Cosmetic composition

Abstract

According to the present invention, there is provided a cosmetic composition suitable for application to menopausal skin, the composition comprising an Ophiopogon japonicus extract and a phytoestrogen isoflavone.

Description

Technical Field

[0001] The present invention is directed to a composition specifically designed for application to menopausal skin. Background Art

[0002] From a cosmetic perspective, healthy-looking skin is characterized by moisturized, smooth and flawless skin, shiny and radiant complexion, and an even, non-greasy complexion. The skin epidermis undergoes a continuous renewal process in which the maintenance of tissue integrity is controlled by maintaining a constant pool of epidermal cells in which the rate of mitosis is balanced with the rates of desquamation and apoptosis. The constant renewal of the skin layers maintains the integrity of the skin barrier function. This is known as epidermal homeostasis. Throughout life, transient changes in, for example, lifestyle, mental health, sleep, nutrition, environmental exposures can lead to transient fluctuations in skin appearance, driven primarily by changes in epidermal homeostasis. Hormones represent an additional extrinsic factor, either naturally produced by endocrine glands coinciding with life stages or provided by supplementation in contraception, performance enhancers, and hormone replacement therapy (HRT), and there is increasing evidence that hormones can influence dermatological mechanisms that will have an impact on cosmetically healthy skin issues.

[0003] The most studied hormonal skin disorder is acne. This skin disease involves a complex chain of events that are controlled by androgens, which affect the pilosebaceous unit, resulting in increased sebum production and inflammation. Sex hormone fluctuations have also been implicated in premenstrual "acne" outbreaks, with peaks in testosterone levels associated with the highest acne prevalence (Williams M, Cunliffe WJ. Explanation for premenstrual acne. Lancet. 1973; 2(7837): 1055–1057 and Geller, Rosen, Frankel, Goldenberg. Perimenstrual Flare of Adult Acne. J Clin Aesthet Dermatol. 2014 Aug; 7(8): 30–34.). However, the effects of hormonal fluctuations are not limited to acne.

[0004] Perhaps the most studied hormone and its effect on the skin is estrogen. Menopause represents a transitional period when estrogen levels plummet. The skin shows the effects of estrogen depletion, with reports of skin dryness, accelerated deterioration of wrinkles and loss of firmness, which are key issues of concern to patients and consumers. These issues correspond to changes in structure and building components (such as collagen content) and reduced sebum production that affects the quality of the skin barrier function. Keratinocytes have estrogen receptors, which are considered to be important regulators of cell differentiation, proliferation and epithelialization, and therefore important regulators of epidermal homeostasis. The above-mentioned skin changes observed in postmenopausal skin are partially rescued in the HRT cohort, indicating the important role of estrogen in epidermal homeostasis. Finally, inflammation is considered to be a key potential biological component of estrogen-deficient skin. Estrogen itself is anti-inflammatory, so an inevitable result of perimenopausal and postmenopausal skin is increased activation of inflammatory cytokine cascades. Interleukin-8 is a chemotactic cytokine that attracts inflammatory cells such as neutrophils to tissues such as skin, thereby initiating an inflammatory response. Therefore, the increased inflammatory response affects epidermal homeostasis and forces further disorder of skin barrier function. These mechanisms are reasonably believed to be the cause of the visible appearance changes observed in perimenopausal and postmenopausal skin. Therefore, although not wishing to be bound by theory, it is believed that the depletion of estrogen can lead to disorder of overall skin barrier function and epidermal homeostasis, resulting in significant changes in skin appearance such as dryness, elasticity, texture, tone, gloss and brightness.

[0005] In addition to the above, psychological stress can also exacerbate various skin diseases, including psoriasis, atopic dermatitis and acne. During stressful periods, the human body produces and releases the hormone cortisol, which is often referred to as the "stress hormone." Increased cortisol levels are also associated with increased inflammation, which in turn affects epidermal homeostasis and skin barrier function. Studies have shown that final exams and interview stress can affect skin barrier function, which is associated with increased plasma cortisol levels and upregulated inflammation (Effect of "Rose Essential Oil" Inhalation on Stress-Induced Skin-Barrier Disruption in Rats and Humans. Mika Fukada, Eri Kano, Michio Miyoshi, Ryoichi Komaki, Tatsuo Watanabe. Chemical Senses, Volume 37, Issue 4, May 2012, Pages 347–356). It is therefore not surprising that the skin is a known target of Cortisol and is in fact capable of producing its own corticosteroids, where corticosteroid (CR) receptors are available to mediate inflammatory biological effects.

[0006] This application seeks to address some of the issues women experience in terms of changes in skin health, moisturization and appearance during the peri- and post-menopausal periods of their lives. Summary of the invention

[0007] According to the present invention, there is provided a cosmetic composition suitable for application to menopausal skin, the composition comprising an Ophiopogon Japonicus extract and plant-derived isoflavones. DETAILED DESCRIPTION

[0008] The present invention relates to a cosmetic composition suitable for application to perimenopausal and postmenopausal skin, the composition comprising an extract of Ophiopogon japonicus and phytoestrogen isoflavones. Unless otherwise specified, the composition referred to in the present invention is the composition referred to in all aspects of the present invention.

[0009] Ophiopogon japonicus extract

[0010] The composition of the present invention comprises an extract of Ophiopogon japonicus. Preferably, the raw material ingredient used in the present invention is an extract of the root of the Ophiopogon japonicus plant.

[0011] Ophiopogon root extract includes a steroidal glycoside called ophiopogonin D (OPD), which has anti-inflammatory benefits. Ophiopogon root also contains a variety of additional bioactive compounds, including steroidal saponins, homoisoflavones and polysaccharides, which have antioxidant, anticancer, antidiabetic, immunomodulatory, anti-acute inflammatory, antitussive and antimicrobial activities.

[0012] Ophiopogon root extract is available from Silab and sold under the trade names Cohesium and Ad-Resyl.

[0013] The level of Ophiopogon japonicus extract present in the composition of the present invention is at least 0.01%, at least 0.1%, at least 1.0%. The level of Ophiopogon japonicus extract present in the composition of the present invention is less than 10%, less than 7.5%, less than 5.0%. The level of Ophiopogon japonicus extract present in the composition of the present invention is 0.1 to 10%, 0.75% to 7.5% and preferably 1 to 5%.

[0014] Phytoestrogen Isoflavones

[0015] Phytoestrogens are estrogen-like compounds found in a variety of plants that are similar in structure. The compositions of the present invention include phytoestrogen isoflavones derived from phytoestrogen plants. Phytoestrogen plants include soybean (Glycine max), red clover (Trifolium pratense), white clover (Trifolium repens), alfalfa (Medicago sativa), garlic (Allium sativum), celery (Apiaceae graveolens), carrot (Daucus carota), potato (Solanum tuberosum), rice (Oryza sativa), wheat (Trwiticumaestivum), sweet potato (Ipomoea batatas), apple (Malus domestica), pomegranate (Punica granatum), chasteberry (Vitex agnus-castus), coffee (Coffea arabica and Coffea robusta), and mixtures thereof.

[0016] In one embodiment, the plant-derived isoflavones are selected from plant-derived plants selected from the group consisting of soybean (Glycine max), red clover (Trifolium pratense), white clover (Trifolium repens), alfalfa (Medicago sativa), and mixtures thereof.

[0017] Isoflavones can be divided into the following two types according to the presence or absence of glycosides: (1) glycosylated phytoestrogen isoflavones (also known as phytoestrogen isoflavone glycosides), which include daidzein, genistein, glycitin, malonyldaidzein, malonylgenistein, malonylglycitin, acetyldaidzin and acetylglycitin; and (2) deglycosylated phytoestrogen isoflavones (also known as phytoestrogen isoflavone aglycones), which include daidzein, genistein and glycitein. Compared with glycosylated phytoestrogen isoflavones, deglycosylated phytoestrogen isoflavones have higher bioavailability and can therefore achieve better health benefits.

[0018] Preferred isoflavones are selected from the group consisting of: genistein (5,7,4'-trihydroxy-isoflavone), genistein (5,7,4'-trihydroxy-isoflavone-7-glucoside), daidzein (7.4'-dihydroxy-isoflavone), equol (4',7-dihydroxy-isoflavane), daidzein (7.4'-dihydroxy-isoflavone-7-glucoside), biochanin A (5.7-dihydroxy-4'-methoxy-isoflavone), glycitein (7.4 '-dihydroxy-6-methoxy-isoflavone), glycitin (7.4'-dihydroxy-6-methoxy-isoflavone-7-glucoside), olopol (5.3',4'-trihydroxy-7-methoxy-isoflavone), olopol (5,7,3',4'-tetrahydroxy-isoflavone), santal (5,7,3'-trihydroxy-4'-methoxy-isoflavone) and / or enzyme inhibitors (5.4'-dihydroxy-7-methoxy-isoflavone) and mixtures thereof.

[0019] In one embodiment of the present invention, the plant-derived isoflavones are soy isoflavones. Soy is known to contain a phytoestrogen, soy isoflavones, which can bind to estrogen receptors and produce estrogen-like physiological effects on the female body, although this effect is weak. Literature on this topic shows that soy isoflavones can be used to treat menopausal symptoms such as mood swings, temperature fluctuations and fatigue in perimenopausal and postmenopausal women. In general, soy isoflavones are described with reference to foods or supplements and are ingestible.

[0020] Methods for preparing soy isoflavones are well known in the art, and soy isoflavones can be easily purchased from manufacturers. In fact, conventional soy milk (also known as filtered soy milk) is prepared by grinding whole soybean material soaked in water, then optionally filtering the resulting soy slurry with gauze, and optionally heating the filtrate so obtained to sterilize. Although the filtering process can remove soybean residues with large particle size from the soy slurry, this process also reduces the amount of active ingredients in the soy slurry, thereby reducing the value of the filtered soy milk.

[0021] In one embodiment of the present invention, the plant-derived isoflavones are contained in a liposomal structure.Liposomal delivery systems are preferred for improving the penetration of isoflavones through the epidermis.

[0022] In one embodiment of the present invention, the plant-derived isoflavone is Lipobelle (trade name) commercially available from Mibelle Biochemistry Group. Lipobelle is a liposomal preparation of genistein.

[0023] In one embodiment of the invention, the cosmetic or dermatological preparations according to the invention comprise from 0.001 to 20% by weight, particularly preferably from 0.01 to 5% by weight, of isoflavones of plant origin.

[0024] In one embodiment, the Ophiopogon japonicus extract and the plant-derived isoflavones are present in a ratio of 5:1 to 1:2. In one embodiment, the Ophiopogon japonicus extract and the plant-derived isoflavones are present in a ratio of 4:1 to 1:1. In one embodiment, the Ophiopogon japonicus extract and the plant-derived isoflavones are present in a ratio of 3.5:1 to 2:1.

[0025] Vitamin B3 or vitamin B3 derivatives

[0026] The cosmetic composition of the present invention preferably includes vitamin B3, also known as niacin or nicotinic acid, and / or a vitamin B3 derivative. The physiologically active form of niacin is niacinamide. Nicotinic acid and niacinamide (nicotinamide or nicotinic acid amide) function in vivo as components of the following two coenzymes: nicotinamide adenine dinucleotide (NAD) and nicotinamide adenine dinucleotide phosphate (NADP).

[0027] The composition used in the present invention may include a safe and effective amount of a (natural or synthetic) vitamin B3 compound. As used herein, "vitamin B3 compound" means a compound having the formula:

[0028]

[0029] wherein R is -CONH2 (ie, nicotinamide), -COOH (ie, nicotinic acid) or -CH2OH (ie, nicotinic alcohol); derivatives thereof; and any salts of the foregoing.

[0030] Exemplary derivatives of the foregoing vitamin B3 compounds include nicotinic acid esters, including non-vasodilating esters of nicotinic acid, nicotinyl amino acid, nicotinyl alcohol esters of carboxylic acids, nicotinic acid N-oxide, and nicotinamide N-oxide.

[0031] Suitable nicotinic acid esters include nicotinic acid esters of C1-C22, preferably C1-C16, more preferably C1-C6 alcohols. The alcohol may be linear or branched, cyclic or acyclic, saturated or unsaturated (including aromatic) and substituted or unsubstituted. Preferred esters are those that do not produce a visible flushing reaction after application to the skin. Alternatively, nicotinic acid substances that do produce a flushing reaction may be used if used in lower doses to reduce the flushing effect. Non-flushing nicotinic acid esters include tocopherol nicotinate and inositol hexanicotinate. Tocopherol nicotinate is preferred.

[0032] Other derivatives of vitamin B3 compounds are derivatives of nicotinamide produced by substitution of one or more amide group hydrogens. Non-limiting examples of derivatives of nicotinamide useful herein include nicotinyl amino acids, derived, for example, from the reaction of activated nicotinic acid compounds (e.g., nicotinic acid azide or nicotinyl chloride) with amino acids, and nicotinyl alcohol esters of organic carboxylic acids (e.g., C1-C18). Specific examples of such derivatives include nicotinyl glycine and nicotinyl hydroxamic acid.

[0033] Exemplary nicotinic alcohol esters include nicotinic alcohol esters of carboxylic acids including salicylic acid, acetic acid, glycolic acid, palmitic acid, etc. Other suitable vitamin B3 compounds are selected from the group consisting of 2-chloronicotinamide, 6-aminonicotinamide, 6-methylnicotinamide, n-methyl-nicotinamide, n,n-diethylnicotinamide, n-(hydroxymethyl)-nicotinamide, quinolinic acid imide, nicotinanilide, n-benzylnicotinamide, n-ethylnicotinamide, nifenazone, nicotinaldehyde, isonicotinic acid, methylisonicotinic acid, thionicotinamide, nialamide, 1-(3-pyridylmethyl)urea, 2-mercaptonicotinic acid, nicomol, niaprazine, and mixtures thereof.

[0034] Examples of the above vitamin B3 compounds are well known in the art and are commercially available from a number of sources, for example, Sigma Chemical Company (St. Louis, MO); ICN Biomedicals, Inc. (Irvin, CA); and Aldrich Chemical Company (Milwaukee, WI).

[0035] The composition of the present invention preferably includes one or more vitamin B3 compounds. Preferred vitamin B compounds are selected from the group consisting of C1-C22 straight or branched chain, cyclic or acyclic, saturated or unsaturated (including aromatic) and substituted or unsubstituted nicotinic acid esters, nicotinyl amino acids, nicotinyl glycine, nicotinyl hydroxamic acid, nicotinyl alcohol esters of carboxylic acids (including salicylic acid, acetic acid, glycolic acid, palmitic acid), 2-chloronicotinamide, 6-aminonicotinamide, 6-methylnicotinamide, n-methyl-nicotinamide, n,n-diethylnicotinamide, n-(hydroxymethyl)-nicotinamide, quinolinic acid imide, nicotinanilide, n-benzylnicotinamide, n-ethylnicotinamide, nifenazone, nicotinaldehyde, isonicotinic acid, methyl isonicotinic acid, thionicotinamide, nyalamid, 1-(3-pyridylmethyl)urea, 2-mercaptonicotinic acid, nicotinamide, nyprazine, nicotinamide, tocopherol nicotinate and mixtures thereof.

[0036] Preferred vitamin B3 compounds are niacinamide and tocopheryl nicotinate. Niacinamide is more preferred.

[0037] Salts of vitamin B3 compounds are also useful herein. Non-limiting examples of salts of vitamin B3 compounds useful herein include organic or inorganic salts, such as inorganic salts with anionic inorganic species (e.g., chlorides, bromides, iodides, carbonates, preferably chlorides), and organic carboxylates (including mono-C1-C18 carboxylates, di-C1-C18 carboxylates, and tri-C1-C18 carboxylates, e.g., acetates, salicylates, glycolates, lactates, malates, citrates, preferably mono-carboxylates, such as acetates).

[0038] The vitamin B3 compound may be included as the substantially pure material, or as an extract isolated from a natural source by suitable physical and / or chemical methods. The vitamin B3 compound is preferably substantially pure, more preferably essentially pure.

[0039] The amount of vitamin B or vitamin B derivative present in the composition may be at least 0.01%, at least 0.05%, at least 0.1%, at least 0.5% by weight; the amount of vitamin B or vitamin B derivative present in the composition may be 5% or less, 4% or less, 3% or less, 2% or less, 1% or less, 0.5% or less, 0.1% or less, or 0.05% or less by weight. When more than one vitamin B or vitamin B derivative is present, these values ​​apply to the total amount of vitamin B or vitamin B derivative in the composition.

[0040] Specifically, the amount of vitamin B or a vitamin B derivative (e.g., niacinamide) present in the composition may be 0.01 to 5%, 0.05% to 3%, 0.1% to 3%, 0.1% to 2%, 0.5% to 1%, or 0.5% to 2% by weight.

[0041] Ceramide

[0042] Ceramides are a family of waxy lipid molecules. Ceramides are composed of sphingosine and fatty acids. In an optional embodiment of the present invention, the composition includes at least one ceramide. Without being limited by theory, the ceramide may be selected from the group consisting of: ceramide 1 (ceramide EOP), ceramide 2 (ceramide NG), ceramide 3 (ceramide NP) and / or ceramide 6 (ceramide AP). The above ceramides are well known in the art and defined by this nomenclature. However, to avoid ambiguity: ceramide 1 (ceramide EOS)-includes a sphingosine base and a non-hydroxy fatty acid chain connected to linoleic acid; ceramide 2 (ceramide NS) includes a sphingosine base and a non-hydroxy fatty acid chain; ceramide 3 (ceramide NP) includes a phytosphingosine base (an OH group at the C4 position on the sphingosine base molecule) and a non-hydroxy fatty acid chain; ceramide 6 (ceramide AP) includes a phytosphingosine base (an OH group at the C4 position on the sphingosine base molecule) and an α-hydroxy fatty acid chain (an additional OH group on the fatty acid relative to the non-hydroxyl group).

[0043] In a preferred aspect of the invention, the composition preferably comprises ceramide 3 (ceramide NP), also known as N-oleoyl-4-hydroxydihydrosphingosine. In a further preferred but optional aspect of the invention, the composition preferably comprises ceramide 6 (ceramide AP).

[0044] Alternatively, the composition may include at least two ceramides, such as ceramide 3 and ceramide 6. Alternatively, the composition may include at least three ceramides, such as ceramide 1, ceramide 3, and ceramide 6.

[0045] In one embodiment of the present invention, the ceramide is Skinmimic (trade name) commercially available from Evonik. Skinmimic is an ingredient comprising a plurality of ceramides including ceramide EOP, ceramide EOS, ceramide NP, ceramide NS, ceramide AP, hexanoyl phytosphingosine and hexanoyl sphingosine.

[0046] When present, the amount of ceramide present in the composition (e.g., the amount of ceramides alone or in combination) can be at least 0.003%, at least 0.005%, at least 0.008%, or at least 0.01% by weight; and / or the amount of at least one ceramide present in the composition (e.g., the combined amount of Ceramides 1, 3, and 6) can be 0.1% or less, 0.05% or less, 0.03% or less, or 0.01% or less by weight.

[0047] When present, the amount of ceramide present in the composition (eg, the amount of ceramides alone or in combination) may be 0.003% to 0.03% or 0.005% to 0.02% by weight.

[0048] Skin Soothing Agent

[0049] The compositions of the present invention may include a skin soothing agent. The skin soothing agent has the effect of calming irritated or sensitive skin and thus has anti-inflammatory activity. These ingredients are usually, but not exclusively, derived from plants.

[0050] A preferred skin soothing agent is an extract of Centella asiatica. Centella asiatica extract, also known as Gotu kola or India Pennyworth. Preferably, the material known as Centella asiatica is an extract from the leaves of the plant and is characterized by the presence of bioactive triterpenes, including madecassoside, and a polyphenolic fraction that contributes to the biological efficacy of the extract. The product is known to have antioxidant benefits and can promote the synthesis of type I and type III collagen. This extract is commercially available from Indena under the trade name Centevita.

[0051] Centella asiatica extract, meaning the extract obtained from a supplier, may be present in the composition of the present invention at a level of 0.001%, alternatively 0.002%, alternatively 0.1% by weight of the composition. The level of Centella asiatica extract in the composition of the present invention may be 0.5% or less, alternatively less than 0.25% or less, or alternatively 0.1% or less. In one embodiment, the level of Centella asiatica extract present in the composition of the present invention may be from 0.001% to 0.5% by weight of the composition. In one embodiment, the level of Centella asiatica extract present in the composition of the present invention may be from 0.005% to 0.25% by weight of the composition. In one embodiment, the level of Centella asiatica extract present in the composition of the present invention may be from 0.01% to 0.1% by weight of the composition.

[0052] An alternative skin soothing agent is the monocyclic sesquiterpene alcohol. Sesquiterpenes are a class of terpenes composed of three isoprene units and generally have a molecular formula of C 15 H 24 . Sesquiterpenes can be acyclic or contain rings. Alternatively, the skin soothing agent can be an alcohol derivative of a monocyclic (single ring) sesquiterpene. For example, the monocyclic sesquiterpene alcohol can be α-bisabolol (shown below, left) or β-bisabolol (shown below, right). Synthetic bisabolol is usually a racemic mixture: α-(±)-bisabolol

[0053]

[0054] The amount of monocyclic sesquiterpene alcohol (e.g., α-bisabolol) present in the composition may be at least 0.001%, at least 0.005%, at least 0.01%, at least 0.05%, at least 0.1% by weight; at least 2.5%; and / or the amount of monocyclic sesquiterpene alcohol (e.g., α-bisabolol) present in the composition may be 2% or less, 1% or less, 0.5% or less by weight.

[0055] Specifically, the amount of monocyclic sesquiterpene alcohol (eg, α-bisabolol) present in the composition may be 0.001% to 2%, 0.01% to 1%, or 0.05% to 0.5% by weight.

[0056] Other components

[0057] The composition of the present invention can be aqueous or emulsion, including water-in-oil or oil-in-water emulsion. When the composition is aqueous, it preferably includes 10% to 99.9% water by weight. In a preferred embodiment, the aqueous composition includes 20% to 80% water by weight. In a preferred embodiment, the aqueous composition includes 40% to 70% water by weight. The aqueous phase also preferably contains a humectant, which can be selected from the following diols or triols. Preferred diols are selected from the group consisting of pentylene glycol, caprylyl glycol, butylene glycol, dipropylene glycol, ethylhexylglycerin, propylene glycol, hexylene glycol, glycerine, butylene glycol, propylene glycol, isoprene glycol, dipropylene glycol, pentylene glycol, hexylene glycol, polypropylene glycol, butylene glycol, polyethylene glycol, sorbitol, glucitol, mannitol, hydroxypropyl sorbitol, erythritol, threitol, pentaerythritol, xylitol and mixtures thereof. Preferred triols are selected from the group consisting of hexanetriol, glycerol, ethoxylated glycerol, propoxylated glycerol, and mixtures thereof.

[0058] When the composition is an emulsion, the oil phase of the emulsion may be provided by any suitable oily component. Suitable oils for the oil phase may include, for example: a) hydrocarbon oils such as paraffin or mineral oil; b) waxes such as beeswax or paraffin; c) natural oils such as sunflower oil, almond oil, shea butter or jojoba oil; d) silicone oils such as dimethicone, silicone elastomer, cyclomethicone or cetyl dimethicone; e) fatty acid esters and ethers such as isopropyl palmitate, isopropyl myristate, caprylic / capric triglyceride, C12-15 alkyl benzoate and polypropylene glycol-15 stearyl ether; f) fatty alcohols such as cetyl alcohol or stearyl alcohol, g) branched primary alcohols such as octyldodecanol; or h) mixtures thereof, for example blends of waxes commercially available under the trade name Cutina (BASF). Preferably, the emulsion comprises an oil phase of 0.1% to 55%, more preferably 15% to 50%, most preferably 30% to 45% by weight of the emulsion. Preferably, the oil phase of the emulsion comprises oil at a level of 50% to 99.9% by weight of the oil phase. More preferably, the oil phase comprises oil at a level of 60% to 99.9%, more preferably 70% to 99.9%, and even more preferably 80% to 99.9% by weight of the oil phase.

[0059] Preferably, the oil phase of the water-in-oil emulsion comprises silicone oil. When present, the silicone-containing oil phase preferably comprises an organopolysiloxane oil. The organopolysiloxane oil used in the composition can be volatile, non-volatile or a mixture of volatile and non-volatile silicones. The term "non-volatile" as used in this context refers to those silicones that are liquid or gel under ambient conditions and have a flash point (at one atmosphere) above 100°C. The term "volatile" as used herein refers to all other silicone oils. Suitable organopolysiloxanes can be selected from various silicones with a wide range of volatility and viscosity. Examples of suitable organopolysiloxane oils include polyalkylsiloxanes, cyclic polyalkylsiloxanes and polyalkylarylsiloxanes.

[0060] Preferred for use herein are organopolysiloxanes selected from the group consisting of polyalkylsiloxanes, alkyl-substituted polydimethylsiloxanes, cyclomethicone, trimethylsiloxysilicate, dimethiconol, polyalkylaryl siloxanes, and mixtures thereof. More preferred for use herein are polyalkylsiloxanes and cyclomethicone. Preferred among the polyalkylsiloxanes is polydimethylsiloxane.

[0061] Optionally, suitable silicones are silicone elastomers. Suitable silicone elastomers for use herein may be crosslinked siloxane elastomers or mixtures thereof that are emulsified or non-emulsified. There are no specific restrictions on the type of curable organopolysiloxane composition that can serve as the starting material for the crosslinked organopolysiloxane elastomer. Examples of this are addition reaction curing organopolysiloxane compositions that are cured by addition reactions between SiH-containing diorganopolysiloxanes and organopolysiloxanes having silicon-bonded vinyl groups under platinum metal catalysis; condensation curing organopolysiloxane compositions that are cured by dehydrogenation reactions between hydroxyl-terminated diorganopolysiloxanes and SiH-containing diorganopolysiloxanes in the presence of organotin compounds, and condensation curing organopolysiloxane compositions that are cured in the presence of organotin compounds or titanates.

[0062] Preferably, the oil phase comprises silicone, and most preferably a silicone elastomer.Preferably, the emulsion composition comprises from 20% to 35% of a silicone elastomer raw material by weight of the emulsion composition.

[0063] The water-in-oil emulsion of the present invention preferably includes an emulsifier. In a preferred embodiment, the composition includes 0.1% to 10% emulsifier by weight of the composition, more preferably 0.25% to 7.5%, and even more preferably 0.5% to 5% emulsifier. The emulsifier helps to disperse and suspend the aqueous phase in the preferred silicone oil phase.

[0064] Sugar isomers

[0065] The composition may include saccharide isomerates. Saccharide isomerates are mainly composed of glucose, fructose, mannose and galactose.

[0066] Saccharide isomers mimic the NMF (natural moisturizing factor) found in human skin and are derived from plant-based glucose. Saccharide isomers are available from DSM Nutritional Products Ltd under the trade name Commercially available.

[0067] The amount of saccharide isomers present in the composition may be at least 0.05%, at least 0.1%, at least 0.2%, or at least 0.3% by weight; and / or the amount of saccharide isomers present in the composition may be 2% or less, 1% or less, 0.8% or less, 0.6 or less, or 0.4% or less by weight.

[0068] Specifically, the amount of saccharide isomers present in the composition may be 0.1% to 0.9% or 0.2% to 0.6% by weight.

[0069] Antioxidants

[0070] The compositions of the present invention may optionally include an antioxidant. Suitable antioxidants may include: a) ascorbic acid and its salts, esters, glucosides and glucosamines, in particular sodium ascorbyl phosphate, magnesium ascorbyl phosphate and ascorbyl palmitate b) vitamin E (tocopherol) and its esters, in particular tocopheryl acetate, and dimethylmethoxychromanol, which is a synthetic analogue of gamma-tocopherol, available from Lipotec SApolygon Industrial Camri Ral under the trade name Lipochroman-6, c) herbal extracts, in particular gingko biloba, such as available from Univar PLC under the trade name "Gingko Biloba Leaf Powder", morus alba, such as available from Solabia under the trade name "Mulberry Concentrate", origanum vulgare, such as available from S Black Ltd under the trade name "Pronalen Origanum HSC", panax ginseng, such as available from S Black Ltd under the trade name "Panax ginseng 1.1 extract 4294" or available from Croda Chemicals Ltd under the trade name "Phytexcell Panax ginseng", birch extracts such as available from Cosmetochem (UK) Ltd under the trade names "SuperHerbasol Extract Birch" and "HP Herbasol Betula" and from Blagden Chemicals under the trade names "Phytelene of Birch" and "Aqueous Spray Dried Birch", tea (camellia sinensis), such as available from Nichimen Europe under the trade name "Herbal Extract Green Tea 75% Solids", rosemary (rosmarrinus officinalis), such as available from S. Black under the trade name "Pronalen Rosemary", acerola powder, such as available from Gee Lawson as Acerola PE, emblica extract, available from Merck Specialitychemicals under the trade name Emblica TM Sold as well as grapeseed oil, such as available from Chesham Chemicals Limited.

[0071] The source of the antioxidant activity of some of these agents is often not completely clear; for example, it is believed that the antioxidant activity of Ginkgo extracts originates from the presence of flavonglycocide and / or terpene lactones, which can be free radical inhibitors. Birch extracts can be produced by extracting the dried leaves of Betula alba with a suitable solvent. It is believed that the anti-free radical activity of birch extracts is due to the presence of flavonoids, such as hyperosid, quencitrosid and / or myricetol-3digalactosid, which can be free radical inhibitors. These products are usually sold in the form of mixtures or solutions.

[0072] Thus, the antioxidant may consist of a number of active ingredients that are free radical inhibitors, or may also include suitable diluents and / or carriers (such as when the anti-free radical agent is some of the products mentioned herein). Therefore, the actual level of the agent in commercially available products may be somewhat unclear. Therefore, as will be appreciated by those skilled in the art, the amount of antioxidant used in the present invention is expressed in dry weight. The total amount of antioxidant present in the composition may range from 0.005% to 10%, preferably from 0.5% to 5%, and most preferably from 1% to 3.5% by weight of the composition.

[0073] Particularly preferred synergistic combinations of antioxidants suitable for inclusion in the skin care compositions of the present invention are: ginseng, mulberry and magnesium ascorbyl phosphate; ginseng, mulberry and sodium ascorbyl phosphate; ginseng, mulberry and rosemary; ginseng, mulberry and oregano.

[0074] In these preferred combinations, (a) ginseng is preferably present in an amount of 0.005% to 0.1%, more preferably 0.01% to 0.05% by weight of the composition; (b) mulberry is preferably present in an amount of 0.0005% to 0.01%, more preferably 0.001% to 0.005% by weight of the composition; (c) sodium or magnesium ascorbyl phosphate is preferably present in an amount of 0.05% to 2.5%, preferably 0.1% to 2%, most preferably 0.15% to 1.5% by weight of the composition, and (d) rosemary or oregano is preferably present in an amount of 0.01% to 0.5%, more preferably 0.05% to 0.2% by weight of the composition.

[0075] Emulsifier

[0076] The composition of the invention may include an emulsifier. Suitable emulsifiers include all those emulsifiers suitable for the purpose and known to those skilled in the art for use in skin care products. Preferably, these emulsifiers have an HLB value of 5 or more, more preferably of 5 to 17, and even more preferably of 10 to 17.

[0077] Among the emulsifiers that can be used herein are various nonionic and anionic emulsifiers, such as sugar esters and polyesters, alkoxylated sugar esters and polyesters, C1-C30 fatty acid esters of C1-C30 fatty alcohols, alkoxylated derivatives of C1-C30 fatty acid esters of C1-C30 fatty alcohols, alkoxylated ethers of C1-C30 fatty alcohols, polyglycerol esters of C1-C30 fatty acids, C1-C30 esters of polyols, C1-C30 ethers of polyols, alkyl phosphates, polyoxyalkylene fatty ether phosphates, fatty acid amides, acyl lactylates, soaps, and mixtures thereof. Non-limiting preferred examples of these non-silicone emulsifiers include: polyethylene glycol 20 sorbitan monolaurate (polysorbate 20), polyethylene glycol 5 soya sterol, steareth-20, ceteareth-20, PPG-2 methyl glucose ether distearate, ceteth-10, polysorbate 80, cetyl phosphate, potassium cetyl phosphate, diethanolamine cetyl phosphate, polysorbate 60, glyceryl stearate, PEG -100 Stearate, Polyoxyethylene 20 Sorbitan Trioleate (Polysorbate 85), Sorbitan Monolaurate, Polyoxyethylene 4 Lauryl Ether Sodium Stearate, Polyglyceryl-4 Isostearate, Hexyl Laurate, Steareth-20, Ceteareth-20, PPG-2 Methyl Glucose Ether Distearate, Ceteth-10, Diethanolamine Cetyl Phosphate, Glyceryl Stearate, PEG-100 Stearate and mixtures thereof.

[0078] Peptides

[0079] The composition of the present invention may include additional peptides. Preferably, the additional peptides are selected from the group consisting of dipeptides, tripeptides, tetrapeptides, pentapeptides and mixtures thereof. A tripeptide means a compound comprising an uninterrupted sequence of three amino acids. A tetrapeptide means a compound comprising an uninterrupted sequence of four amino acids. A pentapeptide means a compound comprising an uninterrupted sequence of five amino acids.

[0080] Dipeptide:

[0081] The composition of the present invention may include a dipeptide selected from the group consisting of: acetyl dipeptide 1 cetyl ester (tyrosine-arginine; commercially available from Sederma under the trade name Idealift), acetyl dipeptide 3 aminocaproate (alanine-arginine), azelayl bis dipeptide 10 (alanine-histidine), coumaroyl dipeptide 3 (alanine-arginine), dicetyl dipeptide 9 (glutamic acid-lysine), dipeptide diaminobutyryl benzylamide diacetate, dipeptide 1 (tyrosine-arginine), dipeptide 10 (alanine-histidine), dipeptide 11 (cysteine-lysine), dipeptide 12 (lysine-lysine), dipeptide 14 (alanine-threonine), (dipeptide 15 (glycine-glycine), dipeptide 16 (leucine-leucine), dipeptide 17 (glycine-proline), dipeptide 18 (glycine-histidine), dipeptide 19 (leucine-glutamic acid), dipeptide 2 (valine-tryptophan), dipeptide 20 (lysine-methionine), dipeptide 3 (alanine-arginine), dipeptide 4 (cysteine Acid-Glycine), Dipeptide 5 (Lysine-Valine), Dipeptide 6 (Proline-Hydroxyproline), Dipeptide 7 (Lysine-Threonine), Dipeptide 8 (Alanine-Hydroxyproline), Dipeptide 8HCL (Alanine-Hydroxyproline), Dipeptide 9 (Glutamic Acid-Lysine), Hexanoyl Dipeptide 3 Norleucine Acetate (Alanine-Arginine), Methyl Undecenoyl Dipeptide 16 (Leucine-Leucine), Nicotinyl Dipeptide 22 (Serine-Valine), Nicotinyl Dipeptide 23 (Proline-Serine), Nicotinyl Dipeptide 2 4 (glutamic acid-threonine), nicotinyl dipeptide 26 (arginine-valine), oleoyl dipeptide 15 (glycine-glycine), palmitoyl dipeptide 10 (alanine-histidine), palmitoyl dipeptide 13 (tryptophan and glutamic acid), palmitoyl dipeptide 17 (glycine-proline), palmitoyl dipeptide 5 diaminobutyryl hydroxythreonine (lysine-valine), palmitoyl dipeptide 5 diaminohydroxybutyrate (lysine-valine), palmitoyl dipeptide 7 (lysine-threonine) and mixtures thereof.

[0082] The dipeptide, when present, is preferably incorporated into the emulsion of the invention at a level of from 0.1 to 50000 ppm, more preferably from 1 to 5000 ppm, most preferably from 10 to 500 ppm.

[0083] Tripeptide:

[0084] The compositions of the present invention preferably include a tripeptide. The tripeptide may be naturally occurring or synthetically derived. Suitable tripeptides include tripeptides 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, derivatives thereof, and mixtures thereof.

[0085] Particularly preferred tripeptides include one or more tripeptides based on His. However, another suitable tripeptide can be Arg-Lys-Arg. Particularly preferred tripeptides are based on the structure Gly-His-Lys and its analogs and derivatives thereof. These are collectively referred to as GHK-tripeptides in this article. In fact, the preferred tripeptides according to this aspect of the present invention have this precise amino acid sequence. The analogs of the preferred tripeptides that can be used herein include one or more analogs of the three amino acids that are reorganized or rearranged in the sequence (e.g., Gly-Lys-His) and / or those in which no more than two amino acids are replaced (e.g., His-Ala-Orn). However, most preferably, the amino acid replacing Gly includes aliphatic side chains such as, but not limited to, β-Ala, Ala, Val, Leu, Pro, sarcosine (Sar) and Ile. Most preferably, Ala, Leu and Ile. The most preferred amino acids replacing Lys or His include amino acids having side chains comprising predominantly charged nitrogen at pH 6, such as, but not limited to, Pro, Lys, Arg, His, desmosine, and isodesmosine. Most preferably, Lys is replaced by Orn, Arg, or citrulline.

[0086] Derivatives are also considered to be included in the term GHK-tripeptide according to the present invention (and therefore also include the more general term tripeptide). Derivatives of the GHK-tripeptide according to the present invention include derivatives of the displacement and rearrangement of the tripeptide described herein. These derivatives especially include acyl derivatives, which are tripeptides substituted with the following: one or more straight or branched chains, long or short chains, saturated or unsaturated, substituted or unsubstituted with hydroxyl, amino, acylamino, sulfate or sulfide groups, which can be derived from acetic acid, capric acid, lauric acid, myristic acid, caprylic acid, palmitic acid, stearic acid, behenic acid, linoleic acid, linolenic acid, lipoic acid, oleic acid, isostearic acid, elaidic acid, 2-ethylhexanoic acid, coconut oil fatty acid, tallow fatty acid, hardened tallow fatty acid, palm kernel oil fatty acid, lanolin fatty acid, etc. Preferred examples of acyl groups include acetyl groups, palmitoyl groups, elaidoyl groups, myristyl groups, biotinyl groups and capryl groups. These can be substituted or unsubstituted. When substituted, they are preferably substituted with hydroxyl or sulfur-containing groups such as, but not limited to, SO3H, SH or SS.

[0087] The tripeptide based on His includes at least one histidine amino acid. The other two amino acids in the sequence can be the same or different. Therefore, it is encompassed but not limited to His-Xaa-Xaa, His-Xaa-Xbb, His-Xbb-Xaa, Xbb-His-Xbb, Xbb-His-Xaa, Xaa-His-Xbb, Xaa-Xaa-His, Xaa-Xbb-His, Xbb-Xaa-His and Xbb-Xbb-His, wherein Xaa and Xbb are two different amino acids, but any one of them can be His. Preferably, at least one of the other amino acids is Gly, β-Ala, Ala, Val, Leu, Pro, sarcosine (Sar) or Ile. Preferably, at least one of the other amino acids is Pro, Lys, Arg, His, desmosine and isodesmosine. Most preferably, Lys is replaced by Orn, Arg or citrulline. Derivatives are also considered to be encompassed in the term His-based tripeptides according to the invention (and therefore also the more general term tripeptides). These derivatives include in particular acyl derivatives, which are tripeptides substituted with one or more linear or branched, long or short chain, saturated or unsaturated, substituted or unsubstituted acyl groups having 1 to 29 carbon atoms. The acyl groups that can be used are the same as those described for the GHK-tripeptide.

[0088] Particularly preferred embodiments of the tripeptides according to the present invention include N-acyl-Gly-His-Lys and most preferably, N-palmitoyl-Gly-His-Lys. Preferred commercially available compositions including tripeptides and tripeptide derivatives include Biopeptide-CL from SEDERMA, Maxilip (R) from SEDERMA, Biobustyl (R) from SEDERMA.

[0089] The tripeptides of the present invention are preferably used in amounts as low as 0.10 ppm to 10,000 ppm, preferably 0.50 ppm to 5,000 ppm, more preferably 1 ppm to 1000 ppm, and most preferably 1 ppm to 500 ppm. These are also based on a % w / w basis. Thus, 100,000 ppm is 10% by weight of the emulsion.

[0090] Tetrapeptide:

[0091] The emulsion of the present invention preferably comprises a tetrapeptide. These may be one or more rigin-based tetrapeptides, one or more ALAMCAT-tetrapeptides or mixtures thereof. These tetrapeptides may be naturally occurring or synthetic in origin. Suitable tetrapeptides for use in the present composition include those selected from the group consisting of: tetrapeptide 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 34, 35, derivatives thereof and mixtures thereof.

[0092] The tetrapeptides based on Rigin according to the present invention are based on the structure Gly-Gln-Pro-Arg (Rigin) and include analogs and derivatives thereof. Rigin is a preferred tetrapeptide. Analogs of tetrapeptide sources useful according to the present invention include those in which one or more of the four amino acids are reorganized or rearranged within the sequence and / or in which no more than two amino acids are replaced (e.g., Ala-Gln-Thr-Arg. More preferably, at least one amino acid within the sequence is Pro or Arg, and most preferably, the tetrapeptide includes both Pro and Arg, although their order and position may be different. Amino acid replacements can be from any amino acid defined herein. Particularly preferred tetrapeptides based on Rigin include Xaa-Xbb-Arg-Xcc, Xaa-Xbb-Xcc-Pro, Xaa-Xbb-P ro-Arg, wherein Xaa-Xbb-Pro-Xcc, Xaa-Xbb-Xcc-Arg, Xaa, Xbb and Xcc may be the same or different and are selected from the following: Xaa is Gly or an amino acid that can be replaced thereby, Xbb is Gln or an amino acid that can be replaced thereby, and Xcc may be Pro or Arg or an amino acid that can be replaced thereby. The most preferred amino acids replacing Gly include aliphatic side chains such as, but not limited to, β-Ala, Ala, Val, Leu, Pro, sarcosine (Sar) and Ile. The most preferred amino acids replacing Gln include side chains containing mainly uncharged amine groups at neutral pH (pH 6-7), such as, but not limited to, Asn, Lys, Orn, 5-hydroxyproline, citrulline and canavanine. When Arg is replaced, it is preferably replaced by amino acids having side chains that mainly include charged nitrogen at pH 6, such as, but not limited to, Pro, Lys, His, desmosine and isodesmosine.

[0093] Derivatives are also considered to be encompassed by the term rigin-based tetrapeptides according to the present invention (and therefore also the more general term tetrapeptides). Derivatives include substituted and rearranged derivatives of the rigin-based tetrapeptides described herein. These derivatives include in particular acyl derivatives, which are tetrapeptides substituted with one or more linear or branched, long or short chain, saturated or unsaturated, substituted with hydroxyl, amino, aminoacyl, sulfate or sulfide groups or unsubstituted with 1 to 29 carbon atoms. N-acyl derivatives include acyl groups derivable from acetic acid, capric acid, lauric acid, myristic acid, caprylic acid, palmitic acid, stearic acid, behenic acid, linoleic acid, linolenic acid, lipoic acid, oleic acid, isostearic acid, elaidic acid, 2-ethylhexanoic acid, coconut oil fatty acids, tallow fatty acids, hardened tallow fatty acids, palm kernel oil fatty acids, lanolin fatty acids, etc. Preferred examples of acyl groups include acetyl groups, palmitoyl groups, elaidoyl groups, myristyl groups, biotinyl groups and octanoyl groups. These can be substituted or unsubstituted. When substituted, they are preferably substituted by hydroxyl or groups including sulphur such as but not limited to SO3H, SH or SS.

[0094] ALAMCAT tetrapeptides are tetrapeptides comprising at least one amino acid comprising a side chain containing an aliphatic group. These amino acids include, but are not limited to, Gly, β-Ala, Ala, Val, Leu, Sarcosine (Sar), and Ile. These tetrapeptides also include at least one amino acid comprising at least one side chain containing NH2. These amino acids include side chains having amine groups that are primarily uncharged at neutral pH (pH 6-7), such as, but not limited to, Gln, Asn, Lys, Orn, 5-hydroxyproline, citrulline, and canavanine. ALAMCAT-tetrapeptides also include at least one amino acid having at least one side chain comprising at least one cationic amine (the primary species being charged, such as NH3+, NH2+, etc. - basic amino acids that are positively charged at pH 6.0). These amino acids include, but are not limited to, Pro, Arg, Lys, His, desmosine, and isodesmosine. The remaining amino acids may be any amino acid, but are preferably amino acids comprising an aliphatic group, a side amino group, or a side cationic group. According to the invention, derivatives are also considered to be encompassed by the term ALAMCAT-tetrapeptide (and therefore also the more general term tetrapeptide). These derivatives include in particular acyl derivatives, which are tetrapeptides substituted with one or more linear or branched, substituted or unsubstituted long or short chain, saturated or unsaturated, acyl groups having 1 to 29 carbon atoms. The acyl groups that can be used are the same as those described for the rigin-based tetrapeptides.

[0095] Preferred embodiments include peptide E, arg-ser-arg-lys, N-acyl-Gly-Gln-Pro-Arg peptides, most preferably N-palmitoyl-Gly-Gln-Pro-Arg.

[0096] Preferred commercial tetrapeptide sources include RIGIN, EYELISS, Haloxyl and MATRIXYL 3000, which includes 50 to 500 ppm of palmitoyl-Gly-Gln-Pro-Arg, and other ingredients such as peptides, chalcone and excipients, commercially available from SEDERMA, France. Tego Pep 417 is available from Evonik. These can be used to produce the compositions of the present invention by adding thereto at least one tripeptide as described herein.

[0097] The tetrapeptide, when present (eg, a lipopeptide), may have an amino acid sequence selected from the group consisting of: (i) GPXG, (ii) LSXX, (iii) XXGD, or (iv) QTAV,

[0098] wherein, for (i), G represents the amino acid glycine and P represents the amino acid proline (according to the internationally recognized single-letter code for amino acids), and X represents an amino acid selected from the group consisting of lysine (K), glutamic acid (E) and serine (S), and mixtures thereof, wherein, for (ii), L represents the amino acid leucine and S represents the amino acid serine (according to the internationally recognized single-letter code for amino acids), and X represents an amino acid selected from the group consisting of valine (V), aspartic acid (D), proline (P), glycine (G), and mixtures thereof, wherein, for (iii), G represents the amino acid glycine and D represents the amino acid aspartic acid (according to the internationally recognized single-letter code for amino acids), and X represents an amino acid selected from the group consisting of glutamic acid (E), lysine (K), leucine (L), alanine (A), isoleucine (I), arginine (R), and mixtures thereof, and for (iv), Q represents the amino acid glutamine, T represents the amino acid threonine, A represents the amino acid alanine, and V represents the amino acid valine.

[0099] In another embodiment, the peptide (e.g., lipopeptide) has an amino acid sequence selected from the group consisting of: (i) Y-GPXG-Z, (ii) Y-LSXX-Z, (iii) Y-XXGD-Z or (iv) Y-QTAV-Z, wherein, for (i), G represents the amino acid glycine and P represents the amino acid proline (according to the internationally recognized single-letter code for amino acids), and X represents an amino acid selected from the group consisting of lysine (K), glutamic acid (E) and serine (S), and mixtures thereof, wherein, for (ii), L represents the amino acid leucine and S represents the amino acid serine (according to the internationally recognized single-letter code for amino acids), and X represents an amino acid selected from the group consisting of An amino acid selected from the group consisting of valine (V), aspartic acid (D), proline (P), glycine (G), and mixtures thereof, wherein, for (iii), G represents the amino acid glycine and D represents the amino acid aspartic acid (according to the internationally recognized single-letter code for amino acids), and X represents an amino acid selected from the group consisting of glutamic acid (E), lysine (K), leucine (L), alanine (A), isoleucine (I), arginine (R), and mixtures thereof, wherein, for (iv), Q represents the amino acid glutamine, T represents the amino acid threonine, A represents the amino acid alanine, and V represents the amino acid valine, and wherein, at the N-terminus, Y is selected from the group consisting of H, -CO-R 1 、-SO2-R 1 or a biotinyl group, at the C-terminus, Z is selected from OH, OR 1 、NHR 1 or NR 1 R 2 The group composed of.

[0100] In one embodiment, R 1 and R 2 Independently selected from the group consisting of alkyl, aryl, aralkyl, alkylaryl, alkoxy, sugar and aryloxy groups, which may be linear, branched, cyclic, polycyclic, unsaturated, hydroxylated, carbonylated, phosphorylated and / or sulfur-containing, the groups comprising 1 to 24 carbon atoms and being able to include one or more heteroatoms O, S and / or N.

[0101] In a preferred embodiment of the invention, the tetrapeptide is modified at the N-terminus and / or the C-terminus.

[0102] In a preferred embodiment, the tetrapeptide of the present invention is selected from the group consisting of: Y-EKGD-Z, Y-ELGD-Z, Y-EAGD-Z, Y-EIGD-Z, Y-ERGD-Z, Y-KEGD-Z, Y-KLGD-Z, Y-KAGD-Z, Y-KIGD-Z, Y-KRGD-Z, Y-LEGD-Z, Y-LKGD-Z, Y-LAGD-Z, Y-LIGD-Z In another embodiment, the tetrapeptide is selected from the group consisting of Y-EKGD-Z, Y-LKGD-Z, Y-IRGD-Z, and Y-AKGD-Z. In another embodiment, the tetrapeptide is Y-EKGD-Z. In another embodiment, the tetrapeptide is Y-LKGD-Z. In another embodiment, the tetrapeptide is Y-IRGD-Z. In another embodiment, the tetrapeptide is Y-AKGD-Z.

[0103] In a preferred embodiment of the tetrapeptide combination of the present invention, the tetrapeptide a) is selected from the group consisting of: Y-LSVD-Z, Y-LSVP-Z, Y-LSVG-Z, Y-LSDV-Z, Y-LSDP-Z, Y-LSDG-Z, Y-LSPV-Z, Y-LSPD-Z, Y-LSPG-Z, Y-LSGV-Z, Y-LSGD-Z and Y-LSGP-Z. In another embodiment, the tetrapeptide is selected from the group consisting of Y-LSVD-Z, Y-LSPG-Z and Y-LSPD-Z. In another embodiment, the tetrapeptide is Pal-LSVD-OH. In another embodiment, the tetrapeptide is Pal-LSPG-OH. In another embodiment, the tetrapeptide is Pal-LSPD-OH.

[0104] In a further preferred embodiment of the present invention, the tetrapeptide is Y-GPKG-Z. In a further preferred embodiment of the present invention, the tetrapeptide is Y-GPEG-Z. In a further preferred embodiment of the present invention, the tetrapeptide is Y-GPSG-Z.

[0105] The tetrapeptides of the present invention are preferably used in amounts of 0.1 ppm (0.00001% w / w, also referred to herein as "weight percent," "weight %" or simply by weight) to 10,000 ppm (0.5% w / w) by weight of the composition, preferably 0.5 ppm to 1000 ppm (0.05% w / w) and most preferably 1 ppm to 500 ppm.

[0106] The combination of tripeptides and tetrapeptides is particularly preferred. The preferred ratio of tetrapeptides to tripeptides, or indeed the ratio of molecules with four amino acids to molecules with three amino acids, can range from 100:1 to 1:100; more preferably 50:1 to 1:50, even more preferably 30:1 to 1:30, and even more preferably 10:1 to 1:10. Most preferably, the ratio of tetrapeptides to tripeptides ranges from 3:1 to 1:3. These ratios are based on weight (% w / w - for example mg of pure peptide per kilogram in the final formulation). In a particularly preferred embodiment, again based on the total weight of the composition, the amount of tripeptides used is greater than the amount of tetrapeptides used when their amounts are considered in parts per million. In a particularly preferred embodiment, the emulsion of the present invention comprises a combination of a tetrapeptide of the sequence Gly-Gln-Pro-Arg, its analogs and derivatives and one or more tripeptides of the sequence Gly-His-Lys, its analogs and derivatives.

[0107] Pentapeptide

[0108] The compositions of the present invention may optionally include pentapeptides, pentapeptide derivatives, and mixtures thereof. As used herein, "pentapeptide" refers to naturally occurring pentapeptides and synthetic pentapeptides. Also useful herein are naturally occurring and commercially available compositions comprising pentapeptides. Suitable pentapeptides are those selected from the group consisting of: pentapeptide 1, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 21, 22, 23, 24, 25, 26, 28, 29, 30, 31, 33, 34, 35, 36, 38, 39, derivatives thereof, and mixtures thereof.

[0109] Suitable pentapeptides for use herein are the pentapeptides lys-thr-thr-lys-ser, Arg-asp-lys-tyr-val (pentapeptide-1) and derivatives thereof. A preferred commercially available composition comprising a pentapeptide derivative is Matrixyl, which comprises 100 ppm of palmitoyl-lys-thr-thr-lys-ser and is commercially available from Sederma, France.

[0110] The pentapeptide and / or pentapeptide derivative, when present, is preferably included in the emulsion in an amount of 0.01% to 20%, more preferably 0.05% to 15%, and even more preferably 0.1% to 10% by weight of the emulsion composition.

[0111] Matrix metalloproteinase inhibitors (MMPi)

[0112] The composition of the present invention may include a matrix metalloproteinase inhibitor. The term "matrix metalloproteinase inhibitor" refers to all molecules and / or plant or bacterial extracts that have inhibitory activity on at least one of the matrix metalloproteinases expressed or synthesized by or in the skin. The matrix metalloproteinase family is formed by several well-defined groups, based on their similarities in structure and substrate specificity (Woessner JF, Faseb Journal, vol. 5, 1991, 2145). Among these groups, there are collagenases capable of degrading fibrillar collagen (MMP-1 or interstitial collagenase, MMP-8 or neutrophil collagenase, MMP-13 or collagenase 3, MMP-18 or collagenase 4), gelatinases that degrade type IV collagen or other denatured collagen forms (MMP-2 or A gelatinase (72 kDa), MMP-9 or B gelatinase (92 kDa)), stromelysins (MMP-3 or stromelysin 1, MMP-10 or stromelysin 2, MMP-11 or stromelysin 3), whose broad spectrum of activity targets proteins of the extracellular matrix, such as glycoproteins (fibronectin, laminin), proteoglycans, etc., stromelysins (MMP-7), metalloelastases (MMP-12) or metalloproteinases (MMP-14, MMP-15, MMP-16 and MMP-17). Metalloproteinases (MMPs) are proteases that use metals (mainly zinc) to coordinate with three cysteine ​​residues and methionine in their active sites, which can degrade the macromolecular components of the extracellular matrix and the basal layer (collagen, elastin, etc. ...) at neutral pH. This group of enzymes is inactivated by metal chelators. The main activity regulators of MMPs are tissue inhibitors of metalloproteinases or TIMPs such as TIMP-1, TIMP-2, TIMP-3 and TIMP-4 (Woessner JF, Faseb Journal, 1991). In addition, MMP expression is also regulated by growth factors, cytokines, oncogene products (ras, jun) or matrix components.

[0113] According to the present invention, the term "matrix metalloproteinase inhibitor" means all molecules that are capable of reducing MMP activity with respect to gene expression (transcription and translation) or with respect to activation of the MMP zymogen form or with respect to local control of the active form. In addition, the metalloproteinase inhibitor according to the present invention can also be an MMP-1 inhibitor of natural or synthetic origin. The term "natural origin" or "synthetic origin" means a metalloproteinase inhibitor in a pure state or in a solution of different concentrations, but the inhibitors referred to as natural origin are obtained from natural elements (e.g. lycopene in tomatoes) by different extraction methods, while inhibitors of synthetic origin are all obtained via chemical synthesis.

[0114] Preferred MMPi are selected from the group consisting of retinoids, N-acetylcysteine, glutathione, 2-furildioxime, vitamin C, flavonoids, isoflavones, hydrolyzed rice protein, alfalfa extract, white lupin, zizyphus jujube extract, dihydroxymethylchromone, kudzu extract, vitis vinifera extract, evening primrose extract, Anogeissus leiocarpus extract, and mixtures thereof.

[0115] When present, the MMPi is present at a level of from 0.01% to 10%, more preferably from 0.1% to 5%, and most preferably from 1% to 2.5% by weight of the composition.

[0116] Skin Conditioners

[0117] The composition of the present invention may optionally include a skin conditioning agent. The skin conditioning agent may preferably be selected from the group consisting of a moisturizer, an emollient, a moisturizer or mixtures thereof. If present, they are preferably present at a level of 0.01% to 20%, more preferably 0.1% to 10%, most preferably 0.5% to 7% by weight of the emulsion.

[0118] Preferred skin conditioning agents are selected from the group consisting of guanidine, urea, glycolic acid and glycolate salts, salicylic acid, lactic acid and lactate salts, aloe vera, shea butter, polyhydroxy alcohols such as sorbitol, mannitol, xylitol, erythritol, glycerol, hexanetriol, butanetriol, (di)propylene glycol, butylene glycol, hexylene glycol, polyethylene glycol, sugars (e.g. fructose, glucose, xylose, honey, mannose, xylose), gluconolactone and starch and its derivatives, pyrrolidones, carboxylic acids, hyaluronic acid and its salts, lactamide monoethanolamine, acetamide monoethanolamine, panthenol, allantoin and mixtures thereof.

[0119] The composition may include hyaluronic acid or a salt thereof, such as sodium hyaluronate or potassium hyaluronate. The composition preferably includes sodium hyaluronate.

[0120] Specifically, the amount of hyaluronic acid or a salt thereof (eg, sodium hyaluronate) present in the composition may be 0.01% to 0.2% or 0.03% to 0.1% by weight.

[0121] More preferably, the skin conditioning agent is selected from glycerin, arabinogalactan, butylene glycol, hyaluronic acid, shea butter, propylene glycol, ethylhexylglycerin and hyaluronate.

[0122] Vitamins

[0123] The composition of the present invention may include one or more vitamins. The composition may include ascorbic acid, such as vitamin C, vitamin C derivatives, ascorbic acid, ascorbyl glucoside, ascorbyl palmitate, magnesium ascorbyl phosphate, sodium ascorbyl phosphate and ethyl ascorbate. The composition may include vitamin B, vitamin B derivatives, vitamin B1 to vitamin B12 and derivatives thereof. In another embodiment, the composition includes the vitamin B3 derivative niacinamide.

[0124] In an alternative embodiment of the present cosmetic composition, the cosmetic composition includes vitamin K, vitamin K derivatives, vitamin H, vitamin D, vitamin D derivatives, and mixtures thereof. In an alternative embodiment of the present cosmetic composition, the cosmetic composition includes vitamin E, vitamin E derivatives such as tocopherol and tocopherol acetate, and provitamins thereof such as panthenol and mixtures thereof.

[0125] In other embodiments, the cosmetic composition includes retinoid compounds, including retinoic acid, retinal, retinol and derivatives thereof. In one embodiment, the cosmetic composition includes retinyl palmitate, retinyl acetate, retinyl retinoate, retinyl propionate, retinyl ascorbate, retinyl linoleate, retinyl retinoate, retinyl sunflower acid and mixtures thereof.

[0126] The vitamin compound can be included as a substantially pure material or as an extract obtained by suitable physical and / or chemical isolation from a natural (e.g., plant) source. In one embodiment, when the vitamin compound is present in the composition of the present invention, the emulsion composition comprises about 0.0001% to 50%, more preferably 0.001% to 10%, still more preferably 0.01% to 8%, and still more preferably 0.1% to 5% of the vitamin compound by weight of the composition.

[0127] Sunscreen

[0128] The compositions of the present invention may optionally include a sunscreen component. Sunscreens may include organic or inorganic sun filters or a combination of both. Suitable inorganic filters include those selected from the group consisting of ultrafine titanium dioxide, ultrafine zinc oxide, boron nitride and mixtures thereof.

[0129] Suitable organic sunscreens include those selected from the group consisting of: a) p-aminobenzoic acid, their esters and derivatives (e.g., 2-ethylhexyl p-dimethylaminobenzoate), b) methoxycinnamate esters (e.g., 2-ethylhexyl p-methoxycinnamate, 2-ethoxyethyl p-methoxycinnamate or a,p-di-(p-methoxycinnamoyl)-a'-(2-ethylhexanoyl)-glycerol, c) benzophenones (e.g., oxybenzone), d) dibenzoylmethanes such as 4-(tert-butyl)- )-4'-methoxydibenzoylmethane, e) 2-phenylbenzimidazole-5 sulfonic acid and its salts, f) alkyl-ss,ss-diphenylacrylates, for example alkyl α-cyano-ss,ss-diphenylacrylates, such as octocrylene, g) triazines, such as 2,4,6-trianilino-(p-carbo-2-ethyl-hexyl-1-oxy)-1,3,5 triazine, h) camphor derivatives such as methylbenzylidene camphor and i) mixtures thereof. Other preferred sunscreen ingredients include those selected from the group consisting of: homosalate, ethylhexyl salicylate, diethylhexyl butyramido triazone, bis-ethylhexyloxyphenol methoxyphenyl triazine, diethylaminohydroxybenzoyl hexyl benzoate, butyl methoxydibenzoylmethane, methylene bis-benzotriazolyl tetramethylbutylphenol, polysilicone-15 and mixtures thereof. Sunscreens are optionally present in amounts of 0.1 to 10% by weight of the composition.

[0130] Other optional ingredients

[0131] The composition of the present invention may also optionally include one or more of the following optional ingredients. Preservatives may be added to the emulsion, such as 2-bromo-2-nitropropane-1,3-diol (bronopol, which is commercially available under the trade name Myacide RTM), benzyl alcohol, bis(hydroxymethyl)imidazolidinyl urea, imidazolidinyl urea, methylparaben, phenoxyethanol, ethylparaben, propylparaben, sodium methylparaben, sodium dehydroacetate, polyhexamethylene biguanide hydrochloride, isothiazolones and sodium propylparaben, suitably in an amount of 0.01% to 10% by weight of the emulsion.

[0132] Thickeners, viscosity modifiers and / or gelling agents may be added to the emulsion composition, such as acrylic acid polymers, for example commercially available under the trade names Carbopol, Pemulen or Ultrez (Lubrizol), or modified celluloses, for example hydroxyethylcellulose (commercially available under the trade name Natrosol (Hercules)) or hydroxypropyl methylcellulose, amine oxides, block polymers of ethylene oxide and propylene oxide (for example, available under the trade name Pluronic" RTM from BASF Wyandotte), PVM, MA, or decadiene crosspolymers (available under the trade name Stabilez 60), ethoxylated fatty alcohols, salts (magnesium chloride, sodium chloride), Aristoflex AVC (Clariant), phthalic acid amides, xanthan gum, sodium polyacrylate, polyvinyl alcohol, fatty alcohols and alkyl galactomannans, available under the trade name N-Hance from Hercules, suitable amounts being from 0.5% to 10% by weight of the composition.

[0133] Chelating agents may be added to the emulsion composition, such as ethylenediaminetetraacetic acid and its salts, suitably in an amount of 0.005% to 0.5% by weight of the composition.

[0134] The composition may also include a wax, such as cocoa butter, suitably in an amount of from 1% to 99% by weight of the composition.

[0135] The composition may also include a suitable, cosmetically acceptable diluent, carrier and / or propellant such as dimethyl ether.

[0136] The composition may also include a pearlising agent, such as stearic acid monoethanolamide and / or mica, suitably in an amount of 0.01% to 10% by weight of the composition.

[0137] Perfumes may suitably be added in amounts of 0.01% to 2% by weight of the composition, and water-soluble dyes such as tartrazine may also suitably be added in amounts of trace amounts (such as 1 x 10-5%) to 0.1% by weight of the composition.

[0138] The composition may also include a pH regulator, such as sodium hydroxide, aminomethyl propanol, triethanolamine, in an amount of 0.01% to 10% by weight of the composition. The composition may be buffered in a manner well known in the art, for example by using a buffer system comprising succinic acid, citric acid, lactic acid and acceptable salts thereof, phosphoric acid, monosodium phosphate or disodium phosphate and sodium carbonate. Suitably, the composition may have a pH between 3 and 10, preferably between 4 and 8.

[0139] method

[0140] Perimenopause and postmenopausal skin show a decrease in the quality of the skin barrier function and an increase in inflammation. Interleukin 8 is a measurable biomarker of inflammation. The effectiveness of the currently described composition in reducing inflammation and promoting skin barrier repair was evaluated by measuring the reduction in interleukin-8 (IL-8) expression in the tested skin cells. Overexpression of IL-8 in the epidermis can lead to the destruction of epidermal homeostasis, i.e., the destruction of skin cell differentiation, proliferation and desquamation processes. The process is essential for maintaining epidermal homeostasis and a healthy epidermal skin barrier. The reduction in IL-8 expression indicates a reduction in inflammation, and therefore reduces the disorder of epidermal homeostasis and skin barrier function.

[0141] In this experiment, the effects of the compounds were evaluated in normal human epidermal keratinocytes (NHEK). More specifically, the effects of these compounds were evaluated using real-time polymerase chain reaction (RT-qPCR) technology. A PCR array designed by Bioalternatives for analyzing 32 target genes (including 2 housekeeping genes) was used to determine the gene expression pattern in NHEK cells by using RNA (mRNA) extracted from treated and control cells.

[0142] Normal human epidermal keratinocytes (NHEK) were seeded in 24-well plates and placed in culture medium (keratinocyte-serum-free medium (SFM) supplemented with epidermal growth factor at a concentration of 0.025 ug / ml and pituitary extract at a concentration of 0.05 mg / ml) for 24 hours. In order to determine the appropriate concentration of non-toxic ingredients, a cytotoxicity assay was first performed, in which NHEK were first treated with ingredients or ingredient blends for 24 hours and then incubated with WST-8 (a highly water-soluble tetrazolium salt), which was reduced by surviving living cells to a water-soluble orange product (formazan) and quantified by optical density measurement at 450 nm using a spectrophotometer (VERSAmax, Molecular Devices). This reduction is proportional to the number of living cells and their metabolic activity.

[0143] For RT-qPCR studies, NHEKs were incubated in culture medium for 24 hours, then the culture medium was removed and replaced with assay medium alone (keratinocyte-SFM) as a negative control, or with assay medium containing the test compound, and the cells were then incubated for 24 hours. The experiments were performed in triplicate. After incubation, the cells were washed in phosphate-buffered saline (PBS) solution and immediately frozen at -80°C.

[0144] IL-8 mRNA expression was analyzed using RT-qPCR as part of the array. Total mRNA was extracted from each sample using TriPure separation reagent (trade name) according to the supplier's instructions (Sigma-Aldrich). The amount and quality of mRNA were evaluated using capillary electrophoresis using a Bioanalyzer 2100 (Agilent technologies). Prior to reverse transcription, the mRNA was analyzed using a Chemagic PCR kit commercially available from Perkin Elmer. TM The mRNA Direct kit is used to purify mRNA. Complementary DNA (cDNA) is synthesized by reverse transcription of total mRNA or mRNA in the presence of oligo (dT) and transcriptor reverse transcriptase (trade name, commercially available from Roche). If necessary, the amount of cDNA is then diluted to obtain equal cDNA concentrations in each test sample, and then PCR (polymerase chain reaction) is performed using the LightCycler (trade name) system (commercially available from Roche Molecular System Inc.) according to the supplier's instructions. The reaction mixture (final 10 μl) is prepared as follows: -2.5 μl of cDNA, -primers (forward and reverse), -a reagent mixture containing taq DNA polymerase, SYBR Green I (asymmetric cyanine dye-Thermo Fisher Scientific) and MgCl2. SYBR Green is a DNA fluorescent dye that binds to a specific groove of the DNA / cDNA molecule. When a laser is directed at it, it emits light, providing a measurable marker. The more copies of DNA / cDNA produced by PCR, the more SYBR Green molecules bound to DNA / cDNA and the higher the fluorescence level. Due to the use of specific primers, only IL-8 cDNA is amplified, and therefore the number of cDNA copies produced after each round of PCR amplification is proportional to the amount of cDNA / mRNA initially present in the cell. During the PCR cycle, the fluorescence incorporation in the amplified cDNA is continuously measured to provide "fluorescence intensity", which allows the evaluation of the relative expression (RE) value of the IL-8 RNA of the cells treated with the test compound compared to the cells treated with the medium alone / negative control.

[0145] result

[0146] Preliminary cytotoxicity studies allowed us to determine the maximum concentration that each tested ingredient / complex could be used without causing loss of viability or death of epidermal keratinocytes. Ophiopogon and niacinamide could be used at a maximum concentration of 500 ppm (0.05%) each, while soy could only be used at a maximum concentration of 10 ppm (0.001%). For the complex, concentrations of 15 ppm (0.0015%) Ophiopogon, 10 ppm (0.001%) soy and 2.5 ppm (0.00025%) niacinamide were used. Despite the use of relatively high concentrations, Ophiopogon itself had no effect on the expression of IL-8-mRNA. On the other hand, when niacinamide was used alone, the expression of IL-8 mRNA increased by 18%, rather than decreased. Soy was the most effective of the three tested ingredients, reducing IL-8 mRNA expression by 43% when used alone. Surprisingly, when the three ingredients were tested together in the form of a complex, the anti-inflammatory effect of soy was further enhanced, reducing IL-8-mRNA by 62%. The mechanism behind this experimental synergy is still unclear. While not wishing to be bound by theory, it is hypothesized that nicotinamide and Ophiopogon japonicus may modify histones such that soy isoflavones more frequently upregulate the IL-8 gene.

[0147]

[0148] Representative Composition Examples

[0149] The composition examples of the present invention are not meant to be limiting.

[0150] Example 1 - Water-in-oil emulsion

[0151]

[0152] Manufacturing method

[0153] In the main container add Dimethicone, Dimethicone Crosspolymer, PEG / PPG-18 / 18 Dimethicone & Polyglyceryl-4 Isostearate & Hexyl Laurate and Cetyl PEG / PPG-10 / 1 Dimethicone to create the oil phase.

[0154] 1. Weigh water, magnesium sulfate, glycerin, phenoxyethanol, caprylyl glycol, ethylhexylglycerin, niacinamide, ophiopogon root extract, water, soy isoflavones, genistein, water, and lecithin, and stir until the solids are dissolved to prepare an aqueous phase.

[0155] 2. Slowly add the water phase to the oil phase while continuing to stir at high speed (create a vortex). Continue stirring for 5 minutes.

[0156] 3. Homogenize the product using a Silverson mixer or equivalent at 3500 rpm for 5 minutes.

[0157] Example 2 - Oil-in-water emulsion

[0158]

[0159]

[0160] Manufacturing method

[0161] 1. Add glycerin to water and dissolve tetrasodium EDTA.

[0162] 2. Use a homogenizing spray on the xanthan gum and continue homogenizing for 5 minutes or until hydrated.

[0163] 3. Heat the water phase to 70-75°C.

[0164] 4. Weigh the oil phase in a separate container and heat to 70-75°C. (Dimethicone, Cetearyl Alcohol, Octyldodecanol, Glyceryl Stearate and PEG-100 Stearate) Add Ammonium Acryloyldimethyltaurate / VP Copolymer and Aluminum Starch Octenylsuccinate under stirring at a certain temperature.

[0165] 5. When both phases are at 70-75°C, add the oil phase to the water phase and homogenize for 2 minutes.

[0166] 6. Add Dimethicone Crosspolymer & Dimethicone and homogenize for 2 minutes.

[0167] 7. Cool to room temperature.

[0168] 8. Stir in phenoxyethanol & caprylyl glycol & ethylhexylglycerin, Ophiopogon japonicus root extract & water and soy isoflavones & genistein & water & lecithin.

[0169] 9. Dissolve niacinamide in a small amount of water and stir to make a stock solution.

[0170] 10. Make up to weight with water and mix well.

[0171] Example 3 - Oil-in-water emulsion containing sunscreen

[0172]

[0173]

[0174] Manufacturing method

[0175] 1. Add glycerin to water and dissolve tetrasodium EDTA.

[0176] 2. Using a homogenizing action, disperse the Carbomer and continue homogenizing for 5 minutes or until hydrated.

[0177] 3. Heat the water phase to 70-75°C.

[0178] 4. Weigh the oil phase in a separate container and heat to 70-75°C. (Dimethicone, Cetearyl Alcohol, Glyceryl Stearate & PEG-100 Stearate, C12-15 Alkyl Benzoate, Butyl Methoxydibenzoylmethane, Ethylhexyl Methoxycinnamate, PEG-20 Stearate)

[0179] 5. When both phases are at 70-75°C, add the oil phase to the water phase and homogenize for 2 minutes.

[0180] 6. Add potassium hydroxide and homogenize for 2 minutes.

[0181] 7. Cool to room temperature.

[0182] 8. Stir in phenoxyethanol & caprylyl glycol & ethylhexylglycerin and ophiopogon japonicus root extract & water and soy isoflavones & genistein & water & lecithin.

[0183] 9. Dissolve niacinamide in a small amount of water and stir to make a stock solution.

[0184] 10. Make up to weight with water and mix well.

[0185] Example 4 - Gel

[0186]

[0187] Manufacturing method

[0188] 1. Add glycerin and propylene glycol to water and dissolve tetrasodium EDTA.

[0189] 2. Use a homogenizing spray in the Acrylates / C10-30 Alkyl Acrylate Crosspolymer and continue homogenizing for 5 minutes or until hydrated.

[0190] 3. Stir in potassium hydroxide to form a gel.

[0191] 4. Stir in phenoxyethanol & caprylyl glycol & ethylhexylglycerin, ophiopogon root extract & water, and ophiopogon root extract & water.

[0192] 5. Dissolve niacinamide in a small amount of water and stir to make a stock solution.

[0193] 6. Make up to weight with water and mix well.

[0194] Example 5 - Detergent Washing

[0195]

[0196] Manufacturing method

[0197] 1. Add tetrasodium EDTA and sodium chloride to water.

[0198] 2. Stir in sodium laureth sulfate, cocamidopropyl betaine, and cocamide DEA.

[0199] 3. Dissolve sodium benzoate in a small amount of water and stir to make a stock solution.

[0200] 4. Stir in Ophiopogon japonicus root extract & water and soy isoflavones & genistein & water & lecithin.

[0201] 5. Dissolve niacinamide in a small amount of water and stir to make a stock solution.

[0202] 6. Add sodium hydroxide and citric acid to achieve the desired pH.

[0203] 7. Make up the weight with water and mix well

[0204] The terms "phytogenic isoflavones" and "phytoestrogen isoflavones" are referred to herein. While "phytogenic isoflavones" are plant-derived isoflavones, and "phytoestrogen isoflavones" are specific expressions of plant-derived isoflavones that have estrogen-like properties (i.e., are able to modulate estrogen receptors), these materials are virtually the same. This is because all plant-derived isoflavones are phytoestrogens (strong or weak), and therefore plant-derived isoflavones are phytoestrogens (see the following references, as described in the following references - Pilsakova L, Riecansky I, Jagla F. The physiological actions of isoflavone phytoestrogens. Physiol Res. 2010; 59(5): 651-664. doi: 10.33549 / physiolres.931902. Epub 2010 Apr 20. PMID: 20406033; Desmawati D, Sulastri D. Phytoestrogens and Their Health Effect. Open Access Maced JMed Sci.2019Feb14;7(3):495-499.doi:10.3889 / oamjms.2019.044.PMID:30834024; PMCID:PMC6390141; and Zuite A. Proanthocyanidin: Chemistry and Biology: From Phenolic Compounds toProanthocyanidins.2014.doi::10.1016 / B978-0-12-409547-2.11046-7).

[0205] Additional details of some commercially available materials sold under identified trademarks are provided below.

[0206] Commercially available materials list

[0207]

[0208]

[0209] List of commercially available plant extracts

[0210]

[0211]

[0212]

Claims

1. A cosmetic composition suitable for application to menopausal skin, the composition comprising an Ophiopogon japonicus extract and plant-derived isoflavones.

2. The composition according to claim 1, wherein The extract is obtained from the root of the Ophiopogon japonicus plant.

3. A composition according to any one of the preceding claims, wherein The Ophiopogon japonicus extract includes a steroidal glycoside called Ophiopogon japonicus saponin D (OP-D).

4. A composition according to any one of the preceding claims, wherein The phytoestrogen isoflavones are derived from phytoestrogen plants selected from the group consisting of soybean (Glycine max), red clover (Trifolium pratense), white clover (Trifolium repens), alfalfa (Medicago sativa), garlic (Allium sativum), celery (Apiaceaegraveolens), carrot (Daucus carota), potato (Solanum tuberosum), rice (Oryza sativa), wheat (Trwiticum aestivum), sweet potato (Ipomoeabatatas), apple (Malus domestica), pomegranate (Punica granatum), chasteberry (Vitex agnus-castus), coffee (Coffea arabica), arabica and robusta coffee (Coffearobusta) and their blends.

5. A composition according to any one of the preceding claims, wherein The phytoestrogen isoflavones are derived from a phytoestrogen plant selected from the group consisting of soybean (Glycinemax), red clover (Trifolium pratense), white clover (Trifolium repens), alfalfa (Medicago sativa), and mixtures thereof.

6. A composition according to any one of the preceding claims, wherein The plant-derived isoflavones are derived from soybeans.

7. A composition according to any one of the preceding claims, wherein The phytoestrogen isoflavones are selected from the group consisting of glycosylated isoflavones (also known as soy isoflavone glycosides) and deglycosylated isoflavones.

8. A composition according to any one of the preceding claims, wherein The phytoestrogen isoflavones are selected from the group consisting of daidzein, genistein, glycitein, malonyl daidzein, malonyl genistein, malonyl glycitein, acetyl daidzein and acetyl glycitein, daidzein, genistein, glycitein and mixtures thereof.

9. A composition according to any one of the preceding claims, wherein The phytoestrogen isoflavones are selected from the group consisting of: genistein (5,7,4'-trihydroxy-isoflavone), genistein (5,7,4'-trihydroxy-isoflavone-7-glucoside), daidzein (7.4'-dihydroxy-isoflavone), equol (4',7-dihydroxy-isoflavane), daidzein (7.4'-dihydroxy-isoflavone-7-glucoside), biochanin A (5.7-dihydroxy-4'-methoxy-isoflavone), glycitein (7 .4'-dihydroxy-6-methoxy-isoflavone), glycitin (7.4'-dihydroxy-6-methoxy-isoflavone-7-glucoside), olopol (5.3',4'-trihydroxy-7-methoxy-isoflavone), olopol (5,7,3',4'-tetrahydroxy-isoflavone), santal (5,7,3'-trihydroxy-4'-methoxy-isoflavone) and / or enzyme inhibitors (5.4'-dihydroxy-7-methoxy-isoflavone) and mixtures thereof.

10. A composition according to any one of the preceding claims, wherein The phytoestrogen isoflavones are present at a level of 0.001 to 20% by weight of the composition.

11. A composition according to any one of the preceding claims, wherein The phytoestrogen isoflavones are present at a level of 0.01 to 5% by weight of the composition.

12. A composition according to any one of the preceding claims, wherein The Ophiopogon japonicus extract and the phytoestrogen isoflavones are present in a ratio of 5:1 to 1:

2.

13. A composition according to any one of the preceding claims, wherein The composition also includes vitamin B or a vitamin B derivative.

14. The composition according to claim 13, wherein The vitamin B or vitamin B derivative is selected from nicotinic acid esters, including non-vasodilating nicotinic acid esters, nicotinyl amino acids, nicotinyl alcohol esters of carboxylic acids, nicotinic acid N-oxide, nicotinamide N-oxide and mixtures thereof.

15. The cosmetic composition according to claim 13 or 14, wherein The vitamin B or vitamin B derivative is selected from: C1-C22 straight or branched, cyclic or acyclic, saturated or unsaturated (including aromatic) and substituted or unsubstituted nicotinic acid esters, nicotinyl amino acids, nicotinyl glycine, nicotinyl hydroxamic acid, nicotinyl alcohol esters of carboxylic acids (including salicylic acid, acetic acid, glycolic acid, palmitic acid), 2-chloronicotinamide, 6-aminonicotinamide, 6-methylnicotinamide, n-methyl-nicotinamide, n,n-diethylnicotinamide, n-(hydroxymethyl)-nicotinamide, quinolinic acid imide, nicotinanilide, n-benzylnicotinamide, n-ethylnicotinamide, nifenazone, nicotinaldehyde, isonicotinic acid, methylisonicotinic acid, thionicotinamide, nyalamid, 1-(3-pyridylmethyl)urea, 2-mercaptonicotinic acid, nicotinamide, niprazine, nicotinamide, tocopherol nicotinate and mixtures thereof.

16. The cosmetic composition according to any one of claims 13 to 15, wherein The vitamin B or vitamin B derivative is niacinamide.

17. A method of cosmetically treating the skin by applying a composition according to any one of the preceding claims.

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