WO2013093880A1 - Utilisation de stéviol, d'un dérivé glycoside de stéviol, ou d'un de leurs isomères, pour prévenir, réduire et/ou traiter une altération du teint de la peau - Google Patents

Utilisation de stéviol, d'un dérivé glycoside de stéviol, ou d'un de leurs isomères, pour prévenir, réduire et/ou traiter une altération du teint de la peau Download PDF

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Publication number
WO2013093880A1
WO2013093880A1 PCT/IB2012/057613 IB2012057613W WO2013093880A1 WO 2013093880 A1 WO2013093880 A1 WO 2013093880A1 IB 2012057613 W IB2012057613 W IB 2012057613W WO 2013093880 A1 WO2013093880 A1 WO 2013093880A1
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Prior art keywords
skin
steviol
complexion
isomers
glycoside derivative
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PCT/IB2012/057613
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English (en)
Inventor
Julien Laboureau
Myrian Kauffmann
Francine Baldo
Yann Mahe
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L'oreal
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Publication of WO2013093880A1 publication Critical patent/WO2013093880A1/fr

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/60Sugars; Derivatives thereof
    • A61K8/602Glycosides, e.g. rutin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97Cosmetics 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
    • A61K8/9783Angiosperms [Magnoliophyta]
    • A61K8/9789Magnoliopsida [dicotyledons]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q1/00Make-up preparations; Body powders; Preparations for removing make-up
    • A61Q1/12Face or body powders for grooming, adorning or absorbing
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/007Preparations for dry skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/02Preparations for care of the skin for chemically bleaching or whitening the skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/74Biological properties of particular ingredients
    • A61K2800/78Enzyme modulators, e.g. Enzyme agonists
    • A61K2800/782Enzyme inhibitors; Enzyme antagonists
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/80Process related aspects concerning the preparation of the cosmetic composition or the storage or application thereof
    • A61K2800/87Application Devices; Containers; Packaging
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/80Process related aspects concerning the preparation of the cosmetic composition or the storage or application thereof
    • A61K2800/88Two- or multipart kits

Definitions

  • the invention relates to the field of cosmetic active agents and more particularly active agents devoted to acting with regard to the melanocytes and the complexion of the skin and/or semi-mucous membranes.
  • Human skin consists of several compartments, three of which cover the whole of the body, namely a superficial compartment, which is the epidermis, the dermis and a deep compartment, which is the hypodermis.
  • the epidermis is a keratinized stratified pavement epithelium. In some regions, such as the lips, it is less keratinized and brings about the transition with the buccal mucous membrane (the term “semimucous membrane” is used). It is composed mainly of keratinocytes but also of other cells, in particular melanocytes. These cells are located in a basal membrane which separates them from the dermis. The dermis is a connective tissue. The keratinocytes differentiate on migrating from the basal membrane toward the surface of the epidermis, where they desquamate. The melanocytes are specialized dendritic cells, the function of which is to synthezise melanin. The latter is composed of two pigments, pheomelanins and eumelanins, the pheomelanins being red-yellow pigments and the eumelanins being brown-black pigments.
  • the dermis is a connective tissue composed of collagen fibers and elastin fibers, and also of glycosaminoglycans, proteoglycans and fibroblasts. Its architecture results from the arrangement and the interactions between the constituents of the extracellular matrix and the fibroblasts, which carry out the synthesis thereof and the degradation thereof.
  • the other cellular constituents are involved in the immune system (macrophages and mastocytes, Langerhans' cells), vascular system (endothelial cells), nervous system or neurosensory system.
  • the dermis is subdivided into two layers, the papillary layer and the reticular layer. The dermis makes up the main bulk of the skin.
  • hypodermis the deepest compartment and which can be the thickest compartment of the skin, invaginates into the dermis and is attached to the overlying dermis via collagen and elastin fibers. It is essentially composed of a type of cell which is specialized in the accumulation and storage of fats, the adipocytes.
  • the skin tissue also comprises sweat glands, pilosebaceous follicles, body hair, head hair or nails.
  • the skin is subjected to numerous modifications and types of damage which are reflected, at the tissue level, by disruption of the architecture of the epidermis, of the dermal-epidermal junction of the dermis and also of the blood irrigation and innervation systems, and a slowing down of or imbalance in various types of cell metabolism, such as those involved in the equilibrium of the barrier function or involved in melanogenesis.
  • aging is reflected by a detrimental change in the physiology or metabolism of the main cell types, such as the fibroblasts of the dermis, keratinocytes of the epidermis, and also melanocytes.
  • a subject matter of the invention is the cosmetic use of steviol, of a steviol glycoside derivative or of one of their isomers to stimulate, restore or regulate the metabolism of melanocytes of the skin and/or semimucous membranes.
  • metabolic is intended to denote, within the meaning of the present invention, the group of molecular and energy transformations which take place in a living cell and which contribute to its homeostasis, that is to say its maintenance of biological activity and of physiological balance.
  • the present invention relates to the cosmetic use of steviol, of a steviol glycoside derivative or of one of their isomers to reduce the melanin synthesis.
  • the present invention also relates to the cosmetic use of steviol, of a steviol glycoside derivative or of one of their isomers to prevent, reduce and/or treat a detrimental change in the complexion of the skin or in the complexion of the semimucous membranes.
  • the present invention relates to the cosmetic use of steviol, of a steviol glycoside derivative or of one of their isomers to for decreasing pigmentation of the skin and/or promoting depigmentation of the skin.
  • the present invention relates to the cosmetic use of steviol, of a steviol glycoside derivative or of one of their isomers to prevent, reduce and/or treat a defect of pigmentation of the skin.
  • the present invention relates to the cosmetic use of steviol, of a steviol glycoside derivative or of one of their isomers to lighten the skin.
  • the term "to prevent” is understood to mean the fact of reducing, at least in part, the risk of the appearance of a given phenomenon, i.e., in the present invention, a detrimental change in the metabolism of the melanocytes, in particular of elderly melanocytes, or a detrimental change in the complexion of the skin or in the complexion of the semimucous membranes.
  • steviol and in particular a steviol glycoside derivative proves to be particularly advantageous in regulating the metabolism of melanocytes and in particular melanogenesis.
  • rebaudioside A proves to be particularly effective in promoting the depigmentation of melanocytes.
  • rebaudioside A might be a molecule of interest in regulating glycemia or the metabolism of the cells of the pancreas and treating diabetes (Abudula et al, Metabolism, 2004, 53, 1378 ; WO 02/060419), in improving cognitive functions (WO 2009/071277) or in treating cardiovascular diseases (WO 2008/134828).
  • WO 07/094312 proposes the use of steviosides to promote the penetration of vitamin C into cells.
  • the present invention is targeted at steviol, a steviol glycoside derivative or one of their isomers as agent for stimulating, restoring or regulating the metabolism of the melanocytes of the skin and/or semimucous membranes.
  • steviol a steviol glycoside derivative or one of their isomers as agent for preventing, reducing and/or treating a detrimental change in the complexion of the skin or in the complexion of the semimucous membranes.
  • the present invention relates to a cosmetic or dermatological composition
  • a cosmetic or dermatological composition comprising an effective amount of steviol, of a steviol glycoside derivative or of one of their isomers, in particular as defined below, in combination with at least one additional active agent chosen from polyols, vitamins, keratolytic and/or desquamating agents, soothing agents and their mixtures.
  • the present invention relates to a kit comprising at least one container containing a composition comprising steviol, a steviol glycoside derivative or one of their isomers and at least one device arranged in order to make possible the administration of said composition to an individual, and/or to increase the effectiveness of said composition for an individual, and/or to promote the topical penetration for an individual of said composition.
  • the present invention relates to a cosmetic method for stimulating, restoring or regulating the metabolism of the melanocytes, in particular elderly melanocytes, of the skin or semimucous membranes, comprising at least one stage of administration, to an individual having need thereof, of steviol, of steviol glycoside derivative or of one of their isomers.
  • a cosmetic method for lightening the skin comprising at least one stage of administration, to an individual having need thereof, of steviol, of steviol glycoside derivative or of one of their isomers.
  • the present invention relates to a cosmetic method for preventing, reducing and/or treating a detrimental change in the complexion of the skin, comprising at least one stage of administration, to an individual having need thereof, of steviol, of steviol glycoside derivative or of one of their isomers.
  • the favoured administration route is the topical route, that is to say the application of the active agent considered according to the present invention directly in contact with the target surface of the skin or of a semimucous membrane.
  • the present invention provides a novel cosmetic active agent which is particularly effective in regulating melanogenesis, in particular on the skin and semimucous membranes.
  • the present invention provides a novel cosmetic active agent of natural origin and thus makes it possible to respond to an increasing demand from consumers in this direction.
  • the present invention relates to the use of an active agent chosen from a steviol, a steviol glycoside derivative or one of their isomers.
  • Steviol is the common precursor of the steviol glycosides.
  • precursor is understood to mean, within the meaning of the present invention, any compound participating in a reaction which produces one or more other compounds.
  • steviol glycoside derivative is understood to mean any compound represented by the formula (II):
  • Rl and R2 respectively positioned on carbons C19 and C 13 of the formula (II), represent, independently of one another, a hydrogen atom or a cyclized or noncyclized, linear or branched, sugar residue.
  • Rl and R2 are other than hydrogen.
  • Rl and R2 which are identical or different and preferably different, represent a sugar residue composed of one or more glucose and/or rhamnose entities.
  • Glu just one sugar entity, in particular glucose, referred to as Glu
  • a sequence of two sugars such as a diholoside, for example a sequence of two glucose entities, or
  • a sequence of three sugar units such as a linear or branched and preferably branched triholoside, for example a branched radical formed of three glucose units and a branched radical formed of a glucose entity substituted by a glucose entity and a rhamnose entity.
  • Rl represents a glucose entity
  • Rl represents a glucose unit and R2 represents a branched triholoside.
  • Rl represents a glucose unit and R2 represents a branched triholoside.
  • a steviol glycoside derivative according to the invention can be chosen from stevioside, rebaudioside A, rebaudioside C (or dulcoside B), dulcoside A, rebaudioside B, rebaudioside D, rebaudioside E, rebaudioside F, steviolbioside, rubusoside, and their mixtures.
  • a steviol glycoside derivative according to the invention is chosen from stevioside, rebaudioside A, rebaudioside C (or dulcoside B), dulcoside A, and their mixtures.
  • a steviol glycoside derivative according to the invention is rebaudioside A.
  • isomers according to the invention are stereoisomers, in particular enantiomers, diastereomers, and mixtures thereof, including racemic mixtures. Mention may in particular be made, as isomer according to the invention, of isosteviol, represented by the formula (III) below:
  • the present invention naturally employs an effective amount of steviol, steviol glycoside derivative or isomers of these, so as to obtain the desired effect.
  • This effective amount can vary with regard to various parameters which are in particular the indication targeted, the characteristics of the individual treated, the pharmaceutical dosage formulation adopted, the nature of the formulation excipients or the presence of additional active agent(s).
  • the term "effective amount” is understood to mean a sufficient and necessary amount of a given active agent to exert the desired effect and in particular to regulate melanogenesis.
  • Such an amount can be determined by any method known to a person skilled in the art, for example by means of in vitro, ex vivo or in vivo trials, such as clinical trials.
  • steviol In order to give an order of magnitude, steviol, a steviol glycoside derivative or an isomer of these can be used in a composition in a proportion of 0.01 to 50% by weight, preferably from 0.05 to 30% by weight, in particular from 0.1 to 10% by weight and more preferably from 0.5 to 5% by weight, with respect to the total weight of the composition in which it is present.
  • a main active agent according to the invention that is to say steviol, a steviol glycoside derivative or one of their isomers, is employed in the form of an extract of at least one plant of the Stevia genus.
  • the use of the main active agent according to the invention in the form of an extract of at least one plant of the Stevia genus is particularly advantageous in that it makes it possible to provide a novel cosmetic active agent of natural origin and thus to meet an increasing demand from consumers in this direction.
  • the Stevia genus belongs to the family of the Asteraceae, which brings together from 150 to 200 species of shrubs or aromatic herbs, some of which comprise natural sweeteners.
  • the Stevia plants are plants originating from the tropical regions of Latin America.
  • the extract of a plant from the Stevia genus can be chemically modified (it is then semisynthetic), but it is preferably a native extract.
  • An extract of a plant of the Stevia genus within the meaning of the present invention, can be prepared from any plant material resulting from said plant or from its cells cultivated according to conventional methods or by biotechnology in vivo or resulting from culturing in vitro.
  • cultivating in vivo is understood to mean any cultivation of conventional type, that is to say in soil in the open air or in a greenhouse, or alternatively without soil.
  • the term "culturing in vitro" is understood to mean all the techniques known to those skilled in the art which make it possible to artificially obtain a plant or a plant part.
  • the selection pressure imposed by the physicochemical conditions during the growth of plant cells in vitro makes it possible to obtain a standardized plant material which is available throughout the year, in contrast to plants cultivated in vivo.
  • An extract of a plant of the Stevia genus employed in the present invention can be obtained from any plant material resulting from this whole plant or from any part of this plant, such as, for example, the leaves, stems, flowers and flowering tops, seeds, buds and roots, undifferentiated cells or plant stem cells.
  • an extract of a plant of the Stevia genus in accordance with the invention is obtained from the leaves.
  • an extract of a plant of the Stevia genus in accordance with the invention originates from a plant of the species Stevia rebaudiana (Bertoni), also known as Eupatorium rebaudianum or "sweet leaf .
  • Such a species is today cultivated in many countries and on other continents than Latin America, in particular in Singapore, Taiwan, Malaysia, South Korea, China, Israel or even Australia.
  • an extract of a plant of the Stevia genus according to the present invention is a native extract.
  • native intends to mean an extract that is not modified after the extraction process, especially by fermentation or by chemical synthesis.
  • an extract of a plant of the Stevia genus according to the present invention is not a fermented extract.
  • an extract of a plant of the Stevia genus according to the present invention is employed in a composition in a proportion of from 0.00001% to 50% by weight, preferably from 0.0001% to 10% by weight and better still from 0.01% to 4% by weight, with respect to the total weight of said composition.
  • rebaudioside A which can be used in the present invention, of the Stevia extract comprising 99% of rebaudioside A sold by Blue California under the name Good'n sweetTM as well as the Stevia extract comprising 97% of rebaudioside A sold by Chengdu Wagott Pharmaceutical under the name ViaSweetTM.
  • Stevia extract fermented by a yeast described in the document WO2003/035090.
  • a main active agent according to the invention that is to say a steviol, a steviol glycoside derivative or one of their isomers, are such that they allow the use, within a composition according to the invention, of compounds or active agents which normally cannot be used on account of being difficult to formulate, dissolve, deliver in a controlled fashion or vectorize.
  • an extract according to the invention can advantageously be combined with at least one additional active agent chosen from polyols, in particular glycerol and propylene glycol, vitamins, keratolytic and/or desquamating agents, soothing agents and their mixtures.
  • additional active agent chosen from polyols, in particular glycerol and propylene glycol, vitamins, keratolytic and/or desquamating agents, soothing agents and their mixtures.
  • the term "desquamating agent” is understood in particular to mean the compounds capable of influencing the desquamation by promoting exfoliation, such as ⁇ - hydroxy acids, in particular salicylic acid and its derivatives (including 5-(n- octanoyl)salicylic acid); a-hydroxy acids, such as glycolic, citric, lactic, tartaric, malic or mandelic acid; urea; gentisic acid; ohgofucoses; cinnamic acid; Saphora japonica extract and resveratrol.
  • the choice and the content of these additional active agents depend in particular on the administration route under consideration, which falls within the competence of a person skilled in the art.
  • additional active agents can be present in a composition according to the invention in a content ranging from 0.001% to 50% by weight, preferably from 0.01% to 10% by weight and more preferably from 0.01% to 5% by weight, with respect to the total weight of the composition in which they are present.
  • Imbalances in the metabolism of the melanocytes can be the cause of various esthetic disorders of the skin. These disorders can affect the complexion and/or the pigmentation of the skin and furthermore occur in an exacerbated fashion in aged skin.
  • defects in pigmentation of the skin are frequent and can occur in a variety of different forms.
  • the defects in skin pigmentation with which the invention is concerned can be defined as involving the appearance of at least one skin region having a darker or lighter color than the average color of the skin surface of the individual examined. This region can be macroscopic or microscopic in size.
  • defects in pigmentation of the skin is understood to mean any event of appearance of a change in the color or in the complexion of all or part of the surface of the skin, which encompasses an overall or local change in the complexion of the skin, and also hyperpigmentation, hypopigmentation or dyspigmentation defects.
  • hypopigmentation defect of the skin is understood to mean any event of appearance of a skin region affected by an excess of pigmentation, in comparison with the average level of pigmentation of the skin surface of an individual.
  • the level of pigmentation of a skin surface can be measured using any appropriate type of color-analysing device, for example with an appropriate spectrocolorimetry device, or else a reflectometer device, which are well known in the art.
  • the level of pigmentation of a skin surface is measured using an appropriate standard color chart.
  • the standard color chart is applied to the skin so that at least one edge of said chart is placed beside the skin region to be measured.
  • the value of degree of color on the chart which is the closest to the color of the skin region which is analysed is recorded by visual comparison.
  • the defects of pigmentation of the skin can be marked by the presence of more or less extensive surface skin blemishes, having a darker or lighter color than the normal color of the skin of the individual which surrounds said skin blemishes.
  • the defects of pigmentation of the skin encompass in particular melasma and lentigines, including liver spots and actinic lentigo.
  • Melasma (also known as chloasma) is most frequently encountered in pregnant women and in women taking anti-ovulatory medicaments. Melasma is also known as "mask of pregnancy”. Melasma appears as a broad dark reticular macula with uneven edges which is found mainly on the cheeks, upper lip and forehead. Melasma is also encountered in men or women not suffering from detectable endocrinal imbalance, but exposure to the sun is necessary for its development.
  • the melasma or chloasma considered by the invention can be triggered by exposure to UV rays, or can occur on photosensitive skin, photoallergic skin or skin subject to a phototoxicity reaction.
  • Lentigines arise in the form of hyperpigmented skin blemishes which can appear at any age and are usually darker and more extensive than freckles.
  • a lentigo is characterized in particular by an increase in the number of melanocytes in the basal layer.
  • Lentigines encompass in particular (i) solar lentigines, which appear in light-skinned individuals on skin regions exposed for a long time to the sun, (ii) lentiginous pigmentation resulting from skin therapies involving UV-A radiation (320-400 nanometers - also known as PUVA therapy), (iii) multiple lentigines, especially on the palms, soles of the feet, mucous membranes or unexposed skin, or also (iv) lentigines affecting the lips, vulva or penis. Defects of pigmentation of the skin also encompass hyperpigmentation situations resulting from inflammation or scarring. Postinflammatory hyperpigmentation is quite independent of the degree of inflammation and depends more on the nature of the trauma which brought about the inflammation.
  • Postinflammatory hyperpigmentation can be severe after certain lesions, such as thermal burns or of acne type, or resulting from insect stings, cuts and other mechanical traumas of the skin, in particular during shaving, and pseudo folliculitis due to body hairs becoming ingrown as a result of shaving or depilation. Postinflammatory hyperpigmentation can persist for months, indeed even for years.
  • the defects of pigmentation of the skin targeted by the invention also concern the dyspigmentations resulting from a dys functioning of the metabolism of the melanocytes of the skin. Mention may be made, as examples of dyspigmentations targeted by the invention, of vitiligo, pityriasis versicolor or depigmentations due to burns or to surgery, the aftereffects of spots due to acne, and postshaving cuts.
  • a defect of pigmentation of the skin more particularly considered by the invention can be chosen from melasma, chloasma, lentigines, liver spots, vitiligo, postinflammatory hyperpigmentations due to an abrasion and/or a burn and/or a scar, genetically-determined hyperpigmentations, hyperpigmentations of metabolic or drug origin, or any other pigmentation lesions.
  • the present invention can also be employed to prevent, reduce and/or treat the mask of pregnancy.
  • An active agent of the invention can more particularly be employed to lighten or whiten the skin.
  • the present invention also relates to esthetic disorders of the skin affecting the complexion of the skin.
  • the invention may suitably be employed to prevent, reduce and/or treat a lack of uniformity in the complexion of the skin, indeed even to improve the complexion of the skin, in particular of aged skin.
  • the invention advantageously makes it possible to promote and maintain the radiance of the complexion of the skin and in particular a uniform complexion.
  • a use according to the invention can make it possible to treat and/or prevent a detrimental change in the radiance of the complexion or a loss in the radiance of the complexion of the skin.
  • a use according to the invention can make it possible to confer, on the skin, a uniform, luminous, more radiant, indeed even more glowing, complexion indicative of skin in good health.
  • the invention advantageously makes it possible to prevent, reduce and/or treat a muddy skin complexion, a lifeless skin complexion, a nonuniform skin complexion or imperfections of the skin chosen in particular from spots, dry patches, dyschromias or blackheads or also to prevent, reduce and/or treat a waxen, sallow, grayish or ashen, indeed even sickly, complexion.
  • Steviol a steviol glycoside derivative or an isomer of these can more preferably be employed to prevent, reduce and/or treat a detrimental change in the complexion of the skin chosen from a detrimental change in the radiance of the complexion of the skin, a muddy skin complexion, a lifeless skin complexion, a nonuniform skin complexion, spots, dry patches, dyschromias and/or blackheads.
  • the present invention can relate more particularly to aged skin.
  • indications subject-matter of the uses according to the invention are indications not involving the production and/or release of stem cell factor (SCF).
  • SCF stem cell factor
  • the present invention relates to the entire surface of the skin of an individual.
  • the present invention can be employed with regard to the skin regions more regularly exposed to the sun, to UV radiation or to external stress factors, such as pollution, irritation due to rubbing, or cigarette smoke.
  • the present invention can advantageously be employed with regard to the skin of the hands, face or neckline.
  • the active agent according to the invention namely steviol, steviol glycoside derivative or one of their isomers, as or not as a mixture with other additional active agent(s), can be formulated in a cosmetic or dermatological composition.
  • a composition of the invention is a cosmetic composition.
  • the main active agent according to the invention is intended for topical administration.
  • compositions comprising the main active agent according to the invention can be in the form of products for caring for the skin or semimucous membranes, such as a protective, treatment or care composition for the face, for the lips, for the hands, for the feet, for the anatomical folds or for the body (for example, day cream, night cream, make-up-removing cream, make-up base, antisun composition, protective or care body milk, aftersun milk, lotion, gel or foam for the care of the skin or scalp, serum, powder, mask, artificial tanning composition, aftershave composition, hair composition, product for the region of the armpits, or hygiene and cleaning product.
  • a protective, treatment or care composition for the face, for the lips, for the hands, for the feet, for the anatomical folds or for the body (for example, day cream, night cream, make-up-removing cream, make-up base, antisun composition, protective or care body milk, aftersun milk, lotion, gel or foam for the care of the skin or scalp, serum, powder, mask, artificial tannin
  • the main active agent according to the invention is intended for oral administration.
  • composition of the invention can be provided in any suitable form, particularly in the form of a solution to be taken orally, a drink, a tablet, a capsule, including a hard gelatin capsule, a nutritional food or a nutritional supplement.
  • the main active agent according to the invention is intended for intracutaneous administration, such as intradermal or subcutaneous administration.
  • This administration can, for example, be carried out by means of a device which makes possible intracutaneous injection (syringe, implant or reservoir and microneedles) or alternatively by means of an ultrasound or iontophoresis device, indeed even a light or thermal device.
  • Such an administration can also be carried out by mesotherapy.
  • the intracutaneous use of a composition of the invention is to be distinguished from a surgical operation and is targeted only at exerting a surface treatment of the skin for esthetic, protective, repair or comfort purposes.
  • the intracutaneous administration route in the present invention is expressed only by superficial penetration of the skin and thus does not come within any medical, surgical or therapeutic context.
  • a main active agent according to the invention is intended for topical administration, that is to say, for administration by application at the surface of the keratinous substance under consideration.
  • a main active agent in accordance with the invention when it is present in a composition, can be formulated in a physiologically acceptable medium.
  • physiologically acceptable medium is intended to denote a medium suitable for the topical, oral or intracutaneous, such as intraepidermal, intradermal or subcutaneous, administration of a composition.
  • a physiologically acceptable medium is preferably a cosmetically or dermato logically acceptable medium, that is to say a medium which is devoid of unpleasant odor or appearance and which is entirely compatible with the administration route under consideration.
  • composition When the composition is intended for topical administration, that is to say for administration by application at the surface of the keratinous substance under consideration, such a medium is considered to be physiologically acceptable when it does not cause stinging, tightness or redness unacceptable to the user.
  • composition When the composition is intended for oral administration, such a medium is considered to be physiologically acceptable when it does not cause digestive intolerance.
  • compositions intended for intracutaneous administration such a medium is considered to be physiologically acceptable when it does not cause a reaction experienced as unpleasant by the user, for example stinging, tightness or redness, indeed even does not cause inflammatory, allergic, edematous or pruritic reactions.
  • composition according to the invention can be provided in any formulation form normally used in cosmetics and dermatology.
  • aqueous solution aqueous/alcoholic solution or oily solution, which is optionally gelled, of a dispersion of the lotion type, which is optionally a two-phase or three-phase lotion, of an oil-in-water or water-in-oil or multiple emulsion, of an aqueous gel, of a dispersion of oils in an aqueous phase, in particular using spherules, it being possible for these spherules to be polymer particles or, better still, lipid vesicles of ionic and/or nonionic type, or alternatively in the form of a powder, of a serum, of a paste, of a solid cake which can disintegrate by rubbing an applicator or of a soft or rigid stick which can melt on the skin or semimucous membranes. It can have a solid, pasty or more or less fluid liquid consistency.
  • the active agent according to the invention can be formulated with the usual constituents. Mention may in particular be made, by way of illustration and without implied limitation of these normal components, of water, volatile or nonvolatile oils, in particular as described in detail below, waxes, pigments, fillers, surfactants, gelling agents, preservatives, coloring materials, antioxidants, UV screening agents and their mixtures.
  • a composition according to the invention can advantageously be provided in the form of an emulsion, obtained in particular by dispersion of an aqueous phase in a fatty phase (W/O) or of a fatty phase in an aqueous phase (O/W), of liquid or semi-liquid consistency of the milk type, or of soft, semi-solid or solid consistency of the cream or gel type, or alternatively of a multiple emulsion (W/O/W or 0/W/O).
  • W/O a fatty phase
  • O/W a fatty phase
  • composition according to the invention can advantageously comprise from 0.1% to 99.9% by weight and preferably from 30% to 95% by weight of water, with respect to the total weight of said composition.
  • a composition according to the invention can also advantageously comprise at least one fatty phase which is liquid at ambient temperature and atmospheric pressure.
  • the amount of oily phase present in the compositions according to the invention can range, for example, from 0.01% to 50% by weight and preferably from 0.1% to 30%) by weight, with respect to the total weight of the composition.
  • oils which can be used in the composition according to the invention of hydrocarbon oils of animal origin, hydrocarbon oils of vegetable origin, synthetic esters and ethers, in particular of fatty acids, linear or branched hydrocarbons of mineral or synthetic origin, fatty alcohols and silicone oils and their mixtures.
  • fatty substances which can be present in the oily phase are, for example, waxes and fatty acids comprising from 8 to 30 carbon atoms, such as stearic acid, lauric acid, palmitic acid and oleic acid. These fatty substances can be chosen in a manner varied by a person skilled in the art in order to prepare a composition having the desired properties, for example of consistency or texture.
  • composition according to the invention can additionally comprise at least one coloring material chosen, for example, from pigments, pearlescent agents, dyes, effect materials and their mixtures.
  • coloring materials can be present in a content ranging from 0.01% to 50%) by weight and preferably from 0.01% to 30%> by weight, with respect to the total weight of the composition.
  • a composition according to the invention can additionally comprise at least one filler, in particular in a content ranging from 0.01% to 50% by weight and preferably ranging from 0.01% to 30% by weight, with respect to the total weight of the composition.
  • fillers can be inorganic or organic and their choice comes within the competence of a person skilled in the art.
  • the administration of the active agent under consideration according to the invention can be carried out via the use of a device adjusted to the method of administration under consideration, that is to say topical, oral or intracutaneous.
  • a device adjusted to the method of administration under consideration that is to say topical, oral or intracutaneous.
  • - devices for direct topical delivery or for delivery by means of a specific applicator such as, for example, intracutaneous microinjections, or simple or iontophoretic patches;
  • the device contributes to stimulating the effectiveness of the active agent according to the invention at the administration site under consideration.
  • kits comprising at least one container containing a composition comprising steviol, a steviol glycoside derivative or one of their isomers and at least one device appropriate for the administration of said composition to an individual, in particular as described above.
  • the present invention relates to a cosmetic method for stimulating, restoring or regulating the metabolism of melanocytes, in particular elderly melanocytes, of the skin or semimucous membranes, comprising at least one stage of administration, to an individual having need thereof, of steviol, of steviol glycoside derivative or of one of their isomers.
  • a cosmetic method for lightening the skin comprising at least one stage of administration, to an individual having need thereof, of steviol, of steviol glycoside derivative or of one of their isomers.
  • the present invention relates to a cosmetic method for preventing, reducing and/or treating a detrimental change in the complexion of the skin, comprising at least one stage of administration, to an individual having need thereof, of steviol, of steviol glycoside derivative or of one of their isomers.
  • a cosmetic method according to the invention can be carried out daily, for example at the rate of a single administration per day or of an administration split up into two or three times per day, for example once in the morning and once in the evening.
  • Figure 1 The viability of the melanocytes and the reduction in the production of melanin by melanocytes in the presence of increasing concentrations of rebaudioside A are illustrated in this figure.
  • the active agent tested is a Stevia extract comprising 99% of rebaudioside A sold by Blue California under the name Good'n sweetTM.
  • rebaudioside A brings about a dose-dependent decrease in the synthesis of melanin, thus resulting in a depigmentation (lower curve in the figure). This effect is observed, of course, at noncytotoxic doses (upper curve in the figure) and at an active agent concentration of greater than 0,08 mg/ml.
  • Stevia extract comprising 99% of rebaudioside
  • Stevia extract comprising 99% of rebaudioside 3.0 A, sold by Blue California under the name
  • Stevia extract comprising 99% of rebaudioside 5.00 A, sold by Blue California under the name

Abstract

La présente invention a pour objet l'utilisation du stéviol, d'un dérivé glycoside de stéviol, ou d'un de leurs isomères, pour prévenir, réduire et/ou traiter une altération du teint de la peau.
PCT/IB2012/057613 2011-12-23 2012-12-21 Utilisation de stéviol, d'un dérivé glycoside de stéviol, ou d'un de leurs isomères, pour prévenir, réduire et/ou traiter une altération du teint de la peau WO2013093880A1 (fr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
FR1162393 2011-12-23
FR1162393A FR2984742A1 (fr) 2011-12-23 2011-12-23 Utilisation de steviol, d'un derive glycoside du steviol, ou d'un de leurs isomeres, pour prevenir, reduire et/ou traiter une alteration du teint de la peau.
US201261585080P 2012-01-10 2012-01-10
US61/585,080 2012-01-10

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WO2012116990A3 (fr) * 2011-03-01 2014-05-01 Dsm Ip Assets B.V. Nouvelle utilisation
CN103893470A (zh) * 2014-04-28 2014-07-02 蚌埠火鹤制药有限公司 一种治疗蝴蝶斑的中药组合物
FR3002443A1 (fr) * 2013-02-28 2014-08-29 Oreal Composition contenant du rebaudioside a et un tensioactif oxyethylene
WO2014132219A3 (fr) * 2013-02-28 2014-11-27 L'oreal Composition contenant un rébaudioside a et un tensioactif oxyéthyléné
CN104352827A (zh) * 2014-10-10 2015-02-18 张成海 一种用于增加皮肤血液循环的淡斑熏蒸草药
US9522929B2 (en) 2014-05-05 2016-12-20 Conagen Inc. Non-caloric sweetener
CN111407698A (zh) * 2020-04-20 2020-07-14 广州市帝臣日化科技有限公司 一种祛皱保湿护肤液及其制备方法
US10752928B2 (en) 2015-04-14 2020-08-25 Conagen Inc. Production of non-caloric sweeteners using engineered whole-cell catalysts
CN113476321A (zh) * 2021-07-07 2021-10-08 珠海沅芷健康科技有限公司 一种用异甜菊醇制备皮肤美白和抗黑色素生成的化妆品制剂的应用

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FR3132215A1 (fr) * 2022-01-31 2023-08-04 L'oreal Compositions cosmétiques comprenant des quantités élevées d’hydroxypropyl tétrahydropyrantriol
WO2023076578A1 (fr) * 2021-10-31 2023-05-04 L'oreal Compositions cosmétiques comprenant des quantités élevées d'hydroxypropyl tétrahydropyrantriol

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Cited By (18)

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WO2012116990A3 (fr) * 2011-03-01 2014-05-01 Dsm Ip Assets B.V. Nouvelle utilisation
FR3002443A1 (fr) * 2013-02-28 2014-08-29 Oreal Composition contenant du rebaudioside a et un tensioactif oxyethylene
WO2014132219A3 (fr) * 2013-02-28 2014-11-27 L'oreal Composition contenant un rébaudioside a et un tensioactif oxyéthyléné
CN103893470A (zh) * 2014-04-28 2014-07-02 蚌埠火鹤制药有限公司 一种治疗蝴蝶斑的中药组合物
US10654881B2 (en) 2014-05-05 2020-05-19 Conagen Inc. Non-caloric sweetener
US10597418B2 (en) 2014-05-05 2020-03-24 Conagen Inc. Non-caloric sweetener
US9527880B2 (en) 2014-05-05 2016-12-27 Conagen Inc. Non-caloric sweetener
US9765104B2 (en) 2014-05-05 2017-09-19 Conagen Inc. Non-caloric sweetener
US9988414B2 (en) 2014-05-05 2018-06-05 Conagen Inc. Non-caloric sweetener
US10138263B2 (en) 2014-05-05 2018-11-27 Conagen Inc. Non-caloric sweetener
US10450339B2 (en) 2014-05-05 2019-10-22 Conagen Inc. Non-caloric sweetener
US9522929B2 (en) 2014-05-05 2016-12-20 Conagen Inc. Non-caloric sweetener
US10941174B2 (en) 2014-05-05 2021-03-09 Conagen Inc. Non-caloric sweetener
CN104352827A (zh) * 2014-10-10 2015-02-18 张成海 一种用于增加皮肤血液循环的淡斑熏蒸草药
US10752928B2 (en) 2015-04-14 2020-08-25 Conagen Inc. Production of non-caloric sweeteners using engineered whole-cell catalysts
CN111407698A (zh) * 2020-04-20 2020-07-14 广州市帝臣日化科技有限公司 一种祛皱保湿护肤液及其制备方法
CN113476321A (zh) * 2021-07-07 2021-10-08 珠海沅芷健康科技有限公司 一种用异甜菊醇制备皮肤美白和抗黑色素生成的化妆品制剂的应用
CN113476321B (zh) * 2021-07-07 2023-09-22 珠海沅芷健康科技有限公司 一种用异甜菊醇制备皮肤美白和抗黑色素生成的化妆品制剂的应用

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