).
  • a first aspect of the present invention relates to a composition
  • a composition comprising tranexamic acid, at least one inhibitor or antagonist of the enzyme tyrosinase, and at least one polyphenol source.
  • the composition also comprises vitamin B3 or a derivative thereof.
  • the invention furthermore relates to the use of the composition in the cosmetic field for the prevention and/or treatment of skin pigmentation alterations, in particular for the treatment of skin hyperpigmentation.
  • Another aspect of the present invention relates to the composition as described above for use as a remedy in the treatment and/or prevention of pathological conditions affecting the skin.
  • composition according to the invention particularly in the form of cream or serum, it is possible to improve/attenuate skin pigmentation alterations.
  • Figure 1 shows the survival of murine melanoma cells (B16) in a concentration-response curve with a positive control (SDS).
  • Figure 2 shows the production of melanin (pg/ml) by melanocytes following treatment with different compositions.
  • Figure 3 shows photographs of tissues treated with various compositions, not treated or treated with a positive control.
  • a first aspect of the present invention relates to a composition
  • a composition comprising tranexamic acid, at least one inhibitor or antagonist of the enzyme tyrosinase, and at least one polyphenol source.
  • the composition comprises tranexamic acid, at least on inhibitor/antagonist of the enzyme tyrosinase, at least one source of polyphenols and vitamin B3 or a derivative thereof.
  • the concentration of tranexamic acid varies between 0.2 and 10% by weight, preferably between 0.5 and 8% by weight.
  • the inhibitor or antagonist of the enzyme tyrosinase is chosen from trihydroxybenzoic acid glucoside, gallic acid (trihydroxybenzoic acid), catechin, epigallocatechin, epigallocatechin-3-0-gallate, methyl gentisate (methyl hydroxybenzoate), and 4-n-butylresorcinol.
  • the inhibitor or antagonist of the enzyme tyrosinase is chosen from gallic acid and trihydroxybenzoic acid glucoside.
  • the concentration of said inhibitor or antagonist of the enzyme tyrosinase varies between 0.2 and 10% by weight, preferably between 0.5 and 8% by weight.
  • the at least one polyphenol source is chosen from soy extract and Polipodium extract (i.e., a fern extract).
  • the at least one polyphenol source is an extract of Polipodium leucotomos, a particular species of fern.
  • the concentration of such at least one source of polyphenols varies between 0.05 and 5% by weight and preferably varies between 0.08 and 3% by weight.
  • composition according to the present invention may furthermore comprise at least one excipient acceptable for pharmaceutical use or for cosmetic use that is useful in the preparation of the composition and is biologically safe and non-toxic.
  • Such excipient can be at least one conditioning agent, preferably at least one skin humectant, occlusive or emollient conditioning agent.
  • such at least one skin humectant, occlusive or emollient agent is chosen among: glycerin, hyaluronic acid, capric/caprylic triglyceride, octyldodecanol, jojoba oil, macadamia oil, aspartic acid, decyl cocoate, soy oil, lactic acid, glyceryl monostearate, beeswax, glyceryl behenate, glyceryl dibehenate, tribehenin, betaine, stearic acid and combinations thereof.
  • such skin humectant, occlusive or emollient agent is chosen from: glycerin, jojoba oil, macadamia oil, capric/caprylic triglyceride, octyldodecanol, aspartic acid, glyceryl monostearate, lactic acid and combinations thereof.
  • the concentration of such conditioning agent varies preferably between 0.008 and 10% by weight, preferably between 0.05 and 6% by weight.
  • the concentration of glycerin varies between 0.5 and 4% by weight and preferably varies between 1 and 3% by weight.
  • the concentration of jojoba oil varies between 0.8 and 5% by weight and preferably varies between 1 and 4% by weight.
  • the concentration of macadamia oil varies between 0.8 and 5% by weight and preferably varies between 1 and 4% by weight.
  • the concentration of capric/caprylic triglyceride varies between 0.8 and 6% by weight and preferably varies between 1 and 4% by weight.
  • the concentration of octyldodecanol varies between 0.8 and 5% by weight and preferably varies between 1 and 4% by weight.
  • the concentration of glyceryl monostearate varies between 0.8 and 5% by weight and preferably varies between 1 and 4% by weight.
  • the concentration of lactic acid varies between 0.008 and 2% by weight and preferably varies between 0.01 and 1% by weight.
  • Such excipient can be furthermore a stabilizing agent or a surfactant.
  • Such stabilizing agent or surfactant is preferably chosen from: aluminum and magnesium silicates, potassium cetyl phosphate, cetyl stearyl alcohol, cetyl alcohol, polyglyceryl-3 dicitrate/stearate, and combinations thereof.
  • the concentration of such stabilizing agent or surfactant varies between 0.1 and 5% by weight and preferably varies between 0.3 and 3% by weight.
  • the concentration of the aluminum and magnesium silicate varies between 0.08 and 2% by weight and more preferably varies between 0.1 and 1% by weight.
  • the concentration of potassium cetyl phosphate varies between 0.1 and 2% by weight and more preferably varies between 0.2 and 1% by weight.
  • excipient can be a preservative, preferably phenoxyethanol/ethylhexylglycerin or pentylene glycol.
  • the concentration of the preservative varies between 0.5 and 5% by weight and more preferably varies between 0.75 and 3% by weight.
  • excipient can be an antioxidant, preferably chosen from: allantoin, tocopherol, tocopherol acetate, vitamin E, vitamin C, sodium lactate, and combinations thereof.
  • the concentration of such antioxidant preferably varies between 0.08 and 5% by weight and more preferably varies between 0.1 and 3% by weight.
  • composition of the present invention is prepared in a solvent, preferably in water.
  • the composition comprises tranexamic acid at a concentration comprised between 1 and 5% by weight, the at least one inhibitor or antagonist of the enzyme tyrosinase at a concentration comprised between 1 and 5% by weight, and the at least one polyphenol source at a concentration comprised between 0.1 and 1% by weight.
  • the composition comprises tranexamic acid at a concentration comprised between 1 and 5% by weight, trihydroxybenzoic acid glucoside at a concentration comprised between 1 and 5% by weight, and Polipodium leucotomos extract at a concentration comprised between 0.1 and 1% by weight.
  • the composition comprises tranexamic acid at a concentration comprised between 1 and 5% by weight, the at least one inhibitor or antagonist of the enzyme tyrosinase at a concentration comprised between 1 and 5% by weight, the at least one polyphenol source at a concentration comprised between 0.1 and 1% by weight, and vitamin D3 or a derivative thereof at a concentration comprised between 1 and 5% by weight.
  • the composition comprises tranexamic acid at a concentration comprised between 1 and 5% by weight, trihydroxybenzoic acid glucoside at a concentration comprised between 1 and 5% by weight, Polipodium leucotomos extract at a concentration comprised between 0.1 and 1% by weight, and niacinamide at a concentration comprised between 1 and 5% by weight.
  • a further aspect of the present invention relates to the composition according to the invention, formulated preferably for topical use as a cream, cream-gel, gel, serum, oil, emulsion, emulsion-gel (emulgel), ointment, spray or stick (such as lip balm).
  • a further aspect of the present invention relates to the cosmetic use of the composition for preventing and/or attenuating skin pigmentation defects, more preferably skin hyperpigmentation defects, such as for example melasma (skin patches), freckles and sun spots.
  • a further aspect of the present invention relates to the composition as described above for use as a remedy.
  • a further aspect of the present invention relates to the composition as described above for use in the treatment and/or prevention of pathological conditions affecting the skin, preferably to prevent and/or treat pigmentation defects, more preferably skin hyperpigmentation defects, such as for example melasma, freckles and sun spots.
  • pigmentation defects more preferably skin hyperpigmentation defects, such as for example melasma, freckles and sun spots.
  • composition according to the invention is capable of improving/attenuating alterations of skin pigmentation with a surprising effect.
  • the composition according to the invention in fact comprises compounds which act on various pathways that lead to the forming of skin patches.
  • tranexamic acid used in therapy as an anti-hemorrhagic, acts on plasmin activation and is capable of also inhibiting melanocyte activation. Tranexamic acid therefore inhibits the mechanisms that lead the melanocyte to synthesize melanin.
  • the tyrosinase inhibitor or antagonist is capable of interfering with the activity of the main enzyme involved in melanin biosynthesis.
  • Vitamin B3 or a derivative thereof acts by inhibiting the transport of melanin in the upper layers of the skin.
  • the at least one polyphenol source has an antioxidant and photoprotective effect, thus reducing the stimulus to produce melanin.
  • the MTT assay was performed in order to assess the potential cytotoxic effect of the composition on a cell line of B16 melanocytes.
  • the test was conducted on murine melanoma cells (B16), a well- known line commonly used in melanogenesis studies.
  • the cells were cultured in DMEM (Dulbecco's modified Eagle medium), containing 2 mM glutamine, 10% fetal bovine serum (FBS) and 1% antibiotics (penicillin and streptomycin) and incubated in standard culture conditions (37°C, 5% CO2). Good cell culture practice was applied.
  • DMEM Dynabecco's modified Eagle medium
  • FBS fetal bovine serum
  • antibiotics penicillin and streptomycin
  • composition being considered was dissolved and then diluted in culture medium to the desired final concentrations, comprised between 0.0391 and 5.0 mg/ml.
  • the negative reference (internal standard) was tested at concentrations comprised between 0.0391 and 5.0 mg/ml, while the positive control (SDS) was tested at concentrations comprised between 0.00313 and 0.4 mg/ml.
  • ODX Average optical density of the cells treated with the sample being considered at concentration X;
  • ODNC Average optical density of the negative controls.
  • IC50 is a parameter that allows to assess the cytotoxicity of a compound according to Table 1 :
  • the tested concentrations comprised between 0.1 and 0.4 mg/ml decreased cell viability significantly.
  • a value of IC50 ⁇ 0,5 mg/ml indicates a cytotoxic effect.
  • Table 2 The same results of Table 2 are shown in the chart in Figure 1.
  • the tested concentrations did not decrease cell viability.
  • a value of IC50 > 0.5 mg/ml indicates absence of cytotoxic effect.
  • the purpose of the test is to assess whether the tested product has a depigmenting activity in vitro on reconstructed human tissues by assessing melanin synthesis. It is deemed that this capacity renders the product a potential "depigmenting" candidate in vivo, potentially capable of reducing patches caused by skin hyperpigmentation.
  • the reconstructed tissues are formed by normal keratinocytes (NHEK) and human melanocytes (NHM) cultured to form a multilayer and highly differentiated model of human epidermis.
  • NHEK normal keratinocytes
  • NHS human melanocytes
  • the melanocytes inside the co-cultures undergo melanogenesis, which leads to tissue pigmentation.
  • the present system provides a useful in vitro instrument for assessing cosmetic and pharmaceutical agents designed to modulate skin pigmentation.
  • the tissues were then removed from the insert by cutting the filter with a scalpel. Each filter was immersed in 360 m ⁇ of Solvable and heated at 100°C for 45 minutes. Optical density was measured on 80 m ⁇ of extract at
  • an MTT test was conducted. For each condition, two tissues were placed in 300 m ⁇ of MTT and incubated for 3 hours at 37°C, 5% CO2. Extraction was performed in 1.5 ml of isopropanol at room temperature, for a minimum of 2 hours. Optical density is measured at 570 nm.
  • Absorbance measured at 490 nm is directly proportional to the quantity of melanin extracted from the tissues.
  • the values were interpolated with a synthetic melanin standard curve in order to obtain the melanin content (pg/ml) of each tissue.
  • the chart expresses the percentage content of melanin with respect to the untreated negative control.
  • This test allows to assess the tolerability of the composition according to the present invention by identifying and classifying the irritation power.
  • the test is conducted on ambulatory volunteers according to the following inclusion criteria:
  • samples were applied, as a function of their characteristics of use: as is or at a standard concentration of 10%.
  • 20 m ⁇ are applied to the skin; 20 pg are applied for solid/semisolid products.
  • the device used to perform an occlusion patch test is the Finn
  • Chamber a patch containing an aluminum disc with a diameter of 7 mm and absorbent paper discs.
  • the Finn Chamber contains absorbent paper discs impregnated with a known quantity (20 m ⁇ ) of sample being considered, in the case of solid products the product to be tested is in direct contact with the skin.
  • the total skin irritation index (IIM tot) is calculated by averaging the irritation indices for erythemas (IIM Er) and edemas (IIM Ed) after 24 hours.
  • Table 7 Classification of the average irritation index (according to amended Draize)
  • composition according to the present invention is not irritant.
  • the method for preparing the cream comprises the steps of:
  • phase B - keeping under agitation up to complete dissolution of phase B.
  • Samples of the depigmentation cream were applied on skin area affected by discoloration twice per day for 84 consecutive days by massaging gently until absorbed, using the amount to cover the discoloration.
  • the melanin is measured by two wavelengths. These wavelengths have been chosen in order to achieve different absorption rates by the melanin pigments. The achieved results are shown on digital displays on a scale from 0-999.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Birds (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Dermatology (AREA)
  • Molecular Biology (AREA)
  • Biotechnology (AREA)
  • Botany (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Emergency Medicine (AREA)
  • Cosmetics (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

L'invention concerne une composition comprenant de l'acide tranexamique, au moins un inhibiteur ou un antagoniste de l'enzyme tyrosinase, et au moins une source de polyphénols. L'invention concerne également l'utilisation cosmétique de la composition pour la prévention et/ou le traitement d'altérations de la pigmentation de la peau, en particulier de l'hyperpigmentation de la peau.
EP19708581.4A 2018-03-12 2019-03-11 Composition cosmétique pour le traitement d'altérations de l'hyperpigmentation de la peau Withdrawn EP3765001A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IT102018000003428A IT201800003428A1 (it) 2018-03-12 2018-03-12 Composizione cosmetica per il trattamento di alterazioni della iperpigmentazione della pelle
PCT/EP2019/056055 WO2019175120A1 (fr) 2018-03-12 2019-03-11 Composition cosmétique pour le traitement d'altérations de l'hyperpigmentation de la peau

Publications (1)

Publication Number Publication Date
EP3765001A1 true EP3765001A1 (fr) 2021-01-20

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EP19708581.4A Withdrawn EP3765001A1 (fr) 2018-03-12 2019-03-11 Composition cosmétique pour le traitement d'altérations de l'hyperpigmentation de la peau

Country Status (3)

Country Link
EP (1) EP3765001A1 (fr)
IT (1) IT201800003428A1 (fr)
WO (1) WO2019175120A1 (fr)

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CA3158316A1 (fr) * 2019-10-16 2021-04-22 Curology, Inc. Compositions et methodes de traitement de l'acne et du photovieillissement
CN119033659B (zh) * 2024-08-29 2025-07-04 澳思美日用化工（广州）有限公司 一种适用于敏感肌的美白组合物、用途和化妆品

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Publication number Priority date Publication date Assignee Title
EP2260831A1 (fr) * 2009-06-12 2010-12-15 L V M H Recherche Extraits de plantes à modulation Myo-X à utiliser dans des compositions
WO2010083368A2 (fr) * 2009-01-16 2010-07-22 Neocutis Sa Compositions de séquestration du calcium et procédés de traitement des troubles et des affections de la pigmentation de la peau
FR2953408B1 (fr) * 2009-12-08 2013-02-08 Oreal Microorganismes probiotiques a titre d'actif pour l'eclat du teint de la peau
US9364689B2 (en) * 2009-12-22 2016-06-14 Avon Products, Inc. Cosmetic compositions comprising fibrous pigments

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