WO2023109289A1 - 包含植物果油和植物籽油的组合物及其应用 - Google Patents

包含植物果油和植物籽油的组合物及其应用 Download PDF

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WO2023109289A1
WO2023109289A1 PCT/CN2022/125277 CN2022125277W WO2023109289A1 WO 2023109289 A1 WO2023109289 A1 WO 2023109289A1 CN 2022125277 W CN2022125277 W CN 2022125277W WO 2023109289 A1 WO2023109289 A1 WO 2023109289A1
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oil
seed oil
fruit
skin
vegetable
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PCT/CN2022/125277
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English (en)
French (fr)
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殷庆飞
张瑶瑶
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上海家化联合股份有限公司
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/92—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof
    • A61K8/922—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof of vegetable origin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/23—Apiaceae or Umbelliferae (Carrot family), e.g. dill, chervil, coriander or cumin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/28—Asteraceae or Compositae (Aster or Sunflower family), e.g. chamomile, feverfew, yarrow or echinacea
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/28—Asteraceae or Compositae (Aster or Sunflower family), e.g. chamomile, feverfew, yarrow or echinacea
    • A61K36/286—Carthamus (distaff thistle)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/32—Burseraceae (Frankincense family)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/42—Cucurbitaceae (Cucumber family)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/52—Juglandaceae (Walnut family)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/53—Lamiaceae or Labiatae (Mint family), e.g. thyme, rosemary or lavender
    • A61K36/534—Mentha (mint)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/53—Lamiaceae or Labiatae (Mint family), e.g. thyme, rosemary or lavender
    • A61K36/535—Perilla (beefsteak plant)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/54—Lauraceae (Laurel family), e.g. cinnamon or sassafras
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/67—Piperaceae (Pepper family), e.g. Jamaican pepper or kava
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/73—Rosaceae (Rose family), e.g. strawberry, chokeberry, blackberry, pear or firethorn
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/73—Rosaceae (Rose family), e.g. strawberry, chokeberry, blackberry, pear or firethorn
    • A61K36/736—Prunus, e.g. plum, cherry, peach, apricot or almond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/75—Rutaceae (Rue family)
    • A61K36/752—Citrus, e.g. lime, orange or lemon
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/81—Solanaceae (Potato family), e.g. tobacco, nightshade, tomato, belladonna, capsicum or jimsonweed
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/87—Vitaceae or Ampelidaceae (Vine or Grape family), e.g. wine grapes, muscadine or peppervine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/88—Liliopsida (monocotyledons)
    • A61K36/889—Arecaceae, Palmae or Palmaceae (Palm family), e.g. date or coconut palm or palmetto
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
    • A61K2800/59—Mixtures
    • A61K2800/592—Mixtures of compounds complementing their respective functions
    • A61K2800/5922—At least two compounds being classified in the same subclass of A61K8/18

Definitions

  • the invention belongs to the field of cosmetics, in particular to a composition containing plant fruit oil and plant seed oil and its application in skin barrier function.
  • Skin barrier broadly includes physical barrier, pigment barrier, nerve barrier, and immune barrier.
  • the narrow sense of the skin barrier mainly refers to the physical barrier, and the skin barrier we usually talk about is a physical barrier.
  • the physical barrier is composed of sebum film, stratum corneum keratin, lipid, "sandwich” structure, brick wall structure, dermal mucopolysaccharides, mucopolysaccharides, etc., to resist external harmful substances, irritants, and sunlight. Moisturizing and regulating anti-inflammatory effect.
  • the basic function of sebum is to moisturize and moisturize, and its weak acidity can also exert a certain antibacterial effect. Sebum forms a "sebum film" on the surface of the skin and is the skin's natural moisturizer.
  • Sebum contains triglycerides, free fatty acids, wax esters, squalene and other components.
  • the sebum film can be rebuilt on the skin surface by applying moisturizing cream, which can effectively isolate external stimuli and prevent Loss of skin moisture.
  • oils can be mainly divided into: vegetable oils, animal oils, mineral oils and synthetic oils.
  • Vegetable oils are skin-friendly, close to the structure of human sebum membrane, with good permeability, deep penetration and nourishment. The skin is favored by many skin care products.
  • Vegetable oils used in cosmetics mainly come from plant fruits, seeds and germs, and some come from other parts of plants such as leaves, bark, roots, petals and stamens.
  • Oils containing plant fruits mainly include avocado tree (Butyrospermum parkii) fruit butter (also known as shea butter), olive (Olea europaea) fruit oil (also known as olive oil), apricot (Prunus armeniaca) kernel oil (also known as sweet almond oil) oil), avocado (Persea gratissima) Oil, Seabuckthorn (Hippophae rhamnoides) Oil, coconut (Cocos nucifera) Oil, Orange (Citrus junos) Oil, Bergamot (Citrus aurantium bergamia) Oil, Citron ( Citrus bedica limonum) fruit oil, tomato (Solanum lycopersicum) fruit oil, dog tooth rose (Rosa canina) fruit oil, etc.
  • avocado tree Butyrospermum parkii) fruit butter (also known as shea butter), olive (Olea europaea) fruit oil (also known as olive oil), apricot (Prunus armeniaca) kernel oil (also known as sweet
  • Oils containing plant seeds mainly include jojoba (Simmondsia chinensis) seed oil, safflower (Carthamus tinctorius) seed oil, white pond flower (Limnanthes alba) seed oil, sunflower (Helianthus annuus) seed oil, macadamia nut (Macadamia ternifolia) seed oil , Castor Bean (Ricinus communis) Seed Oil, Peony (Paeonia suffruticosa) Seed Oil, Grape (Vitis vinifera) Seed Oil, Grapefruit (Citrus paradisi) Seed Oil, Apple (Pyrus malus) Seed Oil, Pomegranate (Punica granatum) Seed Oil , watermelon (Citrullus lanatus) seed oil, zucchini (Cucurbita pepo) seed oil, flax (Linum usitatissimum) seed oil, rapeseed (Brassica campestris) seed oil, sesame (Se
  • Shea butter is directly extracted from the fruit of the African shea tree. It is soft and smooth in texture. It is the most effective natural moisturizing product and has been widely used in the field of cosmetics.
  • shea butter can also be used in lipstick, lip gloss and sunscreen products. It has good adhesion, softness and non-greasy, and can help increase the SPF value of the sun protection factor.
  • shea butter can also be obtained by fractionating edible oil shea butter, for example: Literature Huang Xianxiao, Research on the extraction process of biologically active substances in shea butter oil, China Oils and Fats [J], 2015,40(4):69 -73 proposes that shea butter can be used as a substitute for cocoa butter to make chocolate and candy, etc.
  • Olive oil is a natural oil extracted from olive fresh fruit by appropriate methods, and it is widely used in medicine and daily chemical industries.
  • the literature Ma Xiaoyuan Research Progress on the Efficacy of Natural Vegetable Oils in Sunscreen Cosmetics, China Oils and Fats [J], 2021, 46(1): 71-75, proposed that the polyphenols contained in olive oil have the ability to absorb ultraviolet rays and resist oxidation. It can also eliminate facial wrinkles and prevent skin aging.
  • Jojoba oil has a very significant cosmetic effect on the skin. It can unblock the pores, regulate the oil secretion of oily or mixed skin, and improve inflamed skin, eczema, psoriasis, acne, etc. For dry hair and dry hair Wrinkled skin can restore vitality and radiance, so it is a base oil that can be used for all skin types.
  • the literature Li Chunxia, Application of Jojoba Oil in Cosmetics, Daily Chemical Science [J], 2007, 30 (2) pointed out that Jojoba oil can significantly reduce epidermal moisture by incompletely blocking the evaporation of gas and water
  • it has the functions of easy spreading and lubricating, making the skin smooth and elastic.
  • Safflower seed oil contains 6% saturated fatty acid, 21% oleic acid and 73% linoleic acid. Because its main component is linoleic acid, which is the oil with the highest linoleic acid in food oils, it has high nutritional value and has attracted much attention in medicine, food and cosmetics.
  • linoleic acid which is the oil with the highest linoleic acid in food oils, it has high nutritional value and has attracted much attention in medicine, food and cosmetics.
  • the literature Baoleer the research progress of safflower seed oil, World Latest Medicine Information (Electronic Version) [J], 2021, 21(27): 146-148 pointed out that safflower seed oil has antioxidant effect and can Effectively scavenges free radicals and restores the ability of free radicals caused by chemical factors, and also has anti-aging effects.
  • Literature Jiang Li Analysis of the Efficacy and Application Prospect of Safflower Seed Oil, Agricultural Product Processing [J], 2017, 6:56-58 pointed out that long-term consumption of safflower seed oil can effectively prevent atherosclerosis, reduce blood lipids and serum cholesterol content, soften blood vessels, and indirectly restore the nervous system and other medicinal functions.
  • White Pond Seed Oil is one of the most stable vegetable oils known, due to the presence of natural antioxidant tocopherols.
  • the analysis of trace components in several high oxidation stability vegetable oils and their anti-ultraviolet and antioxidant properties, fragrance, fragrance and cosmetics [J], 2019, 4: 47-51 detected the growth of baicalensis flower seed oil
  • the content of phenol and its anti-oxidation performance, through the removal of DPPH it shows that the white pond flower seed oil has certain anti-oxidation properties, can prevent ultraviolet rays, promote skin microvascular circulation, and make the face naturally rosy and energetic.
  • Rice bran oil is a nutrient-rich vegetable oil rich in unsaturated fatty acids, octacosanol, ⁇ -oryzanol, phytosterols, tocotrienols, squalene and other functional substances. Rice bran oil contains 40-50% oleic acid, 29-42% linoleic acid, 1% linolenic acid and 12-20% palmitic acid. Rice bran oil is highly processed and is widely used in cosmetics, including cosmetics such as washing products, sun protection, anti-aging products and dermatological treatments.
  • acetylated rice bran oil is easy to form long-lasting water-resistant protection Film, with softening and conditioning functions, can be used as a liquid softener in hand or body lotions, and can also be used in shampoo and hair care products to make hair soft and shiny.
  • Sunflower seed oil contains more than 40% unsaturated fatty acids, including 38% oleic acid and about 55% linoleic acid. Its linoleic acid content far exceeds that of peanut oil and sesame oil, and is easily absorbed by the human body. It is regarded as a high-quality oil in the world .
  • the literature Zhao Furong, sunflower seed oil production and comprehensive utilization, China Oils and Fats [J], 2005, 30(1): 9-13 proposed that the ratio of vitamin E and unsaturated fatty acids in sunflower seed oil is relatively balanced, which is beneficial to the human body.
  • Anti-lipid peroxidation protection when taking unsaturated fatty acids it can also effectively reduce serum cholesterol levels, and has the effect of lowering blood pressure. It is a good raw material for cooking, margarine, shortening, mayonnaise and salad oil. .
  • the skin barrier generally refers to the physical barrier of the skin, including the stratum corneum of the skin epidermis and the sebum film on the surface of the stratum corneum.
  • the stratum corneum is the outermost layer of the epidermis and has a "brick-wall structure", where "bricks” refer to corneocytes and "mortar” refers to intercellular lipids.
  • bricks refer to corneocytes
  • mortar refers to intercellular lipids.
  • barrier factors filaggrin FLG
  • loricrin LOR
  • IVL endothelin
  • TGM1 transglutaminase 1
  • TGM1 barrier moisturizing-related factors caspase 14
  • HMGCoA reductase HMGCR
  • AQP3 aquaporin 3
  • ZO-1 keratinocyte intercellular junction-associated factor zona occlusin 1
  • filaggrin FLG is an important constituent protein of the cornified envelope of the outer layer of the skin epidermis, mainly present in the granular layer and transparent layer of the epidermis, and is an important component of the skin barrier; Hydrophilic free amino acids and water-absorbing derivatives help the skin store moisture, maintain skin moisture, and have moisturizing effects.
  • Loricrin LOR
  • Indothelin IVL is mainly expressed in the upper part of the spinous cell layer and the granular layer. It is a marker protein for keratinocyte differentiation. Lipid matrix and keratinocytes are connected to function.
  • TGM1 transglutaminase 1
  • HMGCoA reductase is the rate-limiting enzyme for synthesizing cholesterol. It exists in the endoplasmic reticulum and catalyzes the synthesis of methyldivalenic acid. Afterwards, it undergoes multi-step reactions such as decarboxylation and phosphorylation to generate squalene, and finally squalene is cyclized into wool. sterols are converted to cholesterol. Aquaporin 3 (AQP3) is the most abundant subtype of aquaporin in the AQPs family.
  • Its expression in the epidermis has a spatial hierarchy, mainly expressed in the basal layer of the human epidermis, the spinous cell layer, and the granular layer, and gradually disappears in the stratum corneum .
  • This spatial distribution is consistent with the water content distribution of the skin: the basal and suprabasal layers are about 75% water, while the stratum corneum is only about 10%-15%.
  • the high expression of AQP3 in the basement membrane zone can promote the transport of water, glycerol and urea, making the extracellular environment of the basal layer closer to a neutral equilibrium state; the closer to the stratum corneum, the lower the expression of AQP3, and the lower the water content. The decline is obvious, and the internal environment of the skin gradually becomes acidic.
  • AQP3 plays an important role in the transport of glycerol in the stratum corneum. AQP3 transports endogenous glycerin and triglycerides in the sebaceous glands into the epidermis, making it directly or indirectly affect the moisturizing effect of the skin.
  • Tight junctions are an important part of the physical barrier, mostly appearing in the epidermis of the skin, located on the top side of the gap between adjacent cells. Tight junctions are composed of different types of transmembrane proteins as well as intracellular cytoplasmic proteins. Transmembrane proteins such as water gate protein 1 (CLDN1), occlusion protein (OCLN), etc.; cytoplasmic proteins such as zonular occlusion protein-1 (ZO-1) and so on.
  • ZO-1 is a cytoplasmic protein that belongs to the family of membrane-linked guanylate kinase proteins. It gathers occludins and waterlock proteins through extracellular signal transduction pathways to form basic cell junction strips; ZO-1 is a protein in the skin barrier function. One of the most characterized cytoplasmic proteins.
  • Plant bionic lipid technology (Phyto Bionic Sebum, referred to as PBS technology): select a variety of natural vegetable oils, through scientific proportioning, to simulate the natural lipid components in the skin barrier structure, to supplement the essential unsaturated fatty acids in the stratum corneum of the skin, such as flax Acid, linoleic acid, etc., supplement the lipid components that the skin lacks, and are compatible with sebum, so as to quickly repair the skin barrier and restore the skin to a healthy, moist and shiny state.
  • PBS technology Plant bionic lipid technology
  • vegetable oil mainly comes from including but not limited to plant fruits (for example: shea butter, olive oil, almond oil, avocado fruit oil, sea buckthorn fruit oil, coconut fruit oil, orange fruit oil, bergamot fruit oil , citron fruit oil, tomato fruit oil, rosehip oil, pepper fruit oil, brazil nectarine fruit oil, flat leaf pimento fruit oil, anise fruit oil, mulberry fruit oil, juniper fruit oil, Capsicum fruit oil, satsuma fruit oil, star fruit oil, rosehip oil and coriander fruit oil, etc.), seeds (for example: jojoba seed oil, safflower seed oil, white pond flower seed oil, sunflower seed oil, Macadamia Seed Oil, Castor Seed Oil, Peony Seed Oil, Grape Seed Oil, Grapefruit Seed Oil, Apple Seed Oil, Pomegranate Seed Oil, Watermelon Seed Oil, Zucchini Seed Oil, Flax Seed Oil, Rapeseed Oil, Sesame Seed Oil , borage seed oil, Burr
  • the present invention unexpectedly finds that plant fruit oils (such as shea butter, olive oil, etc.) and plant seed oils (such as jojoba oil, safflower seed oil, sunflower seed oil, etc.) have skin barrier-related effects and can enhance skin Barrier vitality and promotion of expression of skin barrier-related factors FLG, LOR, IVL, TGM1, CASP14, HMGCR, AQP3 and ZO-1. Therefore, the composition comprising plant fruit oil and plant seed oil can be used as an efficacy additive in medicines and external skin preparations.
  • plant fruit oils such as shea butter, olive oil, etc.
  • plant seed oils such as jojoba oil, safflower seed oil, sunflower seed oil, etc.
  • described vegetable oil comprises vegetable fruit oil and vegetable seed oil
  • described vegetable fruit oil is selected from: shea butter, olive fruit oil, sweet almond oil, Avocado Fruit Oil, Sea Buckthorn Fruit Oil, coconut Fruit Oil, Orange Fruit Oil, Bergamot Fruit Oil, Citron Fruit Oil, Tomato Fruit Oil, Rosehip Oil, Pepper Fruit Oil, Nectarine Fruit Oil, Flat Leaf Pimento orchid fruit oil, anise fruit oil, mulberry fruit oil, juniper fruit oil, pheasant fruit oil, satsuma fruit oil, star fruit oil, rosehip oil, coriander fruit oil, or combinations thereof
  • the vegetable seed oil is selected from: jojoba seed oil, safflower seed oil, white pond flower seed oil, sunflower seed oil, rice bran oil, macadamia nut seed oil, castor oil, peony seed oil, grape seed oil , Grapefruit Seed Oil, Apple Seed Oil, Pomegranate Seed Oil, Watermelon Seed Oil, Zucchin
  • the composition of the present invention further comprises a natural surfactant selected from the group consisting of lecithin, cholesterol, lanolin, tea saponin, protein, saponins, sugars, alkyl polyglycosides or their combinations.
  • a natural surfactant selected from the group consisting of lecithin, cholesterol, lanolin, tea saponin, protein, saponins, sugars, alkyl polyglycosides or their combinations.
  • the natural surfactant is hydrogenated lecithin.
  • the weight ratio of vegetable oil to natural surfactant in the composition is 1:1 to 20:1. In a more preferred embodiment, the weight ratio of vegetable oil to natural surfactant in the composition is 10:1 to 20:1.
  • the present invention also relates to the application of the composition containing vegetable oil in enhancing skin barrier function.
  • the enhancement of the skin barrier function is achieved by enhancing the vitality of the skin barrier and/or promoting the expression of skin barrier-related factors.
  • the present invention also relates to the application of the composition comprising vegetable oil in the preparation of medicines and/or external skin preparations for enhancing the skin barrier function.
  • the pharmaceutical and/or external skin preparation contains 0.001-100% by weight of the composition.
  • the present invention relates to a composition comprising plant fruit oil and plant seed oil and its application. It has been found in the research that the composition has the ability to enhance the vitality of the skin barrier and promote the skin barrier-related factors FLG, LOR, IVL, TGM1, CASP14, HMGCR, Effect of AQP3 and ZO-1 expression. Therefore, the composition comprising plant fruit oil and plant seed oil can be used as an efficacy additive for preparing medicines and/or skin external preparations for enhancing skin barrier function.
  • the plant fruit oil in the present invention is also called plant fruit oil, which mainly comes from plant fruits, seeds and germs, and also partly comes from other parts such as leaves, bark, roots, petals and pistils of plants.
  • Plant fruit oils include, but are not limited to, avocado (Butyrospermum parkii) fruit butter (also known as shea butter), olive (Olea europaea) fruit oil (also known as olive oil), apricot (Prunus armeniaca) kernel oil (also known as sweet Almond Oil), avocado (Persea gratissima) Fruit Oil, Sea Buckthorn (Hippophae rhamnoides) Fruit Oil, Coconut (Cocos nucifera) Fruit Oil, Orange (Citrus junos) Fruit Oil, Bergamot (Citrus aurantium bergamia) Fruit Oil, Citron (Citrus bedica limonum) Fruit Oil, Tomato (Solanum lycopersicum) Fruit Oil, Rosa canina (Rosa canina) Fruit Oil, Pepper (P
  • shea butter is relatively close to the indicators of human sebum secretion and oil. It is rich in non-saponifiable ingredients, easy to absorb by the human body, can prevent dryness and cracking, further restore and maintain the natural elasticity of the skin, protect the skin barrier function, and at the same time Can play an anti-inflammatory effect.
  • Olive oil has a slightly heavy skin feel and is very suitable for dry skin. The squalene and fatty acids contained in it can be quickly absorbed by the skin, effectively keeping the skin elastic and moisturized. It is rich in monounsaturated fatty acids, vitamins, and phenols The substance can eliminate facial wrinkles, prevent skin aging, have the effects of skin care and hair care, and prevent chapped hands and feet.
  • Sweet Almond Oil softens, conditions, and is great for repairing and moisturizing dry, cracked, itchy or irritated skin, especially for dry and sensitive skin.
  • avocado oil is used as a lubricant for cosmetics, which can make the skin smooth, has good permeability and moisturizing properties, and can promote skin cell regeneration. It has a good effect on rebuilding skin structure, repairing sunburn and dry skin.
  • coconut oil is a saturated fat, stable lipid, not easy to oxidize and produce free radical attack, its strong antioxidant capacity can help the human body prevent the generation of free radicals, so it can be used for beauty and skin care, its emulsification stability and antioxidant properties can make Makeup is more even and delicate.
  • compositions containing plant fruit oils have skin barrier-related effects, can enhance skin barrier vitality and promote skin barrier-related factors FLG, LOR, IVL, TGM1, Expression of CASP14, HMGCR, AQP3 and ZO-1.
  • compositions of the present invention comprise 0.1-100% by weight vegetable fruit oil. In a preferred embodiment, the composition of the invention comprises 0.1-50% by weight of vegetable fruit oil. In a preferred embodiment, the composition according to the invention comprises 0.1-20% by weight of vegetable fruit oil. In a preferred embodiment, the composition of the invention comprises 0.5-10% by weight of vegetable fruit oil.
  • the vegetable seed oil used in the present invention is also called vegetable seed oil, including but not limited to: jojoba seed oil, safflower seed oil, white pond flower seed oil and sunflower seed oil.
  • Oils containing plant seeds mainly include jojoba (Simmondsia chinensis) seed oil, safflower (Carthamus tinctorius) seed oil, white pond flower (Limnanthes alba) seed oil, sunflower (Helianthus annuus) seed oil, macadamia nut (Macadamia ternifolia) seed oil , Castor Bean (Ricinus communis) Seed Oil, Peony (Paeonia suffruticosa) Seed Oil, Grape (Vitis vinifera) Seed Oil, Grapefruit (Citrus paradisi) Seed Oil, Apple (Pyrus malus) Seed Oil, Pomegranate (Punica granatum) Seed Oil , Watermelon (Citrullus lanatus) Seed Oil, Zucchin
  • jojoba seed oil is the most penetrating base oil, which is easily absorbed by the skin. It is refreshing, moisturizing, and non-greasy. It can restore the pH balance of the skin, remove wrinkles, effectively improve oily skin, regulate the secretion of sebaceous glands, and shrink pores. Also the best skin moisturizing oil.
  • Safflower seed oil is rich in linoleic acid and fat accompanying substances (vitamin E, vitamin A), and it is easy to deteriorate when exposed to air.
  • the nutritional composition and application are similar to sunflower oil. It is usually used as emollient and lubricating ingredients in cosmetics, which can improve Eczema and rough skin, make skin supple and smooth, and help normalize metabolism.
  • White pond flower seed oil contains more than 98% of long-chain fatty acids with anti-oxidative effect. It has a unique molecular structure and moisturizing function. It can form a water-locking film on the surface of the skin, lock moisture to resist dryness, and at the same time stretch the texture of the skin. Deeply repairs skin loss and enhances the overall contour of the skin. Macadamia nut seed oil is characterized by being rich in unsaturated fatty acids, which can prevent heart disease. This natural vegetable oil with a high content of monounsaturated fatty acids can regulate and control blood sugar levels, improve lipid metabolism in diabetic patients, and effectively Moisturizing skin care, is a good sunscreen, skin care products.
  • compositions containing plant seed oils have skin barrier-related effects, can enhance skin barrier vitality and promote skin barrier-related factors FLG, Expression of LOR, IVL, TGM1, CASP14, HMGCR, AQP3 and ZO-1.
  • compositions of the invention comprise 0.1-100% by weight vegetable seed oil. In a preferred embodiment, the composition of the invention comprises 0.1-50% by weight of vegetable seed oil. In a preferred embodiment, the composition of the invention comprises 0.1-20% by weight of vegetable seed oil. In a preferred embodiment, the composition of the invention comprises 0.5-10% by weight of vegetable seed oil.
  • Composition comprising vegetable fruit oil and vegetable seed oil
  • a composition comprising vegetable fruit oil and vegetable seed oil is provided, wherein the weight ratio of the vegetable fruit oil to the vegetable seed oil is 2:8 to 8:2. In a preferred embodiment, the weight ratio of the vegetable fruit oil to the vegetable seed oil is 1:1.
  • compositions of the present invention comprise 0.1-100% by weight of vegetable fruit oils and vegetable seed oils. In a preferred embodiment, the composition of the invention comprises 0.1-50% by weight of vegetable fruit oils and vegetable seed oils. In a preferred embodiment, the composition of the invention comprises 0.1-20% by weight of vegetable fruit oil and vegetable seed oil. In a preferred embodiment, the composition of the invention comprises 0.5-10% by weight of vegetable fruit oil and vegetable seed oil.
  • compositions of the present invention may also contain natural surfactants.
  • Natural surfactants mostly come from plants and animals, which are relatively complex polymer organic matter. Due to its strong hydrophilicity, it can form emulsions. Most of these substances have higher viscosity, which is beneficial to emulsification stability.
  • the natural surfactant contained in the composition of the present invention includes but not limited to: lecithin, cholesterol, lanolin, tea saponin, protein, saponins, sugars, alkyl polyglycosides and the like.
  • Lecithin exists in biological cells, such as animal eggs, brains and other tissues and plant seeds or germs, and egg yolk phosphatidylcholine is extracted from egg yolk; soybeans are rich in lecithin.
  • Lecithin has physiological activities such as emulsification, dispersion, and anti-oxidation. It is a natural and excellent surfactant and an important emulsifier.
  • Hydrogenated lecithin has strong hydrophilicity and moisturizing properties, and has a strong affinity for skin and mucous membranes. It can be used in cosmetic formulations to moisturize, emulsify and disperse; as a surfactant, it can also condition the skin , to achieve a good oil-water balance effect, the use of hydrogenated lecithin can also develop skin care cream, hand cream, lipstick, sunscreen and other advanced cosmetic products.
  • compositions of the present invention comprise 0.1-20% by weight of natural surfactants. In a preferred embodiment, the compositions of the invention comprise 0.1-10% by weight of natural surfactants. In a preferred embodiment, the compositions of the invention comprise 0.1 to 5% by weight of natural surfactants. In a preferred embodiment, the compositions of the invention comprise 0.5-2% by weight of natural surfactants.
  • the weight ratio of vegetable oil (including vegetable fruit oil and vegetable seed oil) to natural surfactant in the composition of the present invention is 1:1 to 20:1. In a more preferred embodiment, the weight ratio of vegetable oil (including vegetable fruit oil and vegetable seed oil) to natural surfactant in the composition is 10:1 to 20:1.
  • composition containing plant seed oil can be used in pharmaceuticals and/or skin external preparations for enhancing skin barrier function.
  • the drug is selected from: tablets, capsules, emulsions, suspensions, powders, granules, solutions, and various drug dosage forms known in the art. Add different dosages according to different types of dosage forms.
  • the external skin preparation is selected from: cleanser, lotion, lotion, cream, gel, mask. Add different dosages according to different types of preparations.
  • the skin external preparation is a general term for all ingredients that are usually used on the outside of the skin, and may be, for example, a cosmetic composition.
  • the cosmetic composition can be basic cosmetics, facial makeup cosmetics, body cosmetics, hair care cosmetics, etc. There is no special limitation on the dosage form, which can be reasonably selected according to different purposes.
  • the cosmetic composition also contains different cosmetically acceptable media or matrix excipients according to different dosage forms and purposes.
  • External preparations for skin contain a dermatologically acceptable carrier or vehicle (eg, lotion, cream, ointment, cleanser, etc.).
  • a dermatologically acceptable carrier or vehicle eg, lotion, cream, ointment, cleanser, etc.
  • a carrier capable of dissolving or dispersing these components at the above-mentioned concentrations according to common knowledge in the art.
  • Said carrier includes, for example, water, alcohols, oils, etc. wait.
  • the external preparation for skin of the present invention may be in the form of a topical product which can be externally applied to the skin and which can be prepared by those ordinary techniques known in the art.
  • the carrier may take various practical forms, such as creams, dressings, gels, lotions, ointments or liquids, including compositions for application and for rinsing off, and their addition to, for example, dry or Wet application, hydrogel matrix, or adhesive (or non-adhesive) patch material carrier.
  • the carrier is a gel or moisturizing lotion, or an applicator in dry or wet form.
  • Typical carriers include emulsions containing water and/or alcohol and emollients such as oils and waxes of hydrocarbons, silicone oils, hyaluronic acid, vegetable, animal or marine fats or oils, glyceride derivatives, Fatty acids, or fatty acid esters or alcohols or alcohol ethers, lanolin and its derivatives, polyols or esters, wax esters, sterols, phospholipids, etc., and generally emulsifiers (nonionic, cationic or anionic), Although some emollients have inherent emulsifying properties. Additionally, these same components can be formulated into creams, gels, or solid sticks using different proportions of their components and/or by incorporating thickeners such as gums or other forms of hydrocolloids.
  • emollients such as oils and waxes of hydrocarbons, silicone oils, hyaluronic acid, vegetable, animal or marine fats or oils, glyceride derivatives, Fatty acids
  • the skin external preparation of the present invention may contain additional components commonly found in skin care compositions, such as emollients, skin conditioners, emulsifiers, preservatives, antioxidants, fragrances, chelating agents, etc., as long as they are compatible with the skin It is sufficient that other components in the external preparation are physically and chemically compatible and do not affect the effect of the vegetable seed oil of the present invention.
  • one or more preservatives may be used. Suitable preservatives include p-hydroxyacetophenone, C1-C4 alkylparabens and phenoxyethanol. Preservatives are used in an amount of about 0.5 to about 2% by weight, preferably about 0.5 to 1% by weight, based on the total weight of the composition.
  • one or more antioxidants can be used. Suitable antioxidants include butylated hydroxytoluene (BHT), ascorbyl palmitate (BHA), butylated hydroxyanisole, phenyl-alpha-naphthylamine, hydroquinone, propyl gallate, nordihydroguaiaretic acid , vitamin E or vitamin E derivatives, vitamin C and its derivatives, calcium pantothenate, green tea extract and mixed polyphenols, and mixtures of the foregoing.
  • BHT butylated hydroxytoluene
  • BHA ascorbyl palmitate
  • butylated hydroxyanisole phenyl-alpha-naphthylamine
  • hydroquinone propyl gallate
  • nordihydroguaiaretic acid a antioxidant that is used in an amount ranging from about 0.02 to 0.5% by weight of the total composition, more preferably from about 0.002 to 0.1% by weight.
  • one or more emollients may be used, which act as lubricants by their ability to remain on the skin surface or in the stratum corneum to reduce flaking, improve The appearance of the skin.
  • Typical emollients include fatty esters, fatty alcohols, mineral oil, polyether siloxane copolymers, and the like.
  • emollients include, but are not limited to, Polypropylene Glycol ("PPG")-15 Stearyl Ether, PPG-10 Cetyl Ether, Steareth-10, Oleth-8, PPG-4 Lauryl Ether Cetyl Ether, Vitamin E Acetate, Lanolin, Cetyl Alcohol, Cetearyl Ethylhexanoate, Cetostearyl Alcohol, Glyceryl Stearate, Capryl Hydroxystearate, Dimethicone Alkanes, and combinations thereof. Cetyl alcohol, cetearyl ethylhexanoate, cetostearyl alcohol, glyceryl stearate and combinations thereof are preferred. When used, emollients are present in amounts ranging from about 0.1 to about 30%, preferably from about 1 to about 30% by weight, based on the total weight of the composition.
  • one or more moisturizing agents can also be used.
  • Humectants also known as humectants, help to enhance the effectiveness of emollients, reduce flaking, stimulate removal of constituent scales and improve skin feel.
  • Polyols may be used as humectants including, but not limited to, glycerin, polyalkylene glycols, alkylene polyols and their derivatives, including butylene glycol, propylene glycol, dipropylene glycol, polyglycerol, polyethylene glycol Alcohol and its derivatives, sorbitol, hydroxypropyl sorbitol, hexanediol, 1,3-dibutylene glycol, 1,2,6-hexanetriol, ethoxylated glycerin, propoxylated glycerin, and their combinations.
  • humectants are used in amounts of about 0.1 to about 20% by weight, preferably about 1 to about 15% by weight, based on the total weight of the composition.
  • one or more emulsifiers may be used.
  • Emulsifiers can be used in effective stabilizing amounts.
  • emulsifiers are used in amounts of from about 1.0 to about 10.0 percent by weight, more preferably from about 3.0 to about 6.0 percent by weight, based on the total weight of the composition.
  • Any emulsifier compatible with the ingredients of the composition may be used.
  • Suitable emulsifiers include Stearic Acid, Cetyl Alcohol, Glyceryl Stearate, Lecithin, Stearyl Alcohol, Steareth-2, Steareth-20, Acrylates/C10-30 Alkyl Acrylates Crosslinked Polymers, and combinations thereof.
  • one or more pH adjusting agents can be used.
  • Beneficial pH regulators in the external preparation for skin of the present invention include tromethamine.
  • the pH adjuster is used in an amount of about 0.1 to about 2% by weight, preferably about 0.1 to about 1% by weight, based on the total weight of the composition.
  • the skin external preparation comprises acrylic acid (ester) type/C10-30 alkanol acrylate crosslinked polymer, glycerin, p-hydroxyacetophenone, glyceryl stearate and lecithin, Hexetearyl Alcohol, Cetearyl Ethylhexanoate, Tromethamine, or combinations thereof.
  • the dosage of the composition of the present invention in external skin preparations is 0.001%-100% (w/w), preferably 0.01%-60% (w/w) by weight, more The preferred weight percentage is 0.01%-40% (w/w).
  • Jojoba seed oil trade name jojoba oil, was purchased from Vantage Specialty Ingredients, Inc.
  • Safflower (CARTHAMUS TINCTORIUS) seed oil trade name safflower seed oil, purchased from Northstar Lipids UK Ltd.
  • White pond flower (LIMNANTHES ALBA) seed oil trade name white pond flower seed oil, purchased from Hemings special chemical company
  • Sunflower (HELIANTHUS ANNUUS) seed oil trade name sunflower oil, purchased from Cargill Grain and Oil (Nantong) Co., Ltd.
  • Hydrogenated lecithin trade name hydrogenated lecithin, purchased from NIKKO CHEMICALS CO.,LTD.
  • pH meter METTLER TOLEDO company SEVENMULTI type
  • Stand mixer IKA @ EUROSTAR, power control-visc.
  • Embodiment 1 preparation composition
  • Embodiment 2 Preparation comprises the composition of vegetable fruit oil
  • Embodiment 3 Preparation comprises the composition of vegetable fruit oil
  • Embodiment 4 Preparation comprises the composition of vegetable fruit oil
  • Embodiment 5 Preparation comprises the composition of vegetable fruit oil
  • Embodiment 6 Preparation comprises the composition of vegetable fruit oil
  • Example 7 Preparation of a composition comprising vegetable seed oil
  • Example 8 Preparation of a composition comprising vegetable seed oil
  • Example 9 Preparation of a composition comprising vegetable seed oil
  • Example 11 Preparation of a composition comprising vegetable seed oil
  • Example 12 Preparation of a composition comprising vegetable fruit oil and vegetable seed oil
  • Example 13 Preparation of a composition comprising vegetable fruit oil and vegetable seed oil
  • Example 14 Preparation of a composition comprising vegetable fruit oil and vegetable seed oil
  • Example 15 Preparation of a composition comprising vegetable fruit oil and vegetable seed oil
  • Example 16 Preparation of a composition comprising vegetable fruit oil and vegetable seed oil
  • Example 17 Preparation of a composition comprising vegetable fruit oil and vegetable seed oil
  • Example 18 Preparation of Compositions Comprising Vegetable Fruit Oil and Vegetable Seed Oil
  • Example 19 Preparation of Compositions Comprising Vegetable Fruit Oil and Vegetable Seed Oil
  • Example 20 Preparation of Compositions Comprising Vegetable Fruit Oil and Vegetable Seed Oil
  • Example 21 Preparation of Compositions Comprising Vegetable Fruit Oil and Vegetable Seed Oil
  • the 3D epidermal reconstruction model is a human-derived 3D epidermal model that can simulate the structure of each layer of the epidermis differentiated by keratinocytes.
  • the skin irritant SDS is used to cause certain damage to the model, and then the surface of the damaged model is covered with an appropriate amount of samples prepared in the embodiment for 24 hours for repair. After 24 hours, the samples were washed away, and the restoration of tissue viability was tested by the MTT method. According to the recovery of tissue vitality, the skin barrier repair ability of the samples of the examples can be evaluated.
  • 1.1 Cell skin model is 3D epidermal skin model (EpiSkin).
  • 3D skin model maintenance medium 3D skin model detection medium
  • 3D skin model detection medium EpiSkin
  • sodium dodecyl sulfate SDS
  • SDS sodium dodecyl sulfate
  • Cabco calcium and magnesium DPBS
  • MTT isopropanol, concentrated hydrochloric acid ( Sinopharm Group).
  • CO2 incubator HERAcell 240i biological safety cabinet 1300SERIES A2, microplate reader Multiskan Mk3 (Thermo); positive pipette M25 (Gilson); 50mL continuous pipette tip Multipette plus (Eppendorf); skin puncher ( area 0.38 cm 2 ).
  • a 1.5% (mass volume ratio) sodium dodecyl sulfate (SDS) solution was prepared with 1 ⁇ phosphate buffered saline (DPBS) solution.
  • SDS sodium dodecyl sulfate
  • the model is divided into a blank control group (without any treatment, 3 repetitions), a negative control group (with 1.5% SDS for damage treatment, 3 repetitions) and Example 1-21 and Example 26-28 sample groups (each 3 replicates for each sample).
  • MTT thiazolyl blue
  • the EP tube was shaken and mixed on a vortex, and placed in a refrigerator at 4°C for 72 hours for color extraction. At the same time, prepare an EP tube containing 1 ml of acidic isopropanol as a blank well for microplate reader detection.
  • the blank control group is the uninjured group, and the relative activity is 100%; the relative activity of the negative control group is controlled at 40-60% compared with the blank control group; the relative activity of the sample group is higher than that of the negative control group, indicating that the sample group has a promotional barrier The ability to repair, this sample group is lower than the negative control group, indicating that this sample group does not have the ability to promote barrier repair.
  • Table 1 The relative viability of tissues in each group detected by MTT method
  • the average relative vitality of the skin model tissue is 54.3%, and the sample of embodiment 19 (shea butter 5% + white pond flower seed oil 5%) skin model tissue mean relative vitality is 68.0%, embodiment 20 sample (shea butter 5%+rice bran oil 5%) skin model tissue mean relative vitality is 52.5%, embodiment 21 sample ( Shea butter 5%+sunflower seed oil 5%) skin model tissue mean relative vitality is 54.2%, embodiment 26 sample (shea butter 100%) skin model tissue mean relative vitality is 68.4%, embodiment 27 sample ( Jojoba oil 100%) average relative vitality of skin model tissue is 65.2%, and example 28 sample (safflower seed oil 100%) average relative vitality of skin model tissue is 70.8% (see Table 1).
  • shea butter has better tissue repair ability in the range of concentration 0.5-100%; in Examples 7-11 and 27, jojoba oil has a concentration in the range of 0.5-100% It has better tissue repair ability; shea butter and jojoba oil have better tissue repair ability in the scope of compounding ratio 5:5/2:8/4:6/6:4/8:2 among the embodiment 12-16 Tissue repair ability; Shea butter compounded with olive oil, safflower oil, rice bran oil and sunflower seed oil (5%+5%) in Examples 17-21 has better tissue repair ability.
  • Test example 2 3D recombinant skin epidermis model barrier-related gene expression test
  • the 3D epidermal reconstruction model is a human-derived 3D epidermal model that can simulate the structure of each layer of the epidermis differentiated by keratinocytes. Cover an appropriate amount of samples on the epidermal model for 24 hours, then collect the total ribonucleic acid (RNA) of the epidermal tissue, use RNA reverse transcription technology and gene microarray technology to quantitatively detect skin barrier-related genes, and then evaluate the skin barrier moisturizing and repair ability.
  • RNA total ribonucleic acid
  • 1.1 Cell skin model is 3D epidermal skin model (EpiSkin).
  • 3D skin model maintenance medium EpiSkin
  • DPBS containing calcium and magnesium Gibco
  • isopropanol, 75% absolute ethanol Sinopharm Group
  • DEPC water Teangen Biology
  • total RNA extraction reagent TRIzol ThermoFisher
  • Reverse transcription kit iScript cDNA Synthesis Kit fluorescence real-time quantitative PCR reagent iTaq TM Universal Green Supermix (Bio-rad).
  • Example 1 The model was divided into Example 1, 4, 9, 12, 17-25 sample groups (3 repetitions for each sample) and a positive control group (rosiglitazone, 3 repetitions).
  • RNA forms a white pellet at the bottom of the EP tube.
  • RNA concentration was measured with a micro-spectrophotometer Nanodrop, and the integrity of the RNA was detected by agarose gel electrophoresis.
  • the dissolved total RNA of the epidermis model tissue was used for subsequent experiments or stored at -80°C for long-term storage after aliquoting.
  • RNA Take 1 microgram of total RNA for reverse transcription, and use the reverse transcription kit iScript cDNA Synthesis Kit to reverse transcribe to obtain cDNA.
  • the reverse transcription system is as follows:
  • the reverse transcription program was as follows: 25°C, 5 minutes; 42°C, 30 minutes; 85°C, 5 minutes.
  • PCR Fluorescent real-time quantitative polymerase chain reaction
  • reagent iTaq TM Universal Green Supermix performs fluorescence real-time quantitative detection to analyze the expression of barrier-related gene messenger RNA (mRNA).
  • the reaction system is as follows:
  • the reaction program is as follows: 95°C, 30 seconds; 95°C, 15 seconds, 60°C, 30 seconds, 40 cycles; 65-95°C, 0.5°C decrease each time (melting curve).
  • primer sequences used in this example are designed as follows:
  • the 2- ⁇ Ct method was used to analyze the gene expression changes of the example sample group and the positive control group (rosiglitazone) relative to the example 1 control group.
  • the amount of gene expression in the sample group in Example 1 is taken as 100%, and compared with it in each group, it is greater than 100%, indicating that the gene expression is up-regulated, and less than 100%, indicating that the gene expression is down-regulated.
  • the up-regulation of genes such as FLG and LOR indicates that this sample group has the ability to moisturize and promote barrier repair; the down-regulation of genes such as FLG and LOR indicates that this sample group does not have the ability to moisturize and promote barrier repair.
  • embodiment 1 (shea butter 0%+jojoba oil 0%) is as contrast, and its gene relative expression is 100%, embodiment 4,9,12,17,18,19,20 , 21, 22, 23, 24 and 25 samples and positive control samples were compared with the gene expression, and the corresponding percentages were obtained.
  • the barrier factor FLG in the sample of embodiment 4 (shea butter 5%), the sample of embodiment 9 (jojoba oil 5%), the sample of embodiment 12 (shea butter 5%+jojoba oil 5%) ), Example 17 sample (shea butter 5%+olive oil 5%), embodiment 18 sample (shea butter 5%+safflower seed oil 5%), embodiment 19 sample (shea butter 5% %+white pond flower seed oil 5%), Example 20 sample (shea butter 5%+rice bran oil 5%), embodiment 21 sample (shea butter 5%+sunflower seed oil 5%), embodiment 22 Sample (safflower seed oil 5%), embodiment 23 sample (olive oil 5%), embodiment 24 sample (sunflower seed oil 5%), embodiment 25 sample (White Pond Seed Oil 5%) and positive control (Luo Glitazone) after treatment, compared with Example 1 sample (shea butter 0%+jojoba oil 0%), respectively 222%, 218%, 225%, 265%, 283%, 223%, 25
  • the barrier factor LOR in the sample of embodiment 4 (shea butter 5%), the sample of embodiment 9 (jojoba oil 5%), the sample of embodiment 12 (shea butter 5%+jojoba oil 5%) ), Example 17 sample (shea butter 5%+olive oil 5%), embodiment 18 sample (shea butter 5%+safflower seed oil 5%), embodiment 19 sample (shea butter 5% %+white pond flower seed oil 5%), Example 20 sample (shea butter 5%+rice bran oil 5%), embodiment 21 sample (shea butter 5%+sunflower seed oil 5%), embodiment 22 Sample (safflower seed oil 5%), embodiment 23 sample (olive oil 5%), embodiment 24 sample (sunflower seed oil 5%), embodiment 25 sample (White Pond Seed Oil 5%) and positive control (Luo Glitazone) after treatment, compared with Example 1 sample (shea butter 0%+jojoba oil 0%), respectively 240%, 236%, 227%, 242%, 247%, 208%, 28
  • the barrier factor IVL in the sample of embodiment 4 (shea butter 5%), the sample of embodiment 9 (jojoba oil 5%), the sample of embodiment 12 (shea butter 5%+jojoba oil 5% ), Example 17 sample (shea butter 5%+olive oil 5%), embodiment 18 sample (shea butter 5%+safflower seed oil 5%), embodiment 19 sample (shea butter 5% %+white pond flower seed oil 5%), Example 20 sample (shea butter 5%+rice bran oil 5%), embodiment 21 sample (shea butter 5%+sunflower seed oil 5%), embodiment 22 Sample (safflower seed oil 5%), embodiment 23 sample (olive oil 5%), embodiment 24 sample (sunflower seed oil 5%), embodiment 25 sample (White Pond Seed Oil 5%) and positive control (Luo Glitazone) after treatment, compared with Example 1 sample (shea butter 0%+jojoba oil 0%), respectively 113%, 87%, 130%, 107%, 109%, 125%, 127%, 12
  • the barrier factor TGM1 in the sample of embodiment 4 (shea butter 5%), the sample of embodiment 9 (jojoba oil 5%), the sample of embodiment 12 (shea butter 5%+jojoba oil 5%) ), Example 17 sample (shea butter 5%+olive oil 5%), embodiment 18 sample (shea butter 5%+safflower seed oil 5%), embodiment 19 sample (shea butter 5% %+white pond flower seed oil 5%), Example 20 sample (shea butter 5%+rice bran oil 5%), embodiment 21 sample (shea butter 5%+sunflower seed oil 5%), embodiment 22 Sample (safflower seed oil 5%), embodiment 23 sample (olive oil 5%), embodiment 24 sample (sunflower seed oil 5%), embodiment 25 sample (White Pond Seed Oil 5%) and positive control (Luo Glitazone) after treatment, compared with Example 1 sample (shea butter 0%+jojoba oil 0%), respectively 134%, 126%, 176%, 170%, 176%, 201%,
  • the barrier factor CASP14 in the sample of embodiment 4 (shea butter 5%), the sample of embodiment 9 (jojoba oil 5%), the sample of embodiment 12 (shea butter 5%+jojoba oil 5% ), Example 17 sample (shea butter 5%+olive oil 5%), embodiment 18 sample (shea butter 5%+safflower seed oil 5%), embodiment 19 sample (shea butter 5% %+white pond flower seed oil 5%), Example 20 sample (shea butter 5%+rice bran oil 5%), embodiment 21 sample (shea butter 5%+sunflower seed oil 5%), embodiment 22 Sample (safflower seed oil 5%), embodiment 23 sample (olive oil 5%), embodiment 24 sample (sunflower seed oil 5%), embodiment 25 sample (White Pond Seed Oil 5%) and positive control (Luo Glitazone) after treatment, compared with Example 1 sample (shea butter 0%+jojoba oil 0%), respectively 188%, 275%, 169%, 201%, 228%, 162%, 17
  • the barrier factor HMGCR in the sample of embodiment 4 (shea butter 5%), the sample of embodiment 9 (jojoba oil 5%), the sample of embodiment 12 (shea butter 5%+jojoba oil 5% ), Example 17 sample (shea butter 5%+olive oil 5%), embodiment 18 sample (shea butter 5%+safflower seed oil 5%), embodiment 19 sample (shea butter 5% %+white pond flower seed oil 5%), Example 20 sample (shea butter 5%+rice bran oil 5%), embodiment 21 sample (shea butter 5%+sunflower seed oil 5%), embodiment 22 Sample (safflower seed oil 5%), embodiment 23 sample (olive oil 5%), embodiment 24 sample (sunflower seed oil 5%), embodiment 25 sample (White Pond Seed Oil 5%) and positive control (Luo Glitazone) after treatment, compared with Example 1 sample (shea butter 0%+jojoba oil 0%), respectively 170%, 223%, 226%, 208%, 253%, 213%, 1
  • the barrier factor AQP3 in the sample of embodiment 4 (shea butter 5%), the sample of embodiment 9 (jojoba oil 5%), the sample of embodiment 12 (shea butter 5%+jojoba oil 5%) ), Example 17 sample (shea butter 5%+olive oil 5%), embodiment 18 sample (shea butter 5%+safflower seed oil 5%), embodiment 19 sample (shea butter 5% %+white pond flower seed oil 5%), Example 20 sample (shea butter 5%+rice bran oil 5%), embodiment 21 sample (shea butter 5%+sunflower seed oil 5%), embodiment 22 Sample (safflower seed oil 5%), embodiment 23 sample (olive oil 5%), embodiment 24 sample (sunflower seed oil 5%), embodiment 25 sample (White Pond Seed Oil 5%) and positive control (Luo Glitazone) after treatment, compared with Example 1 sample (shea butter 0%+jojoba oil 0%), respectively 112%, 105%, 141%, 125%, 133%, 116%
  • the barrier factor ZO-1 in the sample of embodiment 4 (shea butter 5%), the sample of embodiment 9 (jojoba oil 5%), the sample of embodiment 12 (shea butter 5%+jojoba oil 5%), Example 17 sample (shea butter 5%+olive oil 5%), embodiment 18 sample (shea butter 5%+safflower seed oil 5%), embodiment 19 sample (shea butter Oil 5%+Baichihuaseed Oil 5%), Example 20 sample (Shea Butter 5%+Rice Bran Oil 5%), Example 21 sample (Shea Butter 5%+Sunflower Seed Oil 5%), implementation Example 22 sample (safflower seed oil 5%), embodiment 23 sample (olive oil 5%), embodiment 24 sample (sunflower seed oil 5%), embodiment 25 sample (white pond flower seed oil 5%) and positive control After (rosiglitazone) treatment, compared with Example 1 sample (shea butter 0%+jojoba oil 0%), it is respectively 143%, 151%, 160%, 138%, 147%,
  • Example 4 5% shea butter promotes the expression of FLG, LOR, IVL, TGM1, CASP14, HMGCR, AQP3 and ZO-1 barrier factors, which is beneficial to barrier formation and has the function of promoting skin moisturizing and barrier repair.
  • the sample of Example 9 (jojoba oil 5%) promotes the expression of FLG, LOR, TGM1, CASP14, HMGCR, AQP3 and ZO-1 barrier factors, is conducive to barrier formation, and has the effect of promoting skin moisturizing and barrier repair.
  • Example 12 sample (shea butter 5%+jojoba oil 5%) promotes the expression of FLG, LOR, IVL, TGM1, CASP14, HMGCR, AQP3 and ZO-1 barrier factors, is conducive to barrier formation, and has the function of promoting skin moisturizing and barrier repair.
  • Example 17 sample (shea butter 5%+olive oil 5%) promotes the expression of FLG, LOR, IVL, TGM1, CASP14, HMGCR, AQP3 and ZO-1 barrier factors, is conducive to barrier formation, has the function of promoting skin moisturizing and Barrier repair effect.
  • Example 18 sample (shea butter 5% + safflower seed oil 5%) promotes the expression of FLG, LOR, IVL, TGM1, CASP14, HMGCR, AQP3 and ZO-1 barrier factors, which is beneficial to barrier formation and has the effect of promoting skin Moisturizing and barrier repairing properties.
  • the sample of Example 19 (5% shea butter + 5% white pond flower seed oil) promotes the expression of FLG, LOR, IVL, TGM1, CASP14, HMGCR, AQP3 and ZO-1 barrier factors, which is beneficial to barrier formation and has the effect of promoting skin Moisturizing and barrier repairing properties.
  • Example 20 (shea butter 5%+rice bran oil 5%) promotes the expression of FLG, LOR, IVL, TGM1, CASP14, HMGCR, AQP3 and ZO-1 barrier factors, which is beneficial to barrier formation and has the function of promoting skin moisturizing and Barrier repair effect.
  • the sample of Example 21 (shea butter 5% + sunflower seed oil 5%) promotes the expression of FLG, LOR, IVL, TGM1, CASP14, HMGCR, AQP3 and ZO-1 barrier factors, which is beneficial to barrier formation and has the function of promoting skin moisturizing and barrier repair.
  • Example 22 (5% safflower seed oil) promotes the expression of FLG, LOR, IVL, TGM1, CASP14, HMGCR, AQP3 and ZO-1 barrier factors, is beneficial to barrier formation, and has the effect of promoting skin moisturizing and barrier repair.
  • the sample of Example 23 (olive oil 5%) promotes the expression of FLG, LOR, TGM1, CASP14, HMGCR, AQP3 and ZO-1 barrier factors, is conducive to barrier formation, and has the effect of promoting skin moisturizing and barrier repair.
  • Example 24 (5% sunflower seed oil) promotes the expression of FLG, LOR, TGM1, CASP14, HMGCR, AQP3 and ZO-1 barrier factors, is conducive to barrier formation, and has the effect of promoting skin moisturizing and barrier repair.
  • Example 25 (White Pond Seed Oil 5%) promotes the expression of FLG, LOR, IVL, TGM1, CASP14, HMGCR and ZO-1 barrier factors, is conducive to barrier formation, and has the effect of promoting skin moisturizing and barrier repair.
  • composition comprising plant fruit oil and/or plant seed oil according to the present invention can be used as an intermediate raw material or functional additive for the preparation of medicines or skin external preparations, and the skin external preparations are preferably cosmetic compositions, including but not It is limited to the preparation of cream, lotion, gel, lotion, essence, mask, eye cream, aerosol (cleaning foam), spray, shower gel, massage oil, facial cleanser and other dosage forms.
  • the percentage by weight of the composition comprising vegetable fruit oil and/or vegetable seed oil in the skin external preparation of the present invention is 0.001%-100% (w/w); the preferred weight percentage is 0.01%-60% (w/w) w); the most preferred weight percentage is 0.01%-40% (w/w).
  • compositions obtained in Examples 3, 7, 9, 20 and 23 containing vegetable fruit oil and/or vegetable seed oil in external skin preparations as well as the formulations and preparation methods of these dosage forms.
  • Specific application examples are as follows:
  • Examples 2-28 in the present invention can also be used alone as skin external preparations.

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Abstract

本发明提供了一种包含植物油脂的组合物，所述植物油脂包括植物果油和植物籽油，其中，所述植物果油选自下组：乳木果油、橄榄果油、甜杏仁油、鳄梨果油、沙棘果油、椰子果油等；其中，所述植物籽油选自下组：霍霍巴籽油、红花籽油、白池花籽油、向日葵籽油、米糠油、澳洲坚果籽油、蓖麻籽油等，其中，所述植物果油与所述植物籽油的重量比为2:8至8:2，其中，以所述组合物的总重量计，所述组合物包含至少0.5重量％的植物油脂。本发明还涉及包含植物油脂的组合物在增强皮肤屏障功能和/或在制备用于增强皮肤屏障功能的药品和/或皮肤外用剂中的应用。

Description

包含植物果油和植物籽油的组合物及其应用 技术领域
本发明属于化妆品领域，具体涉及含有植物果油与植物籽油的组合物及其在肌肤屏障功能方面的应用。
背景技术
皮肤屏障广义包括物理屏障、色素屏障、神经屏障、免疫屏障。皮肤屏障狭义主要指物理性屏障，我们平时说的皮肤屏障都是物理屏障。物理性屏障由皮脂膜、角质层角蛋白、脂质、“三明治”结构、砖墙结构、真皮粘多糖类、粘多糖类等共同构成，抵御外界有害、刺激物、日光进入，同时具有保湿及调节抗炎作用。皮脂的基本作用是滋润、保湿，同时其弱酸性也可以发挥一定抗菌作用。皮脂在皮肤表面构成“皮脂膜”，是皮肤的天然保湿霜。若缺乏皮脂，皮肤屏障功能会减弱，皮脂中含有甘油三酯、游离脂肪酸、蜡酯、角鲨烯等成分，可通过涂抹保湿霜在皮肤表面重建皮脂膜，能有效地隔绝外界刺激，同时防止肌肤水分的散失。
根据油脂的来源和化学成分的不同，可将油脂主要分为：植物油脂、动物油脂、矿物油脂和合成油脂，植物油脂由于质感亲肤，接近人类皮脂膜结构，渗透性好，深层渗入并滋养皮肤，受到了很多护肤品的青睐。化妆品用的植物油脂主要来自于植物果实、种子和胚芽，也有部分来自植物的叶、皮、根、花瓣和花蕊等其他部位。含有植物果实的油脂主要有牛油果树(Butyrospermum parkii)果脂(又名乳木果油)、油橄榄(Olea europaea)果油(又名橄榄油)、杏(Prunus armeniaca)仁油(又叫甜杏仁油)、鳄梨(Persea gratissima)果油、沙棘(Hippophae rhamnoides)果油、椰子(Cocos nucifera)果油、香橙(Citrus junos)果油、香柠檬(Citrus aurantium bergamia)果油、香橼(Citrus bedica limonum)果油、番茄(Solanum lycopersicum)果油、狗牙蔷薇(Rosa canina)果油等。含有植物种子的油脂主要有霍霍巴(Simmondsia chinensis) 籽油、红花(Carthamus tinctorius)籽油、白池花(Limnanthes alba)籽油、向日葵(Helianthus annuus)籽油、澳洲坚果(Macadamia ternifolia)籽油、蓖麻(Ricinus communis)籽油、牡丹(Paeonia suffruticosa)籽油、葡萄(Vitis vinifera)籽油、葡萄柚(Citrus paradisi)籽油、苹果(Pyrus malus)籽油、石榴(Punica granatum)籽油、西瓜(Citrullus lanatus)籽油、西葫芦(Cucurbita pepo)籽油、亚麻(Linum usitatissimum)籽油、油菜(Brassica campestris)籽油、芝麻(Sesamum indicum)籽油等。
乳木果油(shea butter)是直接提炼自非洲乳木果树的果实，质地柔润幼滑，是最有效的天然保湿品，在化妆品领域得到了广泛地应用。例如，文献陈培丰，乳木果油在化妆品种的应用，福建轻纺[J],2003,12(175):1-4指出，乳木果油既可以用在护肤乳液、膏霜中当润肤剂起到强效的保湿作用外，还可以应用在口红、唇彩及防晒等产品中，涂抹附着性好、柔软不油腻，同时可协助增加防晒系数SPF值。另外，食用油脂乳木果油分提还可得到乳木果脂，例如：文献黄贤校，乳木果液油中生物活性物质提取工艺的研究，中国油脂[J],2015,40(4):69-73中提出，乳木果脂可作为可可脂的替代品用于制作巧克力和糖果等。
橄榄油是用适当方法从油橄榄鲜果中提取得到的天然油脂，在医药和日化等行业有着相当广泛地应用。例如，文献马晓原，天然植物油在防晒化妆品中的功效研究进展，中国油脂[J],2021,46(1):71-75中提出，橄榄油中含有的多酚成分，具有吸收紫外线和抗氧化功能，还能消除面部皱纹，防止肌肤衰老。文献王成章，中国油橄榄发展历程与产业展望，生物质化学工程[J],2013,47(2):41-46中提出，在医药方面，橄榄油可以增进消化系统、减少心血管疾病和预防癌症等，同时橄榄油所含的油酸能降低血压、平衡血脂、血糖。橄榄油肤感略重，非常适合干性肌肤使用，其所含的角鲨烯和脂肪酸能被皮肤快速吸收，有效保持皮肤弹性和润泽，其中所含丰富的单不饱和脂肪酸、维生素、酚类物质能消除面部皱纹，防止肌肤衰老，有护肤护发和防止手足皲裂等功效。
霍霍巴油对肌肤有十分显著的美容功效，可畅通毛细孔，调节油性或混合性肌肤的油脂分泌，并改善发炎的皮肤，湿疹、干癣、面疱等，对于干性发质及干性皱纹肌肤可使其恢复活力光泽，所以是各种皮肤性质都能使用的基础 油。例如，文献李春霞，霍霍巴油在化妆品中的应用，日用化学品科学[J],2007,30(2)中指出，霍霍巴油可以通过不完全阻隔气体及水分的蒸发方式明显减少表皮水分的流失，另外作为一种优异的保湿剂，具有易铺展、润滑的作用，使皮肤光滑有弹性。
红花籽油含饱和脂肪酸6％，油酸21％，亚油酸73％。由于其主要成分是亚油酸，是食物油中亚油酸最高的油，所以营养价值很高，在医药、食品及化妆品等方面备受关注。例如，文献宝乐尔，红花籽油的研究进展，World Latest Medicine Information(Electronic Version)[J],2021,21(27):146-148中指出，红花籽油具有抗氧化作用，可有效清除自由基并还原由化学因素导致的自由基的能力，同时还具有抗衰老作用。文献姜黎，红花籽油的功效及应用前景分析，农产品加工[J],2017,6:56-58中指出，长期食用红花籽油可有效预防动脉粥样硬化、降低血脂和血清胆固醇的含量、软化血管，间接恢复神经系统等多种药效功能。
白池花籽油是已知最稳定的植物油之一，稳定性高是因为存在天然抗氧化剂生育酚。例如，文献苏帝翰，几种高氧化稳定性植物油中微量成分分析及其抗紫外抗氧化性能研究，香料香精化妆品[J],2019,4:47-51中检测了白池花籽油中生育酚的含量及抗氧化性能，通过清除DPPH表明白池花籽油具有一定的抗氧化性，可以防紫外线，促进皮肤微血管循环，使脸色自然红润有活力。
米糠油是一种营养丰富的植物油，富含不饱和脂肪酸、二十八烷醇以及γ-谷维素、植物甾醇、生育三烯酚、角鲨烯等功能性物质。米糠油中含有油酸40～50％，亚油酸29～42％，亚麻酸1％，棕榈酸12～20％。米糠油经过深加工，在化妆品中的应用非常广泛，应用于洗涤产品、防晒、抗衰老产品和皮肤病治疗等化妆品中。例如，文献张森旺，米糠的稳定化处理及其在化妆品种的应用，江西科学[J],2007,25(1):103-107中提出，乙酰化米糠油因其容易形成持久的抗水保护膜，具有柔软和调理功能，可作为液体柔软剂用于手用或体用的润肤膏，还可应用于洗发及护发产品中，使头发柔软、产生光泽感。
向日葵籽油中含有40％以上的不饱和脂肪酸，其中油酸38％、亚油酸55％左右，其亚油酸含量远超出花生油和芝麻油，易被人体吸收，在国际上被视为优质油脂。例如，文献赵富荣，葵花籽制油及综合利用，中国油脂[J],2005,30(1): 9-13中提出，葵花籽油中的维生素E与不饱和脂肪酸比例比较均衡，有利于人体摄入不饱和脂肪酸时的抗脂质过氧化保护，还能有效降低血清胆固醇水平，并具有降血压的作用，是很好的烹饪、人造奶油、起酥油、蛋黄酱和色拉油等产品的原料。
皮肤屏障，一般指皮肤物理屏障，包括皮肤表皮角质层和位于角质层表面的皮脂膜。角质层位于表皮的最外层，具有“砖-墙结构”，其中“砖块”指角质细胞，“砂浆”指细胞间脂。在皮肤屏障形成过程中，有200多个基因与皮肤屏障高度相关。例如，与角质包膜形成有关屏障因子丝聚合蛋白(FLG)、兜甲蛋白(LOR)、内皮蛋白(IVL)、转谷氨酰氨酶1(TGM1)，与屏障保湿相关因子胱天蛋白酶14(CASP14)、HMGCoA还原酶(HMGCR)、水通道蛋白3(AQP3)和角质细胞胞间连接相关因子闭锁小带蛋白1(ZO-1)。
具体来说，丝聚合蛋白(FLG)是皮肤表皮外层的角化包膜的一个重要的组成蛋白，主要存在于表皮颗粒层和透明层，是皮肤屏障的重要组成结构；并可进一步降解成具有亲水性的自由氨基酸和吸水性衍生物，帮助皮肤储存水分，维持皮肤含水量，具有保湿功效。兜甲蛋白(LOR)是角质包膜的主要组成成分，对表皮的屏障功能起重要作用。内皮蛋白(IVL)主要表达于棘细胞层上部与颗粒层，是角质形成细胞分化的标志性蛋白，位于角化包膜的外层，与含有羟基-OH的神经酰胺共价结合，由此将脂质基质和角化细胞连接起来而发挥作用。角化包膜的特性抗性和不溶性是基于由转谷氨酰胺酶1(TGM1)催化的非常稳定的异肽键的形成。
HMGCoA还原酶(HMGCR)是合成胆固醇的限速酶，存在于内质网，催化合成甲基二羟戊酸，之后经过脱羧、磷酸化等多步反应生成鲨烯，最后鲨烯环化为羊毛固醇后转变为胆固醇。水通道蛋白3(AQP3)是AQPs家族表达最丰富的水通道蛋白亚型，其在表皮的表达量具有空间层次，主要表达于人表皮基底层，棘细胞层、颗粒层，到角质层逐渐消失。这种空间性分布与皮肤的含水量分布一致：基底层和基底上部的水含量约为75％，而角质层仅约10％-15％。AQP3在基底膜带的高表达，可以促使水、甘油及尿素的转运，使得基底层的细胞外环境更接近于中性的平衡状态；而越接近角质层，AQP3的表达也越少，水分含量下降明显，皮肤内环境逐渐呈现酸性。此外，AQP3担 负着角质层甘油运输的重要作用，AQP3将内源性的甘油以及皮脂腺中的甘油三酯运输进入表皮，使其直接或间接影响皮肤保湿功效。
紧密连接是物理屏障中的重要组成部分，大多出现在皮肤表皮层，位于相邻细胞间隙的顶端侧面。紧密连接由不同类型的跨膜蛋白及细胞内胞质蛋白组成。跨膜蛋白如水闸蛋白1(CLDN1)、闭锁蛋白(OCLN)等；胞质蛋白如主要有闭锁小带蛋白-1(ZO-1)等。ZO-1是一种胞质蛋白，属于膜连接鸟苷酸激酶蛋白质家族，通过胞外信号传导途径来聚集闭锁蛋白和水闸蛋白，从而形成基本细胞连接条带；ZO-1是皮肤屏障功能中最具特征性的一种胞质蛋白。
植物仿生脂质技术(Phyto Bionic Sebum，简称PBS技术)：精选多种天然植物油，通过科学配比，模拟皮肤屏障结构中的天然脂质成分，补充皮肤角质层必需的不饱和脂肪酸，如亚麻酸、亚油酸等，补充皮肤缺失的脂质成分，与皮脂相容，从而快速修护皮肤屏障，令肌肤重焕健康、滋润、有光泽的状态。
其中：植物油脂主要来源于包括但不限于植物果实(例如：牛油果树果脂、油橄榄果油、杏仁油、鳄梨果油、沙棘果油、椰子果油、香橙果油、香柠檬果油、香橼果油、番茄果油、狗牙蔷薇果油、胡椒果油、巴西油桃木果油、扁叶香果兰果油、茴芹果油、毛瑞榈果油、欧刺柏果油、山鸡椒果油、温州蜜柑果油、星果棕果油、野蔷薇果油和芫荽果油等)、种子(例如：霍霍巴籽油、红花籽油、白池花籽油、向日葵籽油、澳洲坚果籽油、蓖麻籽油、牡丹籽油、葡萄籽油、葡萄柚籽油、苹果籽油、石榴籽油、西瓜籽油、西葫芦籽油、亚麻籽油、油菜籽油、芝麻籽油、玻璃苣籽油、伯尔硬胡桃籽油、草棉籽油、茶籽油、川谷籽油、番木瓜籽油、覆盆子籽油、猴面包树籽油、金盏花籽油、苦油树籽油、辣木籽油、美国山核桃籽油、紫苏籽油、巴巴苏籽油和白羽扇豆籽油等)和胚芽(例如：稻胚芽油、小麦胚芽油、燕麦胚芽油和玉米胚芽油等)，也有部分来源于植物的叶、皮、根、花瓣和花蕊等其他部位。
本发明意外地发现，植物果油(例如乳木果油、橄榄油等)和植物籽油(例如，霍霍巴油、红花籽油、向日葵籽油等)有皮肤屏障相关功效，可以提升皮肤屏障活力和促进皮肤屏障相关因子FLG、LOR、IVL、TGM1、CASP14、 HMGCR、AQP3和ZO-1的表达。因此，这种包含植物果油和植物籽油的组合物可以作为功效添加剂应用于药品和皮肤外用剂中。
发明内容
一方面，提供了一种包含植物油脂的组合物，所述植物油脂包括植物果油和植物籽油，其中，所述植物果油选自：乳木果油、橄榄果油、甜杏仁油、鳄梨果油、沙棘果油、椰子果油、香橙果油、香柠檬果油、香橼果油、番茄果油、狗牙蔷薇果油、胡椒果油、巴西油桃木果油、扁叶香果兰果油、茴芹果油、毛瑞榈果油、欧刺柏果油、山鸡椒果油、温州蜜柑果油、星果棕果油、野蔷薇果油、芫荽果油或它们的组合；其中，所述植物籽油选自：霍霍巴籽油、红花籽油、白池花籽油、向日葵籽油、米糠油、澳洲坚果籽油、蓖麻籽油、牡丹籽油、葡萄籽油、葡萄柚籽油、苹果籽油、石榴籽油、西瓜籽油、西葫芦籽油、亚麻籽油、油菜籽油、芝麻籽油、玻璃苣籽油、伯尔硬胡桃籽油、草棉籽油、茶籽油、川谷籽油、番木瓜籽油、覆盆子籽油、猴面包树籽油、金盏花籽油、苦油树籽油、辣木籽油、美国山核桃籽油、紫苏籽油、巴巴苏籽油、白羽扇豆籽油或它们的组合，其中，以所述组合物的总重量计，所述组合物包含至少0.5重量％的植物油脂。在优选的实施方式中，所述组合物包含植物果油和植物籽油，所述植物果油与所述植物籽油的重量比为2:8至8:2。
在优选的实施方式中，本发明组合物还包含天然表面活性剂，所述天然表面活性剂选自：卵磷脂、胆甾醇、羊毛脂、茶皂素、蛋白质、皂苷类、糖类、烷基多苷或它们的组合。在优选的实施方式中，所述天然表面活性剂是氢化卵磷脂。
在优选的实施方式中，组合物中植物油脂与天然表面活性剂的重量比为1:1至20:1。在更优选的实施方式中，组合物中植物油脂与天然表面活性剂的重量比为10:1至20:1。
另一方面，本发明还涉及包含植物油脂的组合物在增强皮肤屏障功能中的应用。在优选的实施方式中，所述增强皮肤屏障功能通过提升皮肤屏障活力和/或促进皮肤屏障相关因子的表达实现。
又一方面，本发明还涉及包含植物油脂的组合物在制备用于增强皮肤屏障 功能的药品和/或皮肤外用剂中的应用。在优选的实施方式中，所述药品和/或皮肤外用剂包含0.001-100重量％的所述组合物。
具体实施方式
本发明涉及包含植物果油和植物籽油的组合物及其应用，在研究中发现了所述组合物具有提升皮肤屏障活力和促进皮肤屏障相关因子FLG、LOR、IVL、TGM1、CASP14、HMGCR、AQP3和ZO-1的表达的作用。因此，包含植物果油和植物籽油的组合物可以作为功效添加剂，用于制备药品和/或皮肤外用剂，用于增强皮肤屏障功能。
为了提供更简明的描述，本文给出的一些数量表述没有用术语“约”修饰。应当理解，无论是否明确地使用了术语“约”，本文所给出的每个量都意在指代实际的给定值，并且还意在指代由本领域的普通技术人员可合理推测出的这些给定值的近似值，包括这些给定值的由实验和/或测量条件所引起的近似值。
为了提供更简洁的描述，本文中一些数量表述被叙述为约X量至约Y量的范围。应当理解，当叙述范围时，该范围并不限制于所叙述的上下界限，而应包括约X量至约Y量的整个范围或它们之间的任何量。
植物果油
本发明中的植物果油又称植物果实油脂，其主要来自于植物果实、种子和胚芽，也有部分来自植物的叶、皮、根、花瓣和花蕊等其他部位。植物果实油脂包括但不限于，牛油果树(Butyrospermum parkii)果脂(又名乳木果油)、油橄榄(Olea europaea)果油(又名橄榄油)、杏(Prunus armeniaca)仁油(又叫甜杏仁油)、鳄梨(Persea gratissima)果油、沙棘(Hippophae rhamnoides)果油、椰子(Cocos nucifera)果油、香橙(Citrus junos)果油、香柠檬(Citrus aurantium bergamia)果油、香橼(Citrus bedica limonum)果油、番茄(Solanum lycopersicum)果油、狗牙蔷薇(Rosa canina)果油、胡椒(Piper nigrum)果油、巴西油桃木(Caryocar brasiliense)果油、扁叶香果兰(Vanilla planifolia)果油、茴芹(Pimpinella anisum)果油、毛瑞榈(Mauritia flexuosa)果油、欧刺柏(Juniperus communis)果油、山鸡椒(Litsea cubeba)果油、温州蜜柑(Citrus  unshiu)果油、星果棕(Astrocaryum vulgare)果油、野蔷薇(Rosa multiflora)果油和芫荽(Coriandrum sativum)果油等。
例如，乳木果油与人体皮脂分泌油脂的各项指标较为接近，蕴含丰富的非皂化成分，易于人体吸收，能防止干燥开裂，进一步恢复并保持肌肤的自然弹性，保护肌肤屏障功能，同时还能起到消炎作用。橄榄油肤感略重，非常适合干性肌肤使用，其所含的角鲨烯和脂肪酸能被皮肤快速吸收，有效保持皮肤弹性和润泽，其中所含丰富的单不饱和脂肪酸、维生素、酚类物质能消除面部皱纹，防止肌肤衰老，有护肤护发和防止手足皲裂等功效。甜杏仁油可柔软、调理皮肤，对干燥、开裂、发痒或受刺激的皮肤有很好的修复和保湿功效，特别适用于干性和敏感性的肌肤。鳄梨油则用作化妆品的润滑剂，可促使皮肤平滑，具有良好的渗透性和保湿性，且能够促进皮肤细胞再生，对重建皮肤结构，修复晒伤及干燥皮肤有很好的效果。椰子油是饱和脂肪，脂质稳定，不易氧化产生自由基攻击，其很强的抗氧化能力能帮助人体防止自由基的产生，因此可用于美容护肤，其乳化稳定作用和抗氧化性，可使化妆品更加均匀细腻。
本发明意外地发现，包含植物果油(例如，乳木果油、橄榄油等)的组合物具有皮肤屏障相关功效，可以提升皮肤屏障活力和促进皮肤屏障相关因子FLG、LOR、IVL、TGM1、CASP14、HMGCR、AQP3和ZO-1的表达。
在一些实施方式中，本发明的组合物包含0.1-100重量％的植物果油。在优选的实施方式中，本发明的组合物包含0.1-50重量％的植物果油。在优选的实施方式中，本发明的组合物包含0.1-20重量％的植物果油。在优选的实施方式中，本发明的组合物包含0.5-10重量％的植物果油。
植物籽油
本发明中采用的植物籽油又称植物种子油脂，包括但不限于：霍霍巴籽油、红花籽油、白池花籽油和向日葵籽油。含有植物种子的油脂主要有霍霍巴(Simmondsia chinensis)籽油、红花(Carthamus tinctorius)籽油、白池花(Limnanthes alba)籽油、向日葵(Helianthus annuus)籽油、澳洲坚果(Macadamia ternifolia)籽油、蓖麻(Ricinus communis)籽油、牡丹(Paeonia suffruticosa)籽油、葡萄(Vitis vinifera)籽油、葡萄柚(Citrus paradisi)籽油、 苹果(Pyrus malus)籽油、石榴(Punica granatum)籽油、西瓜(Citrullus lanatus)籽油、西葫芦(Cucurbita pepo)籽油、亚麻(Linum usitatissimum)籽油、油菜(Brassica campestris)籽油、芝麻(Sesamum indicum)籽油、玻璃苣(Borago officinalis)籽油、伯尔硬胡桃(Sclerocarya birrea)籽油、草棉(Gossypium herbaceum)籽油、茶(Camellia sinensis)籽油、川谷(Coix lacryma-jobi ma-yuen)籽油、番木瓜(Carica papaya)籽油、覆盆子(Rubus idaeus)籽油、猴面包树(Adansonia digitata)籽油、金盏花(Calendula officinalis)籽油、苦油树(Carapa guaianensis)籽油、辣木(Moringa oleifera)籽油、美国山核桃(Carya illinoinensis)籽油、紫苏(Perilla ocymoides)籽油、巴巴苏(Orbignya oleifera)籽油和白羽扇豆(Lupinus albus)籽油等。
例如，霍霍巴籽油是渗透性最强的基础油，极易被皮肤吸收，清爽滋润、不油腻，能恢复皮肤pH平衡，去皱纹，有效改善油性皮肤，调理皮脂腺分泌机能，收缩毛孔，同时也是最佳的皮肤保湿油。红花籽油富含亚麻油酸、脂肪伴随物质(维生素E、维生素A)，与空气接触易变质，营养成份与应用与葵花油类似，加入化妆品中通常用于润肤及润滑成份，可以改善湿疹和粗糙的皮肤，使肌肤变得水嫩光滑，帮助新陈代谢正常化。白池花籽油则含有98％以上具有抗氧化作用的长链脂肪酸，具有独特的分子结构具有保湿功能，可以在肌肤表面形成锁水性薄膜，紧锁水分抵御干燥，同时也能舒展肌肤纹理，深层修复肌肤损失，提升肌肤整体轮廓。澳洲坚果籽油以富含不饱和脂肪酸为特点，能预防心脏病，这种单不饱和脂肪酸含量极高的天然植物油，能调节和控制血糖水平、改善糖尿病患者的脂质代谢，同时还能有效保湿护肤，是良好的防晒、护肤产品。
本发明意外地发现，包含植物籽油(例如，霍霍巴籽油、红花籽油、向日葵籽油等)的组合物具有皮肤屏障相关功效，可以提升皮肤屏障活力和促进皮肤屏障相关因子FLG、LOR、IVL、TGM1、CASP14、HMGCR、AQP3和ZO-1的表达。
在一些实施方式中，本发明的组合物包含0.1-100重量％的植物籽油。在优选的实施方式中，本发明的组合物包含0.1-50重量％的植物籽油。在优选的实施方式中，本发明的组合物包含0.1-20重量％的植物籽油。在优选的实施方 式中，本发明的组合物包含0.5-10重量％的植物籽油。
包含植物果油和植物籽油的组合物
在本发明的一些实施方式中，提供了一种包含植物果油和植物籽油的组合物，其中，所述植物果油与所述植物籽油的重量比为2:8至8:2。在优选的实施方式中，所述植物果油与所述植物籽油的重量比为1:1。
在一些实施方式中，本发明的组合物包含0.1-100重量％的植物果油和植物籽油。在优选的实施方式中，本发明的组合物包含0.1-50重量％的植物果油和植物籽油。在优选的实施方式中，本发明的组合物包含0.1-20重量％的植物果油和植物籽油。在优选的实施方式中，本发明的组合物包含0.5-10重量％的植物果油和植物籽油。
天然表面活性剂
本发明的组合物还可以包含天然表面活性剂。天然表面活性剂多来自动植物体，为较复杂的高分子有机物。由于其亲水性强，因而能形成乳浊液。而这类物质多有较高的粘度，有益于乳化稳定性。
本发明的组合物中包含的天然表面活性剂包括但不限于：卵磷脂、胆甾醇、羊毛脂、茶皂素、蛋白质、皂苷类、糖类、烷基多苷等。卵磷脂存在于生物细胞中，如动物卵、脑等组织及植物的种子或胚芽中，卵黄磷脂从蛋黄中提取；大豆中含有丰富的卵磷脂。卵磷脂具有乳化、分散、抗氧化等生理活性，是天然优良的表面活性剂，重要的乳化剂。
氢化卵磷脂具有较强的亲水性和保湿性，对皮肤和黏膜有很强的亲和力，用于化妆品的配方中可起到保湿、乳化和分散等作用；作为表面活性剂，还可以调理皮肤，使之达到一个很好的油水平衡效果，利用氢化卵磷脂还可以开发出护肤膏、护手霜、唇膏、防晒油等高级化妆产品。
在一些实施方式中，本发明的组合物包含0.1-20重量％的天然表面活性剂。在优选的实施方式中，本发明的组合物包含0.1-10重量％的天然表面活性剂。在优选的实施方式中，本发明的组合物包含0.1-5重量％的天然表面活性剂。在优选的实施方式中，本发明的组合物包含0.5-2重量％的天然表面活性 剂。
在优选的实施方式中，本发明的组合物中植物油脂(包括植物果油和植物籽油)与天然表面活性剂的重量比为1:1至20:1。在更优选的实施方式中，组合物中植物油脂(包括植物果油和植物籽油)与天然表面活性剂的重量比为10:1至20:1。
药品和/或皮肤外用剂
包含植物籽油的组合物可以被应用于药品和/或皮肤外用剂中，用于增强皮肤屏障功能。
在一些实施方式中，所述药品选自：片剂、胶囊、乳剂、混悬剂、粉末剂、颗粒剂、溶液剂、以及本领域已知的各种药品剂型。根据剂型的不同类型添加不同的用量。
在一些实施方式中，所述皮肤外用剂选自：洁面乳、化妆水、乳液、膏霜、啫喱、面膜。根据制剂的不同类型添加不同的用量。
所述皮肤外用剂是通常用于皮肤外部的所有成分的统称概念，例如可以是化妆品组合物。所述化妆品组合物中可以是基础化妆品、面部妆容化妆品、身体用化妆品、头发护理用化妆品等，对其剂型无特殊限制，根据不同目的可合理选择。所述化妆品组合物中根据剂型和目的的不同还含有不同的化妆品学层面允许的介质或基质赋形剂。
皮肤外用剂含有皮肤学上可接受的载体或媒介物(例如，洗液、面霜、软膏、清洁剂等等)。本领域普通技术人员能够根据本领域公知常识，选择能够以上文所述的浓度溶解或分散这些组分的载体。
本领域普通技术人员能够根据公知常识和它们以最适用于处理时活性组分的浓度而溶解或分散在活性组分中的能力来选择适宜的载体，所述载体例如包括水、醇类、油等。
本发明的皮肤外用剂可以是局部施用产品的形式，其能够从外部施用在皮肤上，并能够以本领域公知的那些普通技术制备。载体可以具有各种实际的形式，例如面霜，敷料，凝胶，洗液，软膏或者液体，其包括敷用和清洗掉的组合物，以及用本领域公知的方法将它们加入到例如干的或湿的涂抹物，水凝胶 基质，或粘性(或非粘性)贴片的材料载体中。优选地，载体是一种凝胶或增加水分的洗剂，或者以干或湿的形式的涂抹物。
典型的载体包括包含水和/或醇和润肤剂的乳剂，其中润肤剂是例如烃的油和蜡，硅油，透明质酸，植物、动物或海洋生物的脂肪或油，甘油酯衍生物，脂肪酸、或脂肪酸酯或醇或醇醚，羊毛脂及其衍生物，多元醇或酯，蜡酯，甾醇，磷脂等等，一般还有乳化剂(非离子的，阳离子的或阴离子的)，尽管一些润肤剂本身具有乳化特性。另外，可以利用其组分的不同比例和/或通过掺入例如树胶或其他形式的亲水胶体的增稠剂将这些相同组分配制成面霜、凝胶、或固体棒。
本发明的皮肤外用剂可以包含在皮肤护理组合物中通常能找到的附加组分，例如润肤剂、皮肤调节剂、乳化剂、防腐剂、抗氧化剂、香料、螯合剂等，只要它们与皮肤外用剂中其他的组分在物理上和化学上相容、且不影响本发明的植物籽油的效果即可。
在本发明的皮肤外用剂的一些实施方式中，可使用一种或多种防腐剂。适宜的防腐剂包括对羟基苯乙酮、C1-C4对羟基苯甲酸烷基酯和苯氧基乙醇。基于组合物总重量，防腐剂的用量为大约0.5至大约2重量％，优选大约0.5至1重量％。
在本发明的皮肤外用剂的一个实例中，可使用一种或多种抗氧化剂。适宜的抗氧化剂包括丁化羟基甲苯(BHT)、抗坏血酸棕榈酸酯(BHA)、丁羟茴醚、苯基-α-萘基胺、氢醌、没食子丙酯、去甲二氢愈创木酸、维生素E或维生素E的衍生物、维生素C及其衍生物、泛酸钙、绿茶提取物和混合的多酚，以及上面所述的物质的混合物。所使用的抗氧化剂是组合物总重量的大约0.02至0.5重量％，更最优选的是从大约0.002至0.1重量％的用量范围。
在本发明的皮肤外用剂的一个实例中，可使用一种或多种润肤剂，通过其保持在皮肤表面上或在角质层中的能力，起到润滑剂的作用，以减少剥落，改善皮肤的外观。典型的润肤剂包括脂肪酯、脂肪醇、矿物油、聚醚硅氧烷共聚物等等。适宜的润肤剂的例子非限定地包括，聚丙二醇(“PPG”)-15十八烷基醚，PPG-10十六烷基醚，Steareth-10，Oleth-8，PPG－4十二烷基醚，维生素E醋酸酯，羊毛脂，鲸蜡醇，鲸蜡硬脂醇乙基己酸酯，十六十八醇，甘油硬脂酸 酯，羟基硬脂酸辛脂，二甲基聚硅氧烷，以及它们的组合。鲸蜡醇，鲸蜡硬脂醇乙基己酸酯，十六十八醇，甘油硬脂酸酯以及它们的组合是优选的。使用时，润肤剂是基于组合物总重量的大约0.1至大约30重量％，优选大约1至大约30重量％的用量范围。
在本发明的皮肤外用剂的一个实例中，还可以使用一种或多种保湿剂。保湿剂也称为湿润剂，其有助于提高润肤剂的效果，减少剥落，刺激组成的鳞皮的去除和提高皮肤触感。可使用多元醇作为保湿剂，包括但并不限于，甘油，聚亚烷基二醇，亚烷基多元醇及其衍生物，包含丁二醇、丙二醇、双丙二醇，聚丙三醇，聚乙二醇及其衍生物，山梨醇，羟丙基山梨醇，己二醇，1,3－二丁二醇，1,2,6-己三醇，乙氧基化甘油，丙氧基化甘油，以及它们的组合。使用时，基于组合物的总重量，保湿剂的用量为大约0.1至大约20重量％，优选是大约1至大约15重量％。
在本发明的皮肤外用剂的一个实例中，可使用一种或多种乳化剂。乳化剂可在有效稳定量的范围内使用。优选地，在组合物总重量的基础上，以大约1.0至大约10.0重量％，更优选的是大约3.0至大约6.0重量％的用量来使用乳化剂。可以使用任何与组合物中的组分相容的乳化剂。适宜的乳化剂包括硬脂酸，鲸蜡醇，甘油硬脂酸酯，卵磷脂，十八烷醇，Steareth-2，Steareth-20，丙烯酸(酯)类/C10-30烷醇丙烯酸酯交联聚合物，以及它们的组合。
在本发明的皮肤外用剂的一个实例中，可使用一种或多种pH调节剂。本发明的皮肤外用剂中有益的pH调节剂包括氨丁三醇。使用时，基于组合物的总重量pH调节剂的用量为大约0.1至大约2重量％，优选是大约0.1至大约1重量％。
在本发明的一个具体实施方式中，皮肤外用剂包含丙烯酸(酯)类/C10-30烷醇丙烯酸酯交联聚合物、甘油、对羟基苯乙酮、甘油硬脂酸酯和卵磷脂、十六/十八醇、鲸蜡硬脂醇乙基己酸酯、氨丁三醇或它们的组合。
在本发明的一些实施方式中，本发明的组合物在皮肤外用剂中的用量为0.001％-100％(w/w)，优选的重量百分比为0.01％-60％(w/w)，更优选的重量百分比为0.01％-40％(w/w)。
实施例
下面结合具体实施例，以进一步阐述本发明。有必要在此指出的是，实施例只用于对本发明进行进一步的说明，不能理解为对本发明保护范围的限制，该领域的技术熟练人员可以根据上述本发明的内容做出一些非本质的改进和调整。下列实施例中未注明具体条件的试验方法，通常按照常规条件，或按照制造厂商所建议的条件。除非另有说明，所有的百分比和份数按重量计。
以下实施例中采用的实验材料包括：
牛油果树(BUTYROSPERMUM PARKII)果脂，商品名精制乳木果油，购自巴斯夫新材料有限公司
油橄榄(OLEA EUROPAEA)果油，商品名精制橄榄油，购自Textron Técnica,S.L.U.
霍霍巴籽油，商品名霍霍巴油，购自Vantage Specialty Ingredients,Inc.
红花(CARTHAMUS TINCTORIUS)籽油，商品名红花籽油，购自Northstar Lipids UK Ltd.
白池花(LIMNANTHES ALBA)籽油，商品名白池花籽油，购自海明斯特殊化学公司
向日葵(HELIANTHUS ANNUUS)籽油，商品名葵花籽油，购自嘉吉粮油(南通)有限公司
氢化卵磷脂，商品名氢化卵磷脂，购自NIKKO CHEMICALS CO.,LTD.。
实施例中采用的实验仪器包括：
称量天平：METTLER TOLEDO公司PB4002-N型
pH计：METTLER TOLEDO公司SEVENMULTI型
水浴锅：上海一恒科技有限公司HWS28型电热恒温水浴锅
均质机：POLYTRON公司PT 3100D型
台式搅拌机：IKA @EUROSTAR,power control-visc。
实施例1：制备组合物
称取0.5质量份氢化卵磷脂于烧杯中，加入99.5质量份的去离子水，搅拌均匀，待用。
实施例2：制备包含植物果油的组合物
称取0.5质量份氢化卵磷脂和0.5质量份乳木果油于烧杯中，边搅拌边加热至75-80℃，后再称取99质量份75-80℃的去离子水于烧杯中，开启均质，速度为3000转/分钟，均质5-10分钟，待用。
实施例3：制备包含植物果油的组合物
称取0.5质量份氢化卵磷脂和2.5质量份乳木果油于烧杯中，边搅拌边加热至75-80℃，后再称取97质量份75-80℃的去离子水于烧杯中，开启均质，速度为3000转/分钟，均质5-10分钟，待用。
实施例4：制备包含植物果油的组合物
称取0.5质量份氢化卵磷脂和5质量份乳木果油于烧杯中，边搅拌边加热至75-80℃，后再称取94.5质量份75-80℃的去离子水于烧杯中，开启均质，速度为3000转/分钟，均质5-10分钟，待用。
实施例5：制备包含植物果油的组合物
称取0.5质量份氢化卵磷脂和7.5质量份乳木果油于烧杯中，边搅拌边加热至75-80℃，后再称取92质量份75-80℃的去离子水于烧杯中，开启均质，速度为3000转/分钟，均质5-10分钟，待用。
实施例6：制备包含植物果油的组合物
称取0.5质量份氢化卵磷脂和10质量份乳木果油于烧杯中，边搅拌边加热至75-80℃，后再称取89.5质量份75-80℃的去离子水于烧杯中，开启均质，速度为3000转/分钟，均质5-10分钟，待用。
实施例7：制备包含植物籽油的组合物
称取0.5质量份氢化卵磷脂和0.5质量份霍霍巴油于烧杯中，边搅拌边加热至75-80℃，后再称取99质量份75-80℃的去离子水于烧杯中，开启 均质，速度为3000转/分钟，均质5-10分钟，待用。
实施例8：制备包含植物籽油的组合物
称取0.5质量份氢化卵磷脂和2.5质量份霍霍巴油于烧杯中，边搅拌边加热至75-80℃，后再称取97质量份75-80℃的去离子水于烧杯中，开启均质，速度为3000转/分钟，均质5-10分钟，待用。
实施例9：制备包含植物籽油的组合物
称取0.5质量份氢化卵磷脂和5质量份霍霍巴油于烧杯中，边搅拌边加热至75-80℃，后再称取94.5质量份75-80℃的去离子水于烧杯中，开启均质，速度为3000转/分钟，均质5-10分钟，待用。
实施例10：制备包含植物籽油的组合物
称取0.5质量份氢化卵磷脂和7.5质量份霍霍巴油于烧杯中，边搅拌边加热至75-80℃，后再称取92.5质量份75-80℃的去离子水于烧杯中，开启均质，速度为3000转/分钟，均质5-10分钟，待用。
实施例11：制备包含植物籽油的组合物
称取0.5质量份氢化卵磷脂和10质量份霍霍巴油于烧杯中，边搅拌边加热至75-80℃，后再称取89.5质量份75-80℃的去离子水于烧杯中，开启均质，速度为3000转/分钟，均质5-10分钟，待用。
实施例12：制备包含植物果油和植物籽油的组合物
称取0.5质量份氢化卵磷脂、5质量份乳木果油和5质量份霍霍巴油于烧杯中，边搅拌边加热至75-80℃，后再称取89.5质量份75-80℃的去离子水于烧杯中，开启均质，速度为3000转/分钟，均质5-10分钟，待用。
实施例13：制备包含植物果油和植物籽油的组合物
称取0.5质量份氢化卵磷脂、2质量份乳木果油和8质量份霍霍巴油于 烧杯中，边搅拌边加热至75-80℃，后再称取89.5质量份75-80℃的去离子水于烧杯中，开启均质，速度为3000转/分钟，均质5-10分钟，待用。
实施例14：制备包含植物果油和植物籽油的组合物
称取0.5质量份氢化卵磷脂、4质量份乳木果油和6质量份霍霍巴油于烧杯中，边搅拌边加热至75-80℃，后再称取89.5质量份75-80℃的去离子水于烧杯中，开启均质，速度为3000转/分钟，均质5-10分钟，待用。
实施例15：制备包含植物果油和植物籽油的组合物
称取0.5质量份氢化卵磷脂、6质量份乳木果油和4质量份霍霍巴油于烧杯中，边搅拌边加热至75-80℃，后再称取89.5质量份75-80℃的去离子水于烧杯中，开启均质，速度为3000转/分钟，均质5-10分钟，待用。
实施例16：制备包含植物果油和植物籽油的组合物
称取0.5质量份氢化卵磷脂、8质量份乳木果油和2质量份霍霍巴油于烧杯中，边搅拌边加热至75-80℃，后再称取89.5质量份75-80℃的去离子水于烧杯中，开启均质，速度为3000转/分钟，均质5-10分钟，待用。
实施例17：制备包含植物果油和植物籽油的组合物
称取0.5质量份氢化卵磷脂、5质量份乳木果油和5质量份橄榄油于烧杯中，边搅拌边加热至75-80℃，后再称取89.5质量份75-80℃的去离子水于烧杯中，开启均质，速度为3000转/分钟，均质5-10分钟，待用。
实施例18：制备包含植物果油和植物籽油的组合物
称取0.5质量份氢化卵磷脂、5质量份乳木果油和5质量份红花籽油于烧杯中，边搅拌边加热至75-80℃，后再称取89.5质量份75-80℃的去离子水于烧杯中，开启均质，速度为3000转/分钟，均质5-10分钟，待用。
实施例19：制备包含植物果油和植物籽油的组合物
称取0.5质量份氢化卵磷脂、5质量份乳木果油和5质量份白池花籽油于烧杯中，边搅拌边加热至75-80℃，后再称取89.5质量份75-80℃的去离子水于烧杯中，开启均质，速度为3000转/分钟，均质5-10分钟，待用。
实施例20：制备包含植物果油和植物籽油的组合物
称取0.5质量份氢化卵磷脂、5质量份乳木果油和5质量份米糠油于烧杯中，边搅拌边加热至75-80℃，后再称取89.5质量份75-80℃的去离子水于烧杯中，开启均质，速度为3000转/分钟，均质5-10分钟，待用。
实施例21：制备包含植物果油和植物籽油的组合物
称取0.5质量份氢化卵磷脂、5质量份乳木果油和5质量份向日葵籽油于烧杯中，边搅拌边加热至75-80℃，后再称取89.5质量份75-80℃的去离子水于烧杯中，开启均质，速度为3000转/分钟，均质5-10分钟，待用。
实施例22：制备包含植物籽油的组合物
称取0.5质量份氢化卵磷脂和5质量份红花籽油于烧杯中，边搅拌边加热至75-80℃，后再称取94.5质量份75-80℃的去离子水于烧杯中，开启均质，速度为3000转/分钟，均质5-10分钟，待用。
实施例23：制备包含植物果油的组合物
称取0.5质量份氢化卵磷脂和5质量份橄榄油于烧杯中，边搅拌边加热至75-80℃，后再称取94.5质量份75-80℃的去离子水于烧杯中，开启均质，速度为3000转/分钟，均质5-10分钟，待用。
实施例24：制备包含植物籽油的组合物
称取0.5质量份氢化卵磷脂和5质量份向日葵籽油于烧杯中，边搅拌边加热至75-80℃，后再称取94.5质量份75-80℃的去离子水于烧杯中，开启均质，速度为3000转/分钟，均质5-10分钟，待用。
实施例25：制备包含植物籽油的组合物
称取0.5质量份氢化卵磷脂和5质量份白池花籽油于烧杯中，边搅拌边加热至75-80℃，后再称取94.5质量份75-80℃的去离子水于烧杯中，开启均质，速度为3000转/分钟，均质5-10分钟，待用。
实施例26：制备组合物
称取100质量份乳木果油，待测试。
实施例27：制备组合物
称取100质量份霍霍巴油，待测试。
实施例28：制备组合物
称取100质量份红花籽油，待测试。
测试例1：3D表皮重组模型组织活力测试
3D表皮重组模型是一种人源的3D表皮模型，可以模拟角质形成细胞分化的表皮各层结构。本发明所采用的3D表皮重组模型组织活力测试方法，首先用皮肤刺激物SDS对模型造成一定的损伤，然后用适量实施例所制备的样品覆盖在损伤模型表面24小时进行修复。24小时后，清洗掉样品，用MTT法测试组织活力恢复情况。根据组织活力恢复情况，可对实施例样品的皮肤屏障修复能力进行评价。
1.试验材料
1.1细胞：皮肤模型为3D表皮皮肤模型
Figure PCTCN2022125277-appb-000001
(EpiSkin)。
1.2试剂：
3D皮肤模型维持培养基、3D皮肤模型检测培养基(EpiSkin)；十二烷基硫酸钠(SDS)(Sigma)；含钙镁DPBS(Gibco)；MTT(Sigma)；异丙醇、浓盐酸(国药集团)。
1.3主要设备
CO 2培养箱HERAcell 240i、生物安全柜1300SERIES A2、酶标仪 Multiskan Mk3(Thermo)；正向移液器M25(Gilson)；50mL连续加样器枪头Multipette plus(Eppendorf)；皮肤打孔器(面积0.38cm 2)。
2.实验方法：
3D重组表皮模型接收及复苏
接收3D表皮重组模型，检查包装完整性、核对模型数量，检查维持培养基、检测培养基的颜色和体积。确认无误后，开始进行模型复苏。
在生物安全柜中进行复苏操作。取一定数量的12孔板，在第一行中加入2毫升/孔的维持培养基，然后用镊子将3D重组表皮模型取出，用棉签小心去除表面凝胶，放入含维持培养基的孔中，复苏24小时。一块12孔板可复苏4个3D重组表皮模型。培养条件：5％CO 2，37℃恒温培养箱培养。
3D重组表皮模型损伤处理及加样品
用1×磷酸缓冲液(DPBS)溶液配置1.5％(质量体积比)十二烷基硫酸钠(SDS)溶液。
将模型分为空白对照组(不做任何处理，3个重复)、阴性对照组(用1.5％SDS进行损伤处理，3个重复)及实施例1-21和实施例26-28样品组(每个样品3个重复)。
先在12孔板第二行中加入2毫升/孔的维持培养基，然后用镊子将位于第一行中的3D重组表皮模型转移至对应的第二行中。
用移液器在阴性对照组和实施例1-6和实施例8-9样品组模型表面滴加50微升1.5％SDS溶液，并确保覆盖均匀，室温孵育15分钟。15分钟后，立即用1×DPBS清洗，并用棉签轻轻擦拭残余液体。再用活塞排代式移液器(M25)取15微升样品涂布在已损伤处理过(1.5％SDS)的样品组模型表面，处理24小时。所有模型放入细胞培养箱中，培养条件：5％CO 2，37℃恒温培养箱培养。
3D重组表皮模型活力测试
用1×DPBS配置3毫克/毫升的噻唑蓝(MTT)母液，再将MTT母液在测试培养基中稀释至0.3毫克/毫升。在12孔板第三行中加入2毫升/孔的稀释MTT溶液。
用50毫升连续加样器吸取1×DPBS，将模型表面的样品冲洗掉(不能直接对准样品进行冲洗，需对准皮肤模型支持框架侧壁)，然后用棉签吸去残余液体，放入12孔板第三行MTT溶液中。最后放入细胞培养箱中，置于37℃，5％CO 2的培养箱中孵育3小时。
配置酸性异丙醇，1.8毫升盐酸加入500毫升异丙醇中。取模型相应数量的1.5毫升的小型离心管(EP管)，每管中加入500微升酸性异丙醇。待表皮组织在MTT中孵育3小时后，用打孔器将表皮组织取下，用两把小号弯头镊子将表皮组织与其下的胶原底座分离，并将表皮组织翻转，然后将表皮组织和胶原底座一起转移至含酸性异丙醇的1.5毫升EP管中。将EP管在涡旋器上震荡混匀，放入4℃冰箱中72小时进行颜色萃取。同时，准备一支含1毫升酸性异丙醇EP管，作为酶标仪检测时的空白孔。
从4℃冰箱取出含酸性异丙醇和皮肤模型的1.5毫升EP管，震荡混匀溶液，每管取150微升萃取溶液转移到96孔板中，取3次，加入96孔板中。同时，准备3-6孔酸性异丙醇，作为检测时的空白对照，排除背景光密度值(OD值)。在570纳米波长下读取OD值。根据下面公式计算各组模型相对活力(空白对照组为100％)：
Figure PCTCN2022125277-appb-000002
3.结果判断
空白对照组为未损伤组，相对活力为100％；阴性对照组相对活力与空白对照组相比，控制在40-60％；样品组相对活力高于阴性对照组，表明该样品组有促进屏障修复的能力，该样品组低于阴性对照组，表明该样品组不具有促进屏障修复的能力。
表1：MTT法检测各组组织相对活力情况
Figure PCTCN2022125277-appb-000003
Figure PCTCN2022125277-appb-000004
Figure PCTCN2022125277-appb-000005
如表1所示，空白对照组皮肤模型组织平均相对活力为100％，阴性对照组(1.5％SDS处理)皮肤模型组织平均相对活力为41.0％。实施例1样品(乳木果油0％+霍霍巴油0％)皮肤模型组织平均相对活力为48.4％，实施例2样品(乳木果油0.5％)皮肤模型组织平均相对活力为64.1％，实施例3样品(乳木果油2.5％)皮肤模型组织平均相对活力为75.5％，实施例4样品(乳木果油5％)皮肤模型组织平均相对活力为75.3％，实施例5样品(乳木果油7.5％)皮肤模型组织平均相对活力为76.1％，实施例6样品(乳木果油10％)皮肤模型组织平均相对活力为76.1％，实施例7样品(霍霍巴油0.5％)皮肤模型组织平均相对活力为60.6％，实施例8样品(霍霍巴油2.5％)皮肤模型组织平均相对活力为57.0％，实施例9样品(霍霍巴油5％)皮肤模型组织平均相对活力为66.9％，实施例10样品(霍霍巴油7.5％)皮肤模型组织平均相对活力为68.9％，实施例11样品(霍霍巴油10％)皮肤模型组织平均相对活力为63.0％，实施例12样品(乳木果油5％+霍霍巴油5％)皮肤模型组织平均相对活力为66.5％，实施例13样品(乳木果油2％+霍霍巴油8％)皮肤模型组织平均相对活力为76.9％，实施例14样品(乳木果油4％+霍霍巴油6％)皮肤模型组织平均相对活力为69.7％，实施例15样品(乳木果油6％+霍霍巴油4％)皮肤模型组织平均相对活力为69.8％，实施例16样品(乳木果油8％+霍霍巴油2％)皮肤模型组织平均相对活力为57.4％，实施例17样品(乳木果油5％+橄榄油5％)皮肤模型组织平均相对活力为69.0％，实施例18样品(乳木果油5％+红花籽油5％) 皮肤模型组织平均相对活力为54.3％，实施例19样品(乳木果油5％+白池花籽油5％)皮肤模型组织平均相对活力为68.0％，实施例20样品(乳木果油5％+米糠油5％)皮肤模型组织平均相对活力为52.5％，实施例21样品(乳木果油5％+向日葵籽油5％)皮肤模型组织平均相对活力为54.2％，实施例26样品(乳木果油100％)皮肤模型组织平均相对活力为68.4％，实施例27样品(霍霍巴油100％)皮肤模型组织平均相对活力为65.2％，实施例28样品(红花籽油100％)皮肤模型组织平均相对活力为70.8％(见表1)。
综上，实施例2-6和26中乳木果油在浓度0.5-100％范围内具有较好的组织修复能力；实施例7-11和27中霍霍巴油在浓度0.5-100％范围内具有较好的组织修复能力；实施例12-16中乳木果油和霍霍巴油在复配比例5:5/2:8/4:6/6:4/8:2范围内具有较好的组织修复能力；实施例17-21中乳木果油复配橄榄油、红花籽油、米糠油和向日葵籽油(5％+5％)具有较好的组织修复能力。
测试例2：3D重组皮肤表皮模型屏障相关基因表达测试
3D表皮重组模型是一种人源的3D表皮模型，可以模拟角质形成细胞分化的表皮各层结构。将适量样品覆盖在表皮模型上24小时，然后收集表皮组织总核糖核酸(RNA)，采用RNA反转录技术和基因微阵列技术对皮肤屏障相关基因进行定量检测，进而评估样品的皮肤屏障保湿和修复能力。
1.试验材料
1.1细胞：皮肤模型为3D表皮皮肤模型
Figure PCTCN2022125277-appb-000006
(EpiSkin)。
1.2试剂：
3D皮肤模型维持培养基(EpiSkin)；含钙镁DPBS(Gibco)；异丙醇、75％无水乙醇(国药集团)；DEPC水(天根生物)；总RNA抽提试剂TRIzol(ThermoFisher)；反转录试剂盒iScript cDNA Synthesis Kit、荧光实时定量PCR试剂iTaq TM Universal
Figure PCTCN2022125277-appb-000007
Green Supermix(Bio-rad)。
1.3主要设备
CO 2培养箱HERAcell 240i、生物安全柜1300SERIES A2、超微量紫 外分光光度计NanoDrop ONE(Thermo)；基因扩增仪C1000Touch、实时定量PCR仪CFX Connect(Bio-rad)；高速冷冻离心机MIKRO 220R(Hittich)；正向移液器M25(Gilson)；50mL连续加样器枪头Multipette plus(Eppendorf)；皮肤打孔器(面积0.38cm 2)。
2.实验方法：
3D重组表皮模型接收及复苏
接收3D表皮重组模型，检查包装完整性、核对模型数量，检查维持培养基、检测培养基的颜色和体积。确认无误后，开始进行模型复苏。
在生物安全柜中进行复苏操作。取一定数量的12孔板，在第一行中加入2毫升/孔的维持培养基，然后用镊子将3D重组表皮模型取出，用棉签小心去除表面凝胶，放入含维持培养基的孔中，复苏24小时。一块12孔板可复苏4个3D重组表皮模型。培养条件：5％CO 2，37℃恒温培养箱培养。
3D重组表皮模型样品处理
将模型分为实施例1、4、9、12、17-25样品组(每个样品3个重复)及阳性对照组(罗格列酮，3个重复)。
先在12孔板第二行中加入2毫升/孔的维持培养基，然后用镊子将位于第一行中的3D重组表皮模型转移至对应的第二行中。
用活塞排代式移液器(M25)在阳性对照组中加入15微升罗格列酮溶液(100微摩尔，溶于1×DPBS)，在样品组中加入15微升样品，并用吸嘴在皮肤模型表面轻轻将样品涂布均匀，每个样品三个重复。所有模型放入细胞培养箱中，培养24小时。培养条件：5％CO 2，37℃恒温培养箱培养。
3D重组表皮模型收集总RNA样品
用50毫升连续加样器吸取1×DPBS，将模型表面的样品冲洗掉(不能直接对准样品进行冲洗，需对准皮肤模型支持框架侧壁)，然后用棉签吸去残余液体。用打孔器将表皮组织切下，并用两把小号弯头镊子将表皮组织与其下的胶原底座分离，将表皮组织放入含有1毫升总RNA抽提试剂 (TRIzol)的EP管中，用1毫升无RNA酶的移液器吸嘴反复吹打表皮组织，至仅剩透明状的角质层。随后，在原EP管中加入0.2毫升氯仿，剧烈振荡，低温高速离心15分钟。用无RNA酶的移液器吸嘴取上层水相500微升，然后加入等体积的预冷(负20度)的异丙醇颠倒混匀，低温高速离心10分钟。离心后的RNA在EP管底部形成白色片状沉淀，用75％乙醇漂洗两次，用离心机和吸嘴去掉残留乙醇，开盖室温晾干至透明状。用40微升无RNA酶的H 2O溶解，混匀。再用微量分光光度计Nanodrop测RNA浓度，并用琼脂糖凝胶电泳检测RNA的完整性。溶解后的表皮模型组织总RNA用于后续实验或分装后放-80℃长期保存。
RT-qPCR法定量检测皮肤屏障相关基因
取1微克总RNA进行反转录，采用反转录试剂盒iScript cDNA Synthesis Kit反转录得到cDNA。
反转录体系如下：
Figure PCTCN2022125277-appb-000008
反转录程序如下：25℃，5分钟；42℃，30分钟；85℃，5分钟。
用荧光实时定量聚合酶链式反应(PCR)试剂iTaq TM Universal
Figure PCTCN2022125277-appb-000009
Green Supermix进行荧光实时定量检测，分析屏障相关基因信使RNA(mRNA)表达情况。
反应体系如下：
Figure PCTCN2022125277-appb-000010
Figure PCTCN2022125277-appb-000011
反应程序如下：95℃，30秒；95℃，15秒，60℃，30秒，40个循环；65-95℃，每次降低0.5℃(熔解曲线)。
本实施例所用引物序列设计如下：
Figure PCTCN2022125277-appb-000012
采用2 -△△Ct法，分析实施例样品组及阳性对照组(罗格列酮)基因表达相对于实施例1对照组的基因变化情况。
3.结果判断
实施例1样品组基因表达量作为100％，各组与之相比，大于100％，表明基因表达上调，小于100％，表明基因表达下调。FLG、LOR等基因上调，表明该样品组有保湿和促进屏障修复的能力；FLG、LOR等基因下调，表明该样品组不具有保湿和促进屏障修复的能力。
表2：各组样品处理后的皮肤屏障因子表达情况
Figure PCTCN2022125277-appb-000013
Figure PCTCN2022125277-appb-000014
如表2所示，实施例1(乳木果油0％+霍霍巴油0％)作为对照，其基 因相对表达量为100％，实施例4、9、12、17、18、19、20、21、22、23、24和25样品和阳性对照样品的基因表达情况与之相比，得到相应百分比。
具体来说，屏障因子FLG在实施例4样品(乳木果油5％)、实施例9样品(霍霍巴油5％)、实施例12样品(乳木果油5％+霍霍巴油5％)、实施例17样品(乳木果油5％+橄榄油5％)、实施例18样品(乳木果油5％+红花籽油5％)、实施例19样品(乳木果油5％+白池花籽油5％)、实施例20样品(乳木果油5％+米糠油5％)、实施例21样品(乳木果油5％+向日葵籽油5％)、实施例22样品(红花籽油5％)、实施例23样品(橄榄油5％)、实施例24样品(向日葵籽油5％)、实施例25样品(白池花籽油5％)和阳性对照(罗格列酮)处理后，与实施例1样品(乳木果油0％+霍霍巴油0％)相比，分别为222％、218％、225％、265％、283％、223％、258％、213％、274％、205％、283％、175％和362％。
具体来说，屏障因子LOR在实施例4样品(乳木果油5％)、实施例9样品(霍霍巴油5％)、实施例12样品(乳木果油5％+霍霍巴油5％)、实施例17样品(乳木果油5％+橄榄油5％)、实施例18样品(乳木果油5％+红花籽油5％)、实施例19样品(乳木果油5％+白池花籽油5％)、实施例20样品(乳木果油5％+米糠油5％)、实施例21样品(乳木果油5％+向日葵籽油5％)、实施例22样品(红花籽油5％)、实施例23样品(橄榄油5％)、实施例24样品(向日葵籽油5％)、实施例25样品(白池花籽油5％)和阳性对照(罗格列酮)处理后，与实施例1样品(乳木果油0％+霍霍巴油0％)相比，分别为240％、236％、227％、242％、247％、208％、281％、217％、307％、216％、293％、201％和351％。
具体来说，屏障因子IVL在实施例4样品(乳木果油5％)、实施例9样品(霍霍巴油5％)、实施例12样品(乳木果油5％+霍霍巴油5％)、实施例17样品(乳木果油5％+橄榄油5％)、实施例18样品(乳木果油5％+红花籽油5％)、实施例19样品(乳木果油5％+白池花籽油5％)、实施例20样品(乳木果油5％+米糠油5％)、实施例21样品(乳木果油5％+向日葵籽油5％)、实施例22样品(红花籽油5％)、实施例23样品(橄榄油5％)、实施例24样品(向日葵籽油5％)、实施例25样品(白池花籽油 5％)和阳性对照(罗格列酮)处理后，与实施例1样品(乳木果油0％+霍霍巴油0％)相比，分别为113％、87％、130％、107％、109％、125％、127％、127％、117％、97％、90％、103％和103％。
具体来说，屏障因子TGM1在实施例4样品(乳木果油5％)、实施例9样品(霍霍巴油5％)、实施例12样品(乳木果油5％+霍霍巴油5％)、实施例17样品(乳木果油5％+橄榄油5％)、实施例18样品(乳木果油5％+红花籽油5％)、实施例19样品(乳木果油5％+白池花籽油5％)、实施例20样品(乳木果油5％+米糠油5％)、实施例21样品(乳木果油5％+向日葵籽油5％)、实施例22样品(红花籽油5％)、实施例23样品(橄榄油5％)、实施例24样品(向日葵籽油5％)、实施例25样品(白池花籽油5％)和阳性对照(罗格列酮)处理后，与实施例1样品(乳木果油0％+霍霍巴油0％)相比，分别为134％、126％、176％、170％、176％、201％、161％、160％、201％、156％、146％、149％和161％。
具体来说，屏障因子CASP14在实施例4样品(乳木果油5％)、实施例9样品(霍霍巴油5％)、实施例12样品(乳木果油5％+霍霍巴油5％)、实施例17样品(乳木果油5％+橄榄油5％)、实施例18样品(乳木果油5％+红花籽油5％)、实施例19样品(乳木果油5％+白池花籽油5％)、实施例20样品(乳木果油5％+米糠油5％)、实施例21样品(乳木果油5％+向日葵籽油5％)、实施例22样品(红花籽油5％)、实施例23样品(橄榄油5％)、实施例24样品(向日葵籽油5％)、实施例25样品(白池花籽油5％)和阳性对照(罗格列酮)处理后，与实施例1样品(乳木果油0％+霍霍巴油0％)相比，分别为188％、275％、169％、201％、228％、162％、175％、192％、493％、198％、248％、279％和330％。
具体来说，屏障因子HMGCR在实施例4样品(乳木果油5％)、实施例9样品(霍霍巴油5％)、实施例12样品(乳木果油5％+霍霍巴油5％)、实施例17样品(乳木果油5％+橄榄油5％)、实施例18样品(乳木果油5％+红花籽油5％)、实施例19样品(乳木果油5％+白池花籽油5％)、实施例20样品(乳木果油5％+米糠油5％)、实施例21样品(乳木果油5％+向日葵籽油5％)、实施例22样品(红花籽油5％)、实施例23样品(橄 榄油5％)、实施例24样品(向日葵籽油5％)、实施例25样品(白池花籽油5％)和阳性对照(罗格列酮)处理后，与实施例1样品(乳木果油0％+霍霍巴油0％)相比，分别为170％、223％、226％、208％、253％、213％、199％、192％、242％、188％、202％、175％和229％。
具体来说，屏障因子AQP3在实施例4样品(乳木果油5％)、实施例9样品(霍霍巴油5％)、实施例12样品(乳木果油5％+霍霍巴油5％)、实施例17样品(乳木果油5％+橄榄油5％)、实施例18样品(乳木果油5％+红花籽油5％)、实施例19样品(乳木果油5％+白池花籽油5％)、实施例20样品(乳木果油5％+米糠油5％)、实施例21样品(乳木果油5％+向日葵籽油5％)、实施例22样品(红花籽油5％)、实施例23样品(橄榄油5％)、实施例24样品(向日葵籽油5％)、实施例25样品(白池花籽油5％)和阳性对照(罗格列酮)处理后，与实施例1样品(乳木果油0％+霍霍巴油0％)相比，分别为112％、105％、141％、125％、133％、116％、163％、172％、148％、99％、116％、97％和131％。
具体来说，屏障因子ZO-1在实施例4样品(乳木果油5％)、实施例9样品(霍霍巴油5％)、实施例12样品(乳木果油5％+霍霍巴油5％)、实施例17样品(乳木果油5％+橄榄油5％)、实施例18样品(乳木果油5％+红花籽油5％)、实施例19样品(乳木果油5％+白池花籽油5％)、实施例20样品(乳木果油5％+米糠油5％)、实施例21样品(乳木果油5％+向日葵籽油5％)、实施例22样品(红花籽油5％)、实施例23样品(橄榄油5％)、实施例24样品(向日葵籽油5％)、实施例25样品(白池花籽油5％)和阳性对照(罗格列酮)处理后，与实施例1样品(乳木果油0％+霍霍巴油0％)相比，分别为143％、151％、160％、138％、147％、128％、180％、190％、203％、131％、170％、134％和246％。
综上，实施例4样品(乳木果油5％)促进FLG、LOR、IVL、TGM1、CASP14、HMGCR、AQP3和ZO-1屏障因子的表达，有利于屏障形成，具有促进皮肤保湿和屏障修护功效。实施例9样品(霍霍巴油5％)促进FLG、LOR、TGM1、CASP14、HMGCR、AQP3和ZO-1屏障因子的表达，有利于屏障形成，具有促进皮肤保湿和屏障修护功效。实施例12样品(乳木果 油5％+霍霍巴油5％)促进FLG、LOR、IVL、TGM1、CASP14、HMGCR、AQP3和ZO-1屏障因子的表达，有利于屏障形成，具有促进皮肤保湿和屏障修护功效。实施例17样品(乳木果油5％+橄榄油5％)促进FLG、LOR、IVL、TGM1、CASP14、HMGCR、AQP3和ZO-1屏障因子的表达，有利于屏障形成，具有促进皮肤保湿和屏障修护功效。实施例18样品(乳木果油5％+红花籽油5％)促进FLG、LOR、IVL、TGM1、CASP14、HMGCR、AQP3和ZO-1屏障因子的表达，有利于屏障形成，具有促进皮肤保湿和屏障修护功效。实施例19样品(乳木果油5％+白池花籽油5％)促进FLG、LOR、IVL、TGM1、CASP14、HMGCR、AQP3和ZO-1屏障因子的表达，有利于屏障形成，具有促进皮肤保湿和屏障修护功效。实施例20样品(乳木果油5％+米糠油5％)促进FLG、LOR、IVL、TGM1、CASP14、HMGCR、AQP3和ZO-1屏障因子的表达，有利于屏障形成，具有促进皮肤保湿和屏障修护功效。实施例21样品(乳木果油5％+向日葵籽油5％)促进FLG、LOR、IVL、TGM1、CASP14、HMGCR、AQP3和ZO-1屏障因子的表达，有利于屏障形成，具有促进皮肤保湿和屏障修护功效。实施例22样品(红花籽油5％)促进FLG、LOR、IVL、TGM1、CASP14、HMGCR、AQP3和ZO-1屏障因子的表达，有利于屏障形成，具有促进皮肤保湿和屏障修护功效。实施例23样品(橄榄油5％)促进FLG、LOR、TGM1、CASP14、HMGCR、AQP3和ZO-1屏障因子的表达，有利于屏障形成，具有促进皮肤保湿和屏障修护功效。实施例24样品(向日葵籽油5％)促进FLG、LOR、TGM1、CASP14、HMGCR、AQP3和ZO-1屏障因子的表达，有利于屏障形成，具有促进皮肤保湿和屏障修护功效。实施例25样品(白池花籽油5％)促进FLG、LOR、IVL、TGM1、CASP14、HMGCR和ZO-1屏障因子的表达，有利于屏障形成，具有促进皮肤保湿和屏障修护功效。
应用例
本发明所述的包含植物果油和/或植物籽油的组合物可以作为中间体原料或功效添加剂用于药品或皮肤外用剂的制备，所述皮肤外用剂优选为化妆品组合物，包括但不限于膏霜、乳液、啫喱、化妆水、精华液、面膜、 眼霜、气雾(清洁泡)、喷雾、沐浴露、按摩油、洗面奶等剂型的产品的制备。
本发明所述包含植物果油和/或植物籽油的组合物在皮肤外用剂中的重量百分比为0.001％-100％(w/w)；优选的重量百分比为0.01％-60％(w/w)；最优选的重量百分比为0.01％-40％(w/w)。
以下是实施例3、7、9、20和23获得的包含植物果油和/或植物籽油的组合物在皮肤外用剂中的具体应用例，以及这些剂型的配方和制备方法。具体应用例如下：
应用例1：面霜的制备
Figure PCTCN2022125277-appb-000015
Figure PCTCN2022125277-appb-000016
应用例2：乳液的制备
Figure PCTCN2022125277-appb-000017
应用例3：眼霜的制备
Figure PCTCN2022125277-appb-000018
Figure PCTCN2022125277-appb-000019
应用例4：面膜的制备
Figure PCTCN2022125277-appb-000020
Figure PCTCN2022125277-appb-000021
应用例5：精华液的制备
Figure PCTCN2022125277-appb-000022
Figure PCTCN2022125277-appb-000023
应用例6：本发明中的实施例2-28也可以单独作为皮肤外用剂单独使用。

Claims (10)

  1. 一种包含植物油脂的组合物，所述植物油脂包括植物果油和植物籽油，
    其中，所述植物果油选自：乳木果油、橄榄果油、甜杏仁油、鳄梨果油、沙棘果油、椰子果油、香橙果油、香柠檬果油、香橼果油、番茄果油、狗牙蔷薇果油、胡椒果油、巴西油桃木果油、扁叶香果兰果油、茴芹果油、毛瑞榈果油、欧刺柏果油、山鸡椒果油、温州蜜柑果油、星果棕果油、野蔷薇果油、芫荽果油或它们的组合；
    其中，所述植物籽油选自：霍霍巴籽油、红花籽油、白池花籽油、向日葵籽油、米糠油、澳洲坚果籽油、蓖麻籽油、牡丹籽油、葡萄籽油、葡萄柚籽油、苹果籽油、石榴籽油、西瓜籽油、西葫芦籽油、亚麻籽油、油菜籽油、芝麻籽油、玻璃苣籽油、伯尔硬胡桃籽油、草棉籽油、茶籽油、川谷籽油、番木瓜籽油、覆盆子籽油、猴面包树籽油、金盏花籽油、苦油树籽油、辣木籽油、美国山核桃籽油、紫苏籽油、巴巴苏籽油、白羽扇豆籽油或它们的组合，
    其中，以所述组合物的总重量计，所述组合物包含至少0.5重量％的植物油脂。
  2. 如权利要求1所述的组合物，所述组合物包含植物果油和植物籽油，所述植物果油与所述植物籽油的重量比为2:8至8:2。
  3. 如权利要求1所述的组合物，其中，所述组合物还包含天然表面活性剂，所述天然表面活性剂选自：卵磷脂、胆甾醇、羊毛脂、茶皂素、蛋白质、皂苷类、糖类、烷基多苷或它们的组合。
  4. 如权利要求3所述的组合物，其中，所述天然表面活性剂是氢化卵磷脂。
  5. 如权利要求3-4中任一项所述的组合物，其中，所述植物油脂与所述天然表面活性剂的重量比为1:1至20:1。
  6. 如权利要求5所述的组合物，其中，所述植物油脂与所述天然表面活性剂的重量比为10:1至20:1。
  7. 如权利要求1所述的组合物在增强皮肤屏障功能中的应用。
  8. 如权利要求7所述的应用，其中，所述增强皮肤屏障功能通过提升皮 肤屏障活力和/或促进皮肤屏障相关因子的表达实现。
  9. 如权利要求1所述的组合物在制备用于增强皮肤屏障功能的药品和/或皮肤外用剂中的应用。
  10. 如权利要求9所述的应用，所述药品和/或皮肤外用剂包含0.001-100重量％的所述组合物。
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