WO2023109290A1 - Composition containing microbial oil and vegetable oil and use thereof - Google Patents

Composition containing microbial oil and vegetable oil and use thereof Download PDF

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Publication number
WO2023109290A1
WO2023109290A1 PCT/CN2022/125279 CN2022125279W WO2023109290A1 WO 2023109290 A1 WO2023109290 A1 WO 2023109290A1 CN 2022125279 W CN2022125279 W CN 2022125279W WO 2023109290 A1 WO2023109290 A1 WO 2023109290A1
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Prior art keywords
oil
fruit
seed oil
skin
seed
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PCT/CN2022/125279
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French (fr)
Chinese (zh)
Inventor
张瑶瑶
殷庆飞
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上海家化联合股份有限公司
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Publication of WO2023109290A1 publication Critical patent/WO2023109290A1/en

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/92Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof
    • A61K8/922Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof of vegetable origin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/02Algae
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/02Algae
    • A61K36/05Chlorophycota or chlorophyta (green algae), e.g. Chlorella
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0014Skin, i.e. galenical aspects of topical compositions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/16Emollients or protectives, e.g. against radiation
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q17/00Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin

Definitions

  • the invention belongs to the field of cosmetics, and in particular relates to a composition containing microbial oil and vegetable oil and its application in skin barrier function.
  • the skin is the largest organ in the human body, covering the entire body surface and playing an important role as a barrier.
  • the skin barrier function not only refers to its physical barrier function, but also includes skin pigment barrier function, nerve barrier function, immune barrier function and many other aspects related to skin function; narrow skin barrier function usually Refers to the physical or mechanical barrier structure of the epidermis, especially the stratum corneum. Having a healthy skin barrier is tantamount to having beautiful, natural-looking skin. However, due to factors such as environment, diet and wrong skin care, the skin barrier is damaged, which makes the skin's own defense ability insufficient, and the skin is extremely sensitive and damaged. Used in cosmetics, oil can make the skin soft, lubricated and purify the surface.
  • Microbial oil is another new edible oil resource developed by humans after vegetable oil and animal oil.
  • Microorganisms capable of producing oil include yeast, mold, bacteria, and algae. Among them, eukaryotic yeast, mold, and algae can synthesize triglycerides similar to vegetable oil, while prokaryotic bacteria can synthesize special lipids.
  • Microalgae contains essential nutrients such as protein, fat, carbohydrates and vitamins, etc., and the content of oil is relatively high. The content of neutral fat accounts for about 20-50% of the dry weight of cells, and a few microalgae can reach 75%. The amount of oil is significantly higher than that of agricultural oil crops. Therefore, microalgae oil is considered to be the oil resource with the most development potential, and has received great attention internationally.
  • omega-3 series such as eicosapentaenoic acid (EPA) and docosahexaenoic acid Dienoic acid (DHA); omega-6 linoleic acid series and omega-9 oleic acid series.
  • EPA eicosapentaenoic acid
  • DHA Dienoic acid
  • omega-6 linoleic acid series and omega-9 oleic acid series.
  • Polyunsaturated fatty acids can regulate blood lipids, enhance the body's immunity, nourish the brain and improve the symptoms of arthritis and relieve pain.
  • omega-3 series fatty acids are beneficial to the health of brain and retina, skin and kidney function. It is very important. DHA is called melatonin. It has important functions for the nervous system. It has the functions of strengthening the brain, improving memory and vision. It can especially promote the development of fetal brain cells and the growth of infant brain cells, and promote the improvement of memory in teenagers. Prevention and treatment of senile dementia.
  • 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 oil is a natural compound formed by the reaction of higher fatty acids and glycerol, which is widely distributed in nature. All fats extracted from plant seeds, pulp and other parts are collectively referred to as vegetable oils.
  • 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.
  • Common vegetable oils include avocado (Butyrospermum parkii) fruit fat (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, jojoba (Simmondsia chinensis) seed oil, safflower (Carthamus tinctorius) seed oil, white pond flower (Limnanthes alba) seed oil, sunflower (Helianthus annuus) seed oil, etc.
  • Vegetable oil has a skin-friendly texture and is close to the human sebum membrane structure. It is easier to be absorbed by the skin than water and has better permeability, so it can penetrate deeply and nourish the skin.
  • 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.
  • the barrier factors filaggrin (FLG), loricrin (LOR), endothelin (IVL), transglutaminase 1 (TGM1), and barrier moisturizing factor caspase 14 are related to the formation of the corneous envelope. (CASP14), HMGCoA reductase (HMGCR), aquaporin 3 (AQP3) and keratinocyte intercellular junction-associated factor zona occlusin 1 (ZO-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 is responsible for the important role of glycerol transport in the stratum corneum. AQP3 transports endogenous glycerol 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 microbial oils (such as microalgae oil, etc.) and vegetable oils (such as jojoba oil, safflower seed oil, sunflower seed oil, etc.) have skin barrier-related effects, which can enhance the vitality of the skin barrier and promote skin barrier function. Expression of related factors FLG, LOR, IVL, TGM1, CASP14, HMGCR, AQP3 and ZO-1. Therefore, the composition comprising microbial oil and vegetable oil can be used as an efficacy additive in medicines and external skin preparations.
  • microbial oils such as microalgae oil, etc.
  • vegetable oils such as jojoba oil, safflower seed oil, sunflower seed oil, etc.
  • the present invention provides an oil composition
  • the oil includes microbial oil and vegetable oil, wherein, based on the total weight of the composition, the composition comprises at least 0.5% by weight of oil.
  • the weight ratio of microbial oil to vegetable oil in the oil composition of the present invention is 1:8 to 8:1.
  • the oil composition of the present invention also includes a natural surfactant selected from the group consisting of: lecithin, cholesterol, lanolin, tea saponin, protein, saponins, sugars, alkanes base polyglycosides or their combinations.
  • a natural surfactant selected from the group consisting of: lecithin, cholesterol, lanolin, tea saponin, protein, saponins, sugars, alkanes base polyglycosides or their combinations.
  • the natural surfactant is hydrogenated lecithin.
  • the weight ratio of oil and natural surfactant in the oil composition of the present invention is 1:1 to 20:1. In a more preferred embodiment, the weight ratio of vegetable oil to natural surfactant in the oil composition of the present invention is 10:1 to 20:1.
  • the vegetable oil in the oil composition of the present invention is vegetable seed oil, vegetable fruit oil or a combination thereof.
  • the vegetable seed oil is selected from: jojoba seed oil, safflower seed oil, white pond flower seed oil, sunflower seed oil, macadamia nut seed oil, castor oil, peony seed oil, grape seed oil, grapefruit seed oil 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 Hard Walnut Seed Oil, Cottonseed Oil, Tea Seed Oil, Guava Seed Oil, Papaya Seed Oil, Raspberry Seed Oil, Baobab Seed Oil, Calendula Seed Oil, Oleifera Seed Oil, Moringa Seed Oil, American Pecan Seed Oil, Perilla Seed Oil, Babassu seed oil, white lupine seed oil, or a combination thereof.
  • the plant fruit oil is selected from: shea butter, olive 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, dog tooth rosehip oil, pepper fruit oil, Brazilian nectarine fruit oil, flat-leaf pimento fruit oil, anise fruit oil, mulberry fruit oil, juniper fruit oil, pheasant fruit oil, Satsuma fruit oil, star palm fruit oil, rosehip oil, coriander fruit oil or a combination thereof.
  • the microbial oil in the oil composition of the present invention is selected from: oil of microalgae, oil of Haematococcus pluvialis, oil of Dentate algae or combinations thereof.
  • the present invention also relates to the application of the oil composition 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 oil composition in the preparation of medicines and/or skin external preparations for enhancing 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 microbial oil and vegetable 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, AQP3 and Effect of ZO-1 Expression. Therefore, the composition comprising microbial oil and vegetable oil can be used as an efficacy additive for the preparation of medicines and/or skin external preparations for enhancing the skin barrier function.
  • the composition of the present invention comprises microbial oil selected from: microalgae oil, Haematococcus Pluvialis (HAEMATOCOCCUS PLUVIALIS) oil, long ear algae (ODONTELLA AURITA) oil.
  • microalgae oil is an additive in health products, medicine and cosmetics, and can also be used as a renewable energy source for edible oil. In terms of food, microalgae oil can be used as a functional nutritional enhancer or directly made into health care products.
  • Microalgae oil not only contains unsaturated fatty acids such as DHA and EPA, but also contains hydrocarbons and trace alcohols that are beneficial to human health .
  • microalgae oil In terms of medicine, functional polyunsaturated fatty acids in microalgae oil can be used as medicine. At present, linoleic acid and arachidonic acid in microalgae oil are widely used in the medical field. Congestion and digestive system ulcers and other diseases are very effective. In the farming industry, microalgae oil can be added to the feed to obtain the functional agricultural and sideline products we want.
  • the microalgae oil in the present invention is glyceryl trioleate, which is rich in more than 90% of omega-9 unsaturated fatty acid beneficial to human body, ie oleic acid.
  • Oleic acid is a monounsaturated fatty acid commonly found in the diet and is not an essential fatty acid, but it still has benefits for general health. Omega-9s are found in olives, almonds, queensland nuts, hazelnuts, sesame, avocado, flaxseed and their oils. High consumption of olive oil in Mediterranean countries has been linked to lower rates of breast cancer and heart disease. Research from the University of California pointed out that a diet high in monounsaturated fatty acids can prevent the oxidation of low-density lipoprotein cholesterol and protect blood vessel walls. This type of fat can also promote the function of high-density cholesterol to control low-density cholesterol. Saturated fat makes the antioxidant vitamin E more effective in protecting cells from free radical damage.
  • compositions comprising microbial oils have skin barrier-related effects, can enhance skin barrier vitality and promote skin barrier-related factors FLG, LOR, IVL, TGM1, CASP14, HMGCR, AQP3 and Expression of ZO-1.
  • the composition of the present invention comprises 0.1-100% by weight of microbial oil. In a preferred embodiment, the composition of the present invention comprises 0.1-50% by weight of microbial oil. In a preferred embodiment, the composition of the present invention comprises 0.1-20% by weight of microbial oil. In a preferred embodiment, the composition of the present invention comprises 0.5-10% by weight of microbial oil.
  • Vegetable oil is widely used in food, industry, cosmetics and medicine.
  • the most widely used vegetable oil in cosmetics is shea butter.
  • Shea butter has many effects and functions, such as excellent nourishing and moisturizing functions. This is because Shea butter is rich in unsaponifiable substances, contains a lot of fat and fatty acids, etc., and has a strong moisturizing function.
  • high-quality shea butter has good UV protection because it contains an excellent natural sunscreen ingredient-cinnamic acid, which can absorb ultraviolet rays in the sun and protect the skin from sun damage;
  • high-quality milk Argan oil also has very effective anti-inflammatory and anti-allergic functions, so it is suitable for relatively weak and sensitive parts such as eyes and lips, and its phytosterol component has a good anti-inflammatory and repairing effect on injured skin.
  • compositions of the present invention may comprise vegetable fats and oils from various sources.
  • compositions of the invention comprise vegetable fruit oils.
  • Vegetable fruit oil also known as plant fruit oil, mainly comes from plant fruits, seeds and germs, and some come from other parts of plants such as leaves, bark, roots, petals and stamens.
  • 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 (Piper nigrum) Fruit Oil, Brazilian Nectarine (Caryocar brasiliense) Fruit Oil, Flat Leaf Pansy ( Vanilla planifolia) fruit oil, Pimpinella anisum fruit oil, Mauritia
  • 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 comprising vegetable oils have skin barrier-related effects, can enhance skin barrier vitality and promote skin barrier-related factors FLG, LOR, IVL, TGM1, CASP14, HMGCR, AQP3 and ZO-1 expression.
  • the composition of the present invention comprises 0.1-100% by weight of vegetable oil. In a preferred embodiment, the composition of the invention comprises 0.1-50% by weight of vegetable oil. In a preferred embodiment, the composition of the invention comprises 0.1-20% by weight of vegetable oil. In a preferred embodiment, the composition of the invention comprises 0.5-10% by weight of vegetable oil.
  • compositions comprising microbial oils and vegetable oils
  • a composition comprising microbial oil and vegetable oil is provided, wherein the weight ratio of the microbial oil to the vegetable oil is 1:8 to 8:1. In a preferred embodiment, the weight ratio of the microbial oil to the vegetable oil is 1:1.
  • the composition of the present invention comprises 0.1-100% by weight of microbial oil and vegetable oil. In a preferred embodiment, the composition of the present invention comprises 0.1-50% by weight of microbial fats and vegetable fats. In a preferred embodiment, the composition of the invention comprises 0.1-20% by weight of microbial fats and vegetable fats. In a preferred embodiment, the composition of the present invention comprises 0.5-10% by weight of microbial fats and vegetable fats.
  • 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 oil (including microbial oil and vegetable 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 the oil in the composition (including microbial oil and vegetable oil) to the natural surfactant is 10:1 to 20:1.
  • composition containing microbial oil and vegetable oil can be applied to 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 Other components in the external preparation are physically and chemically compatible and do not affect the effect of the microbial oil and vegetable 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 their combinations.
  • 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).
  • Triolein trade name microalgae oil, purchased from LUBRIZOL ADVANCED MATERIALS, INC.
  • Hydrogenated lecithin trade name hydrogenated lecithin, purchased from NIKKO CHEMICALS CO.,LTD.
  • pH meter SEVENMULTI type from METTLER TOLEDO;
  • Homogenizer POLYTRON company PT 3100D type
  • Stand mixer IKA@EUROSTAR, power control-visc..
  • Embodiment 1 preparation composition
  • Embodiment 2 Preparation comprises the composition of vegetable oil
  • Embodiment 3 Preparation comprises the composition of microbial grease
  • Embodiment 4 Preparation comprises the composition of microbial oil and vegetable oil
  • Embodiment 5 preparation comprises the composition of microbial oil and vegetable oil
  • Embodiment 6 Preparation comprises the composition of microbial oil and vegetable oil
  • Embodiment 7 Preparation comprises the composition of microbial oil and vegetable oil
  • Embodiment 8 Preparation comprises the composition of microbial oil and vegetable oil
  • Embodiment 9 Preparation comprises the composition of microbial oil and vegetable oil
  • Test example 1 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).
  • the model was divided into sample groups of Examples 1-9 (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 sample group of the example and the positive control group (rosiglitazone) relative to the control group of Example 1.
  • 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.
  • Example 2 the sample of Example 1 (microalgae oil 0%+shea butter 0%) is used as a control, and its gene relative expression is 100%.
  • the gene expression of samples 8 and 9 and the positive control sample were compared to obtain the corresponding percentages.
  • the barrier factor FLG in the sample of Example 2 (shea butter 5%), the sample of Example 3 (microalgae oil 5%), the sample of Example 4 (microalgae oil 1%+shea butter 8% ), Example 5 sample (microalgae oil 3%+shea butter 6%), embodiment 6 sample (microalgae oil 4.5%+shea butter 4.5%), embodiment 7 sample (microalgae oil 6% + shea butter 3%), Example 8 sample (microalgae oil 7%+shea butter 2%), embodiment 9 sample (microalgae oil 8%+shea butter 1%) and positive control ( Rosiglitazone) after treatment, compared with Example 1 sample (microalgae oil 0%+shea butter 0%), respectively 222%, 340%, 381%, 439%, 767%, 457%, 381%, 340%, and 362%.
  • the barrier factor LOR in the sample of embodiment 2 (shea butter 5%), the sample of embodiment 3 (microalgae oil 5%), the sample of embodiment 4 (microalgae oil 1%+shea butter 8% ), Example 5 sample (microalgae oil 3%+shea butter 6%), embodiment 6 sample (microalgae oil 4.5%+shea butter 4.5%), embodiment 7 sample (microalgae oil 6% + shea butter 3%), Example 8 sample (microalgae oil 7%+shea butter 2%), embodiment 9 sample (microalgae oil 8%+shea butter 1%) and positive control ( Rosiglitazone) after treatment, compared with Example 1 sample (microalgae oil 0%+shea butter 0%), respectively 240%, 319%, 422%, 504%, 839%, 544%, 422%, 323%, and 351%.
  • Example 2 sample shea butter 5%
  • embodiment 3 sample microalgae oil 5%
  • embodiment 4 sample microalgae oil 1%+shea butter 8%
  • Example 5 sample microalgae oil 3%+shea butter 6%
  • embodiment 6 sample microalgae oil 4.5%+shea butter 4.5%
  • embodiment 7 sample microalgae oil 6% + shea butter 3%
  • Example 8 sample microalgae oil 7%+shea butter 2%
  • embodiment 9 sample microalgae oil 8%+shea butter 1%) and positive control ( Rosiglitazone) after treatment, compared with Example 1 sample (microalgae oil 0%+shea butter 0%), respectively 113%, 75%, 116%, 132%, 120%, 129%, 116%, 113%, and 103%.
  • the barrier factor TGM1 in the sample of embodiment 2 (shea butter 5%), the sample of embodiment 3 (microalgae oil 5%), the sample of embodiment 4 (microalgae oil 1%+shea butter 8% ), Example 5 sample (microalgae oil 3%+shea butter 6%), embodiment 6 sample (microalgae oil 4.5%+shea butter 4.5%), embodiment 7 sample (microalgae oil 6% + shea butter 3%), Example 8 sample (microalgae oil 7%+shea butter 2%), embodiment 9 sample (microalgae oil 8%+shea butter 1%) and positive control ( Rosiglitazone) after treatment, compared with Example 1 sample (microalgae oil 0%+shea butter 0%), respectively 134%, 134%, 178%, 211%, 246%, 195%, 178%, 149%, and 161%.
  • the barrier factor CASP14 in the sample of embodiment 2 (shea butter 5%), the sample of embodiment 3 (microalgae oil 5%), the sample of embodiment 4 (microalgae oil 1%+shea butter 8% ), Example 5 sample (microalgae oil 3%+shea butter 6%), embodiment 6 sample (microalgae oil 4.5%+shea butter 4.5%), embodiment 7 sample (microalgae oil 6% + shea butter 3%), Example 8 sample (microalgae oil 7%+shea butter 2%), embodiment 9 sample (microalgae oil 8%+shea butter 1%) and positive control ( Rosiglitazone) after treatment, compared with Example 1 sample (microalgae oil 0%+shea butter 0%), respectively 188%, 316%, 300%, 485%, 667%, 424%, 300%, 279%, and 330%.
  • the barrier factor HMGCR in the sample of embodiment 2 (shea butter 5%), the sample of embodiment 3 (microalgae oil 5%), the sample of embodiment 4 (microalgae oil 1%+shea butter 8% ), Example 5 sample (microalgae oil 3%+shea butter 6%), embodiment 6 sample (microalgae oil 4.5%+shea butter 4.5%), embodiment 7 sample (microalgae oil 6% + shea butter 3%), Example 8 sample (microalgae oil 7%+shea butter 2%), embodiment 9 sample (microalgae oil 8%+shea butter 1%) and positive control ( Rosiglitazone) after treatment, compared with Example 1 sample (microalgae oil 0%+shea butter 0%), respectively 170%, 281%, 291%, 326%, 450%, 342%, 291%, 284%, and 229%.
  • the barrier factor AQP3 in the sample of embodiment 2 (shea butter 5%), the sample of embodiment 3 (microalgae oil 5%), the sample of embodiment 4 (microalgae oil 1%+shea butter 8% ), Example 5 sample (microalgae oil 3%+shea butter 6%), embodiment 6 sample (microalgae oil 4.5%+shea butter 4.5%), embodiment 7 sample (microalgae oil 6% + shea butter 3%), Example 8 sample (microalgae oil 7%+shea butter 2%), embodiment 9 sample (microalgae oil 8%+shea butter 1%) and positive control ( Rosiglitazone) after treatment, compared with Example 1 sample (microalgae oil 0%+shea butter 0%), respectively 112%, 131%, 151%, 197%, 204%, 167%, 151%, 171%, and 131%.
  • the barrier factor ZO-1 in the sample of embodiment 2 (shea butter 5%), the sample of embodiment 3 (microalgae oil 5%), the sample of embodiment 4 (microalgae oil 1%+shea butter 8%), Example 5 sample (microalgae oil 3%+shea butter 6%), embodiment 6 sample (microalgae oil 4.5%+shea butter 4.5%), embodiment 7 sample (microalgae oil 6%+shea butter 3%), Example 8 sample (microalgae oil 7%+shea butter 2%), example 9 sample (microalgae oil 8%+shea butter 1%) and positive After the control (rosiglitazone) was treated, it was 143%, 214%, 314%, 318%, 402%, 303%, respectively, compared with the sample of Example 1 (microalgae oil 0%+shea butter 0%) %, 314%, 240%, and 246%.
  • Example 2 5% shea butter
  • Example 3 microalgae oil 5%
  • FLG, LOR, 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 repair.
  • Example 4 (microalgae oil 1%+shea butter 8%) 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 5 (microalgae oil 3%+shea butter 6%) 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 6 (microalgae oil 4.5%+shea butter 4.5%) 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 7 (microalgae oil 6%+shea butter 3%) 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 8 (microalgae oil 7%+shea butter 2%) 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 (microalgae oil 8%+shea butter 1%) 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.
  • compositions comprising microbial oils and vegetable oils of the present invention can be used as intermediate raw materials or functional additives for the preparation of medicines or external skin preparations, and the external skin preparations are preferably cosmetic compositions, including but not limited to creams, Preparation of lotion, gel, lotion, essence, mask, eye cream, aerosol (cleaning foam), spray, shower gel, massage oil, facial cleanser and other dosage forms.
  • cosmetic compositions including but not limited to creams, Preparation of lotion, gel, lotion, essence, mask, eye cream, aerosol (cleaning foam), spray, shower gel, massage oil, facial cleanser and other dosage forms.
  • the weight percent of the composition comprising microbial oil and vegetable oil in the skin external preparation of the present invention is 0.001%-100% (w/w); the preferred weight percent is 0.01%-60% (w/w); more The preferred weight percentage is 0.01%-40% (w/w).
  • compositions containing microbial oils and vegetable oils obtained in Examples 3-6 and 8 in external skin preparations are specific application examples of the compositions containing microbial oils and vegetable oils obtained in Examples 3-6 and 8 in external skin preparations, as well as the formulations and preparation methods of these dosage forms. Specific application examples are as follows:

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Abstract

The present invention provides an oil composition. The oil comprises a microbial oil and a vegetable oil. Calculating on the basis of the total weight of the composition, the composition comprises at least 0.5 wt% of the oils. The present invention further relates to a use of the oil composition in enhancing a skin barrier function and/or in preparing a drug and/or an external skin agent which enhances a skin barrier function.

Description

包含微生物油脂和植物油脂的组合物及其应用Composition comprising microbial oil and vegetable oil and application thereof 技术领域technical field
本发明属于化妆品领域,具体涉及含有微生物油脂和植物油脂的组合物及其在肌肤屏障功能方面的应用。The invention belongs to the field of cosmetics, and in particular relates to a composition containing microbial oil and vegetable oil and its application in skin barrier function.
背景技术Background technique
皮肤是人体面积最大的器官,覆盖于整个体表,起到了重要的屏障作用。从广义上来看,皮肤的屏障功能不仅仅指其物理性屏障作用,还应包括皮肤的色素屏障作用、神经屏障作用、免疫屏障作用以及其他与皮肤功能相关的诸多方面;狭义的皮肤屏障功能通常指表皮尤其是角质层的物理性或机械性屏障结构。拥有健康的皮肤屏障就等于拥有了美丽自然的皮肤。然而,由于环境、饮食和错误的皮肤护理等原因,皮肤屏障受损,使得皮肤自身防御能力不足,皮肤极易敏感受损。油脂用在化妆品中可使皮肤柔软、润滑和表面净化,在皮肤表面上起摩擦效果,同时形成憎水性薄膜起到保护作用,并能预防外来的有害物质侵袭,寒冷时亦可抑制皮肤表皮水分的蒸发,保护皮肤和头发,使头发光泽、柔软。The skin is the largest organ in the human body, covering the entire body surface and playing an important role as a barrier. In a broad sense, the skin barrier function not only refers to its physical barrier function, but also includes skin pigment barrier function, nerve barrier function, immune barrier function and many other aspects related to skin function; narrow skin barrier function usually Refers to the physical or mechanical barrier structure of the epidermis, especially the stratum corneum. Having a healthy skin barrier is tantamount to having beautiful, natural-looking skin. However, due to factors such as environment, diet and wrong skin care, the skin barrier is damaged, which makes the skin's own defense ability insufficient, and the skin is extremely sensitive and damaged. Used in cosmetics, oil can make the skin soft, lubricated and purify the surface. It has a friction effect on the skin surface, and at the same time forms a hydrophobic film to protect it and prevent the invasion of harmful substances from the outside. It can also inhibit the moisture of the skin epidermis when it is cold. Evaporation protects skin and hair, leaving hair shiny and soft.
微生物油脂是继植物油脂、动物油脂之后人类开发出的又一种食用油脂新资源。能够生产油脂的微生物有酵母、霉菌、细菌和藻类等,其中真核的酵母、霉菌和藻类能合成与植物油组成相似的甘油三酯,而原核的细菌则合成特殊的脂类。微藻中含有蛋白质、脂肪、碳水化合物和维生素等人类所必需的营养素,油脂含量较高,中性脂的含量约占细胞干重的20-50%,少数微藻可达75%,单位产油量显著高于农业油料作物。因此微藻油被认为是最具发展潜力的油脂资源,在国际上受到极大关注。大多数微藻中含有丰富的长链多不饱和脂肪酸,自然界中常见的不饱和脂肪酸主要分为3大类:ω-3系列,如二十碳五烯酸(EPA)和二十二碳六烯酸(DHA);ω-6亚油酸系列和ω-9油酸系列。多不饱和脂肪酸可调节血脂、增强机体免疫、补脑健脑和改善关节炎症状缓解疼痛 等。例如,文献江木兰,油脂微藻的研究进展,中国油料作物学报[J],2010,32(4):571-576指出,ω-3系列脂肪酸对脑和视网膜、皮肤和肾功能的健全来说非常重要,DHA被人们称为脑白金,对于神经系统有重要的功能,具有健脑、提高记忆力和视力的功能,尤其可以促进胎儿脑细胞发育和婴幼儿脑细胞生长,促进青少年提高记忆,防治老年性痴呆。例如文献刘冀红,ω-3多不饱和脂肪酸在肿瘤防治中的意义,肠外与肠内营养[J],2004,11(1):54-56指出,多不饱和脂肪酸具有较好的抗癌作用,绝经后的乳癌病人,摄入的EPA和DHA在膳食中的比例及乳腺脂肪组织中DHA占磷脂的比例,明显低于乳腺良性疾病病人,所以摄入ω-3脂肪酸可以预防乳癌的发生。Microbial oil is another new edible oil resource developed by humans after vegetable oil and animal oil. Microorganisms capable of producing oil include yeast, mold, bacteria, and algae. Among them, eukaryotic yeast, mold, and algae can synthesize triglycerides similar to vegetable oil, while prokaryotic bacteria can synthesize special lipids. Microalgae contains essential nutrients such as protein, fat, carbohydrates and vitamins, etc., and the content of oil is relatively high. The content of neutral fat accounts for about 20-50% of the dry weight of cells, and a few microalgae can reach 75%. The amount of oil is significantly higher than that of agricultural oil crops. Therefore, microalgae oil is considered to be the oil resource with the most development potential, and has received great attention internationally. Most microalgae are rich in long-chain polyunsaturated fatty acids. The common unsaturated fatty acids in nature are mainly divided into three categories: omega-3 series, such as eicosapentaenoic acid (EPA) and docosahexaenoic acid Dienoic acid (DHA); omega-6 linoleic acid series and omega-9 oleic acid series. Polyunsaturated fatty acids can regulate blood lipids, enhance the body's immunity, nourish the brain and improve the symptoms of arthritis and relieve pain. For example, the literature Jiang Mulan, the research progress of oily microalgae, Chinese Journal of Oil Crops [J], 2010, 32 (4): 571-576 pointed out that omega-3 series fatty acids are beneficial to the health of brain and retina, skin and kidney function. It is very important. DHA is called melatonin. It has important functions for the nervous system. It has the functions of strengthening the brain, improving memory and vision. It can especially promote the development of fetal brain cells and the growth of infant brain cells, and promote the improvement of memory in teenagers. Prevention and treatment of senile dementia. For example, the literature Liu Jihong, Significance of ω-3 polyunsaturated fatty acids in tumor prevention and treatment, parenteral and enteral nutrition [J], 2004, 11 (1): 54-56 pointed out that polyunsaturated fatty acids have better anticancer The role of postmenopausal breast cancer patients, the intake of EPA and DHA in the diet and the ratio of DHA to phospholipids in mammary adipose tissue are significantly lower than those of benign breast disease patients, so intake of omega-3 fatty acids can prevent the occurrence of breast cancer .
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。植物油脂是由高级脂肪酸和甘油反应而成的天然化合物,广泛分布于自然界中。凡是从植物种子、果肉及其它部分提取所得的脂肪统称植物油脂。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。常见的植物油有牛油果树(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、霍霍巴(Simmondsia chinensis)籽油、红花(Carthamus tinctorius)籽油、白池花(Limnanthes alba)籽油和向日葵(Helianthus annuus)籽油等。植物油脂由于质感亲肤,接近人类皮脂膜结构,比水更容易被皮肤吸收,渗透性也更好,因此能深层渗入并滋养皮肤。According to the source and chemical composition of oils, 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 oil is a natural compound formed by the reaction of higher fatty acids and glycerol, which is widely distributed in nature. All fats extracted from plant seeds, pulp and other parts are collectively referred to as vegetable oils. 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. Common vegetable oils include avocado (Butyrospermum parkii) fruit fat (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, jojoba (Simmondsia chinensis) seed oil, safflower (Carthamus tinctorius) seed oil, white pond flower (Limnanthes alba) seed oil, sunflower (Helianthus annuus) seed oil, etc. Vegetable oil has a skin-friendly texture and is close to the human sebum membrane structure. It is easier to be absorbed by the skin than water and has better permeability, so it can penetrate deeply and nourish the skin.
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)。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. In the process of skin barrier formation, more than 200 genes are highly related to skin barrier. For example, the barrier factors filaggrin (FLG), loricrin (LOR), endothelin (IVL), transglutaminase 1 (TGM1), and barrier moisturizing factor caspase 14 are related to the formation of the corneous envelope. (CASP14), HMGCoA reductase (HMGCR), aquaporin 3 (AQP3) and keratinocyte intercellular junction-associated factor zona occlusin 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。Specifically, 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) is the main component of the corneous envelope and plays an important role in the barrier function of the epidermis. 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. The characteristic resistance and insolubility of the cornified envelope is based on the formation of very stable isopeptide bonds catalyzed by transglutaminase 1 (TGM1).
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将内源性的甘油运输进入表皮,使其直接或间接影响皮肤保湿功效。HMGCoA reductase (HMGCR) 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. In addition, AQP3 is responsible for the important role of glycerol transport in the stratum corneum. AQP3 transports endogenous glycerol into the epidermis, making it directly or indirectly affect the moisturizing effect of the skin.
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。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.
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。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.
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。Among them: 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 walnut seed oil, cottonseed oil, tea seed oil, millet seed oil, papaya seed oil, raspberry seed oil, baobab seed oil, calendula seed oil, oleifera Seed Oil, Moringa Seed Oil, Pecan Seed Oil, Perilla Seed Oil, Babassu Seed Oil, and White Lupine Seed Oil, etc.) and Germ (Examples: Rice Germ Oil, Wheat Germ Oil, Oat Germ Oil, and Corn Germ Oil Oil, etc.), and some are derived from other parts of plants such as leaves, bark, roots, petals and stamens.
本发明意外地发现,微生物油脂(例如微藻油等)和植物油脂(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,这种包含微生物油脂和植物油脂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。The present invention unexpectedly finds that microbial oils (such as microalgae oil, etc.) and vegetable oils (such as jojoba oil, safflower seed oil, sunflower seed oil, etc.) have skin barrier-related effects, which can enhance the vitality of the skin barrier and promote skin barrier function. Expression of related factors FLG, LOR, IVL, TGM1, CASP14, HMGCR, AQP3 and ZO-1. Therefore, the composition comprising microbial oil and vegetable oil can be used as an efficacy additive in medicines and external skin preparations.
发明内容Contents of the invention
一方面,本发明提供了一种油脂组合物,所述油脂包括微生物油脂和植物油脂,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%的油脂。在优选的实施方式中,本发明油脂组合物中微生物油脂与植物油脂的重量比为1:8至8:1。In one aspect, the present invention provides an oil composition, the oil includes microbial oil and vegetable oil, wherein, based on the total weight of the composition, the composition comprises at least 0.5% by weight of oil. In a preferred embodiment, the weight ratio of microbial oil to vegetable oil in the oil composition of the present invention is 1:8 to 8:1.
在优选的实施方式中,本发明油脂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。In a preferred embodiment, the oil composition of the present invention also includes a natural surfactant selected from the group consisting of: lecithin, cholesterol, lanolin, tea saponin, protein, saponins, sugars, alkanes base polyglycosides or their combinations. In a preferred embodiment, the natural surfactant is hydrogenated lecithin.
在优选的实施方式中,本发明油脂组合物中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,本发明油脂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。In a preferred embodiment, the weight ratio of oil and natural surfactant in the oil composition of the present invention is 1:1 to 20:1. In a more preferred embodiment, the weight ratio of vegetable oil to natural surfactant in the oil composition of the present invention is 10:1 to 20:1.
在优选的实施方式中,本发明油脂组合物中的植物油脂为植物种子油脂、植物果实油脂或它们的组合。例如,所述植物种子油脂选自: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、白羽扇豆籽油或它们的组合。例如,所述植物果实油脂选自: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。In a preferred embodiment, the vegetable oil in the oil composition of the present invention is vegetable seed oil, vegetable fruit oil or a combination thereof. For example, the vegetable seed oil is selected from: jojoba seed oil, safflower seed oil, white pond flower seed oil, sunflower seed oil, macadamia nut seed oil, castor oil, peony seed oil, grape seed oil, grapefruit seed oil 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 Hard Walnut Seed Oil, Cottonseed Oil, Tea Seed Oil, Guava Seed Oil, Papaya Seed Oil, Raspberry Seed Oil, Baobab Seed Oil, Calendula Seed Oil, Oleifera Seed Oil, Moringa Seed Oil, American Pecan Seed Oil, Perilla Seed Oil, Babassu seed oil, white lupine seed oil, or a combination thereof. For example, the plant fruit oil is selected from: shea butter, olive 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, dog tooth rosehip oil, pepper fruit oil, Brazilian nectarine fruit oil, flat-leaf pimento fruit oil, anise fruit oil, mulberry fruit oil, juniper fruit oil, pheasant fruit oil, Satsuma fruit oil, star palm fruit oil, rosehip oil, coriander fruit oil or a combination thereof.
在优选的实施方式中,本发明油脂组合物中的微生物油脂选自:微藻油、雨生红球藻油、长耳齿状藻油或它们的组合。In a preferred embodiment, the microbial oil in the oil composition of the present invention is selected from: oil of microalgae, oil of Haematococcus pluvialis, oil of Dentate algae or combinations thereof.
另一方面,本发明还涉及所述油脂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。On the other hand, the present invention also relates to the application of the oil composition in enhancing skin barrier function. In a preferred embodiment, 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.
另一方面,本发明还涉及油脂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。On the other hand, the present invention also relates to the application of the oil composition in the preparation of medicines and/or skin external preparations for enhancing skin barrier function. In a preferred embodiment, the pharmaceutical and/or external skin preparation contains 0.001-100% by weight of the composition.
具体实施方式Detailed ways
本发明涉及包含微生物油脂和植物油脂的组合物及其应用,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 微生物油脂和植物油脂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。The present invention relates to a composition comprising microbial oil and vegetable 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, AQP3 and Effect of ZO-1 Expression. Therefore, the composition comprising microbial oil and vegetable oil can be used as an efficacy additive for the preparation of medicines and/or skin external preparations for enhancing the skin barrier function.
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。In order to provide a more concise description, some quantitative expressions given herein are not modified by the term "about". It is to be understood that, whether or not the term "about" is explicitly used, each quantity given herein is intended to refer to the actual given value, and also to refer to what one of ordinary skill in the art could reasonably infer. Approximations to these given values include approximations to these given values that result from experimental and/or measurement conditions.
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。In order to provide a more concise description, some quantitative expressions are described herein as ranging from about X amount to about Y amount. It should be understood that when a range is recited, that range is not limited to the upper and lower limits recited, but includes the entire range from about X amount to about Y amount or any amount therebetween.
微生物油脂microbial oil
本发明的组合物包含微生物油脂选自:微藻油、雨生红球藻(HAEMATOCOCCUS PLUVIALIS)油、长耳齿状藻(ODONTELLA AURITA)油。微藻油是保健品、医药和化妆品的添加剂,也可以作为食用油的可再生能源。食品方面,微藻油可以作为功能性营养强化剂或直接做成保健产品,微藻油中不仅含有DHA、EPA等不饱和脂肪酸,而且还含有对人体健康有益的烃类和微量的醇类成分。医药方面,微藻油中的功能性多不饱和脂肪酸可以作为药物使用,目前微藻油中的亚油酸和花生四烯酸在医学领域应用相当广泛,对治疗高血压、缓解支气管哮喘、鼻充血以及消化系统溃疡等疾病疗效十分显著。在养殖业中,微藻油可以加入饲料中,从而得到我们想要的功能性农副产品。The composition of the present invention comprises microbial oil selected from: microalgae oil, Haematococcus Pluvialis (HAEMATOCOCCUS PLUVIALIS) oil, long ear algae (ODONTELLA AURITA) oil. Microalgae oil is an additive in health products, medicine and cosmetics, and can also be used as a renewable energy source for edible oil. In terms of food, microalgae oil can be used as a functional nutritional enhancer or directly made into health care products. Microalgae oil not only contains unsaturated fatty acids such as DHA and EPA, but also contains hydrocarbons and trace alcohols that are beneficial to human health . In terms of medicine, functional polyunsaturated fatty acids in microalgae oil can be used as medicine. At present, linoleic acid and arachidonic acid in microalgae oil are widely used in the medical field. Congestion and digestive system ulcers and other diseases are very effective. In the farming industry, microalgae oil can be added to the feed to obtain the functional agricultural and sideline products we want.
本发明中的微藻油为三油酸甘油酯,富含超过90%的有益人体的ω-9不饱和脂肪酸,即油酸。油酸是一种饮食中常见的单元不饱和脂肪酸,不是必须脂肪酸,但它仍对一般健康状况有益。ω-9存在于橄榄、杏仁、昆士兰果、榛实、芝麻、鳄梨、亚麻仁及其油内。地中海国家橄榄油的消费高与他们乳癌和心脏病发病率较低有关。加州大学的研究指出,单元不饱和脂肪酸含量高的饮食能预防低密度脂蛋白的胆固醇的氧化,并能保护血管壁,这类脂肪也可促进高密度胆固醇控制低密度胆固醇的功能,同时单元不饱和脂肪使抗氧化的维生素E更有效的保护细胞免遭自由基破坏。The microalgae oil in the present invention is glyceryl trioleate, which is rich in more than 90% of omega-9 unsaturated fatty acid beneficial to human body, ie oleic acid. Oleic acid is a monounsaturated fatty acid commonly found in the diet and is not an essential fatty acid, but it still has benefits for general health. Omega-9s are found in olives, almonds, queensland nuts, hazelnuts, sesame, avocado, flaxseed and their oils. High consumption of olive oil in Mediterranean countries has been linked to lower rates of breast cancer and heart disease. Research from the University of California pointed out that a diet high in monounsaturated fatty acids can prevent the oxidation of low-density lipoprotein cholesterol and protect blood vessel walls. This type of fat can also promote the function of high-density cholesterol to control low-density cholesterol. Saturated fat makes the antioxidant vitamin E more effective in protecting cells from free radical damage.
本发明意外地发现,包含微生物油脂(例如,微藻油)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。The present invention surprisingly found that compositions comprising microbial oils (e.g., microalgae oil) have skin barrier-related effects, can enhance skin barrier vitality and promote skin barrier-related factors FLG, LOR, IVL, TGM1, CASP14, HMGCR, AQP3 and Expression of ZO-1.
在一些实施方式中,本发明的组合物包含0.1-100重量%的微生物油脂。在优选的实施方式中,本发明的组合物包含0.1-50重量%的微生物油脂。在优选的实施方式中,本发明的组合物包含0.1-20重量%的微生物油脂。在优选的实施方式中,本发明的组合物包含0.5-10重量%的微生物油脂。In some embodiments, the composition of the present invention comprises 0.1-100% by weight of microbial oil. In a preferred embodiment, the composition of the present invention comprises 0.1-50% by weight of microbial oil. In a preferred embodiment, the composition of the present invention comprises 0.1-20% by weight of microbial oil. In a preferred embodiment, the composition of the present invention comprises 0.5-10% by weight of microbial oil.
植物油脂vegetable oil
植物油在食品、工业、化妆品和医药等方面应用广泛,在化妆品中应用最广泛的植物油为乳木果油,乳木果油的功效、功能非常多,比如极好的滋养保湿功能,这是因为乳木果油中含有丰富的不可皂化物质,蕴含大量的脂肪及脂肪酸等,具有强效的滋润补水功能。另外,优质的乳木果油具有很好防紫外线,是因为它内含极好的天然防晒成份-肉桂酸,它能吸收阳光中的紫外线,保护皮肤免受日晒侵害;而且,优质的乳木果油还具有非常有效的抗炎抗敏功能,所以适用于较为薄弱敏感的部位如眼睛及唇部,而且其植固醇成份,对于受伤的皮肤具有很好的消炎和修复作用。Vegetable oil is widely used in food, industry, cosmetics and medicine. The most widely used vegetable oil in cosmetics is shea butter. Shea butter has many effects and functions, such as excellent nourishing and moisturizing functions. This is because Shea butter is rich in unsaponifiable substances, contains a lot of fat and fatty acids, etc., and has a strong moisturizing function. In addition, high-quality shea butter has good UV protection because it contains an excellent natural sunscreen ingredient-cinnamic acid, which can absorb ultraviolet rays in the sun and protect the skin from sun damage; moreover, high-quality milk Argan oil also has very effective anti-inflammatory and anti-allergic functions, so it is suitable for relatively weak and sensitive parts such as eyes and lips, and its phytosterol component has a good anti-inflammatory and repairing effect on injured skin.
本发明组合物可以包含各种来源的植物油脂。例如,本发明组合物包含植物果油。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。The compositions of the present invention may comprise vegetable fats and oils from various sources. For example, compositions of the invention comprise vegetable fruit oils. Vegetable fruit oil, also known as plant fruit oil, mainly comes from plant fruits, seeds and germs, and some come from other parts of plants such as leaves, bark, roots, petals and stamens. 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 (Piper nigrum) Fruit Oil, Brazilian Nectarine (Caryocar brasiliense) Fruit Oil, Flat Leaf Pansy ( Vanilla planifolia) fruit oil, Pimpinella anisum fruit oil, Mauritia flexuosa fruit oil, Juniperus communis fruit oil, Litsea cubeba fruit oil, Citrus unshiu fruit oil Oil, Astrocaryum vulgare, Rosa multiflora, Coriandrum sativum, etc.
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。For example, 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.
本发明意外地发现,包含植物油脂(例如,乳木果油)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。The present invention unexpectedly finds that compositions comprising vegetable oils (for example, shea butter) have skin barrier-related effects, can enhance skin barrier vitality and promote skin barrier-related factors FLG, LOR, IVL, TGM1, CASP14, HMGCR, AQP3 and ZO-1 expression.
在一些实施方式中,本发明的组合物包含0.1-100重量%的植物油脂。在优选的实施方式中,本发明的组合物包含0.1-50重量%的植物油脂。在优选的实施方式中,本发明的组合物包含0.1-20重量%的植物油脂。在优选的实施方式中,本发明的组合物包含0.5-10重量%的植物油脂。In some embodiments, the composition of the present invention comprises 0.1-100% by weight of vegetable oil. In a preferred embodiment, the composition of the invention comprises 0.1-50% by weight of vegetable oil. In a preferred embodiment, the composition of the invention comprises 0.1-20% by weight of vegetable oil. In a preferred embodiment, the composition of the invention comprises 0.5-10% by weight of vegetable oil.
包含微生物油脂和植物油脂的组合物Compositions comprising microbial oils and vegetable oils
在本发明的一些实施方式中,提供了一种包含微生物油脂和植物油脂的组合物,其中,所述微生物油脂与所述植物油脂的重量比为1:8至8:1。在优选的实施方式中,所述微生物油脂与所述植物油脂的重量比为1:1。In some embodiments of the present invention, a composition comprising microbial oil and vegetable oil is provided, wherein the weight ratio of the microbial oil to the vegetable oil is 1:8 to 8:1. In a preferred embodiment, the weight ratio of the microbial oil to the vegetable oil is 1:1.
在一些实施方式中,本发明的组合物包含0.1-100重量%的微生物油脂和植物油脂。在优选的实施方式中,本发明的组合物包含0.1-50重量%的微生物油脂和植物油脂。在优选的实施方式中,本发明的组合物包含0.1-20重量%的 微生物油脂和植物油脂。在优选的实施方式中,本发明的组合物包含0.5-10重量%的微生物油脂和植物油脂。In some embodiments, the composition of the present invention comprises 0.1-100% by weight of microbial oil and vegetable oil. In a preferred embodiment, the composition of the present invention comprises 0.1-50% by weight of microbial fats and vegetable fats. In a preferred embodiment, the composition of the invention comprises 0.1-20% by weight of microbial fats and vegetable fats. In a preferred embodiment, the composition of the present invention comprises 0.5-10% by weight of microbial fats and vegetable fats.
天然表面活性剂natural surfactant
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。The 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.
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。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.
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。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.
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。In some embodiments, the 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.
在优选的实施方式中,本发明的组合物中的油脂(包括微生物油脂和植物油脂)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,组合物中的油脂(包括微生物油脂和植物油脂)与天然表面活性剂的重量比为10:1至20:1。In a preferred embodiment, the weight ratio of oil (including microbial oil and vegetable 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 the oil in the composition (including microbial oil and vegetable oil) to the natural surfactant is 10:1 to 20:1.
药品和/或皮肤外用剂Medicines and/or skin topical agents
包含微生物油脂和植物油脂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。The composition containing microbial oil and vegetable oil can be applied to pharmaceuticals and/or skin external preparations for enhancing skin barrier function.
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。In some embodiments, 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.
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。In some embodiments, the external skin preparation is selected from: cleanser, lotion, lotion, cream, gel, mask. Add different dosages according to different types of preparations.
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。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.
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。External preparations for skin contain a dermatologically acceptable carrier or vehicle (eg, lotion, cream, ointment, cleanser, etc.). Those of ordinary skill in the art can select a carrier capable of dissolving or dispersing these components at the above-mentioned concentrations according to common knowledge in the art.
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。Those of ordinary skill in the art can select suitable carriers based on common knowledge and their ability to dissolve or disperse in the active ingredient at the concentration most suitable for processing the active ingredient. Said carrier includes, for example, water, alcohols, oils, etc. wait.
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。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. Preferably, the carrier is a gel or moisturizing lotion, or an applicator in dry or wet form.
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。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.
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、且不影响本发明的微生物油脂和植物油脂的效果即可。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 Other components in the external preparation are physically and chemically compatible and do not affect the effect of the microbial oil and vegetable oil of the present invention.
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%。In some embodiments of the external preparation for skin 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.
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。In one example of the external preparation for skin of the present invention, 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. The antioxidant 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.
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。In one example of the skin external preparation of the present invention, 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. Examples of suitable 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.
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%。In one example of the external preparation for skin of the present invention, 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. When used, 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.
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。In one example of the external preparation for skin of the present invention, one or more emulsifiers may be used. Emulsifiers can be used in effective stabilizing amounts. Preferably, 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 their combinations.
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%。In one example of the external preparation for skin of the present invention, one or more pH adjusting agents can be used. Beneficial pH regulators in the external preparation for skin of the present invention include tromethamine. When used, 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.
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。In a specific embodiment of the present invention, 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.
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)。In some embodiments of the present invention, 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).
实施例Example
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。Below in conjunction with specific embodiment, to further illustrate the present invention. It is necessary to point out here that embodiment is only used to further illustrate the present invention, can not be interpreted as the limitation of protection scope of the present invention, those skilled in the art can make some non-essential improvements according to the content of the present invention above and adjust. The test methods for which specific conditions are not indicated in the following examples are generally in accordance with conventional conditions, or in accordance with the conditions suggested by the manufacturer. All percentages and parts are by weight unless otherwise indicated.
以下实施例中采用的实验材料包括:Experimental materials adopted in the following examples include:
三油精,商品名微藻油,购自LUBRIZOL ADVANCED MATERIALS,INC.Triolein, trade name microalgae oil, purchased from LUBRIZOL ADVANCED MATERIALS, INC.
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;Avocado tree (Butyrospermum parkii) fruit fat, trade name refined shea butter, purchased from BASF Advanced Materials Co., Ltd.;
氢化卵磷脂,商品名氢化卵磷脂,购自NIKKO CHEMICALS CO.,LTD.。Hydrogenated lecithin, trade name hydrogenated lecithin, purchased from NIKKO CHEMICALS CO.,LTD.
实施例中采用的实验仪器包括:The experimental equipment adopted in the embodiment includes:
称量天平:METTLER TOLEDO公司PB4002-N型;Weighing balance: METTLER TOLEDO company PB4002-N type;
pH计:METTLER TOLEDO公司SEVENMULTI型;pH meter: SEVENMULTI type from METTLER TOLEDO;
水浴锅:上海一恒科技有限公司HWS28型电热恒温水浴锅;Water bath: Shanghai Yiheng Technology Co., Ltd. HWS28 electric constant temperature water bath;
均质机:POLYTRON公司PT 3100D型;Homogenizer: POLYTRON company PT 3100D type;
台式搅拌机:IKA@EUROSTAR,power control-visc.。Stand mixer: IKA@EUROSTAR, power control-visc..
实施例1:制备组合物Embodiment 1: preparation composition
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。Weigh 0.5 parts by mass of hydrogenated lecithin into a beaker, add 99.5 parts by mass of deionized water, stir evenly, and set aside.
实施例2:制备包含植物油脂的组合物Embodiment 2: Preparation comprises the composition of vegetable oil
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。Weigh 0.5 parts by mass of hydrogenated lecithin and 5 parts by mass of shea butter in a beaker, heat to 75-80°C while stirring, then weigh 94.5 parts by mass of deionized water at 75-80°C in the beaker, and turn on Homogenizing, the speed is 3000 rpm, homogenizing for 5-10 minutes, and set aside.
实施例3:制备包含微生物油脂的组合物Embodiment 3: Preparation comprises the composition of microbial grease
称取0.5质量份氢化卵磷脂和5质量份微藻油于烧杯中,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。Weigh 0.5 parts by mass of hydrogenated lecithin and 5 parts by mass of microalgae oil in a beaker, heat to 75-80°C while stirring, then weigh 94.5 parts by mass of deionized water at 75-80°C in the beaker, turn on the homogenizer Homogenize at a speed of 3000 rpm, homogenize for 5-10 minutes, and set aside.
实施例4:制备包含微生物油脂和植物油脂的组合物Embodiment 4: Preparation comprises the composition of microbial oil and vegetable oil
称取0.5质量份氢化卵磷脂、1质量份微藻油和8质量份乳木果油于烧杯中,边搅拌边加热至75-80℃,后再称取90.5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。Weigh 0.5 parts by mass of hydrogenated lecithin, 1 part by mass of microalgae oil and 8 parts by mass of shea butter in a beaker, heat to 75-80°C while stirring, and then weigh 90.5 parts by mass of 75-80°C detoxified Put the ionized water in the beaker, turn on the homogenizer, the speed is 3000 rpm, homogenize for 5-10 minutes, and set aside.
实施例5:制备包含微生物油脂和植物油脂的组合物Embodiment 5: preparation comprises the composition of microbial oil and vegetable oil
称取0.5质量份氢化卵磷脂、3质量份微藻油和6质量份乳木果油于烧杯中,边搅拌边加热至75-80℃,后再称取90.5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。Weigh 0.5 parts by mass of hydrogenated lecithin, 3 parts by mass of microalgae oil and 6 parts by mass of shea butter in a beaker, heat to 75-80°C while stirring, and then weigh 90.5 parts by mass of 75-80°C detoxified Put the ionized water in the beaker, turn on the homogenizer, the speed is 3000 rpm, homogenize for 5-10 minutes, and set aside.
实施例6:制备包含微生物油脂和植物油脂的组合物Embodiment 6: Preparation comprises the composition of microbial oil and vegetable oil
称取0.5质量份氢化卵磷脂、4.5质量份微藻油和4.5质量份乳木果油于烧杯中,边搅拌边加热至75-80℃,后再称取90.5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。Weigh 0.5 parts by mass of hydrogenated lecithin, 4.5 parts by mass of microalgae oil and 4.5 parts by mass of shea butter in a beaker, heat to 75-80°C while stirring, and then weigh 90.5 parts by mass of 75-80°C detoxified Put the ionized water in the beaker, turn on the homogenizer, the speed is 3000 rpm, homogenize for 5-10 minutes, and set aside.
实施例7:制备包含微生物油脂和植物油脂的组合物Embodiment 7: Preparation comprises the composition of microbial oil and vegetable oil
称取0.5质量份氢化卵磷脂、6质量份微藻油和3质量份乳木果油于烧杯中,边搅拌边加热至75-80℃,后再称取90.5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。Weigh 0.5 parts by mass of hydrogenated lecithin, 6 parts by mass of microalgae oil and 3 parts by mass of shea butter in a beaker, heat to 75-80°C while stirring, and then weigh 90.5 parts by mass of 75-80°C detoxified Put the ionized water in the beaker, turn on the homogenizer, the speed is 3000 rpm, homogenize for 5-10 minutes, and set aside.
实施例8:制备包含微生物油脂和植物油脂的组合物Embodiment 8: Preparation comprises the composition of microbial oil and vegetable oil
称取0.5质量份氢化卵磷脂、7质量份微藻油和2质量份乳木果油于烧杯中,边搅拌边加热至75-80℃,后再称取90.5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。Weigh 0.5 parts by mass of hydrogenated lecithin, 7 parts by mass of microalgae oil and 2 parts by mass of shea butter in a beaker, heat to 75-80°C while stirring, and then weigh 90.5 parts by mass of 75-80°C detoxified Put the ionized water in the beaker, turn on the homogenizer, the speed is 3000 rpm, homogenize for 5-10 minutes, and set aside.
实施例9:制备包含微生物油脂和植物油脂的组合物Embodiment 9: Preparation comprises the composition of microbial oil and vegetable oil
称取0.5质量份氢化卵磷脂、8质量份微藻油和1质量份乳木果油于烧杯中,边搅拌边加热至75-80℃,后再称取90.5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。Weigh 0.5 parts by mass of hydrogenated lecithin, 8 parts by mass of microalgae oil and 1 part by mass of shea butter in a beaker, heat to 75-80°C while stirring, and then weigh 90.5 parts by mass of 75-80°C detoxified Put the ionized water in the beaker, turn on the homogenizer, the speed is 3000 rpm, homogenize for 5-10 minutes, and set aside.
测试例1:3D重组皮肤表皮模型屏障相关基因表达测试Test example 1: 3D recombinant skin epidermis model barrier-related gene expression test
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。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.
1.试验材料1. Test material
1.1细胞:皮肤模型为3D表皮皮肤模型
Figure PCTCN2022125279-appb-000001
(EpiSkin)。
1.1 Cell: skin model is 3D epidermal skin model
Figure PCTCN2022125279-appb-000001
(EpiSkin).
1.2试剂:1.2 Reagents:
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 PCTCN2022125279-appb-000002
Green Supermix(Bio-rad)。
3D skin model maintenance medium (EpiSkin); DPBS containing calcium and magnesium (Gibco); isopropanol, 75% absolute ethanol (Sinopharm Group); DEPC water (Tiangen Biology); total RNA extraction reagent TRIzol (ThermoFisher); Reverse transcription kit iScript cDNA Synthesis Kit, fluorescence real-time quantitative PCR reagent iTaq TM Universal
Figure PCTCN2022125279-appb-000002
Green Supermix (Bio-rad).
1.3主要设备1.3 Main equipment
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)。 CO 2 incubator HERAcell 240i, biological safety cabinet 1300SERIES A2, ultra-micro ultraviolet spectrophotometer NanoDrop ONE (Thermo); gene amplification instrument C1000Touch, real-time quantitative PCR instrument CFX Connect (Bio-rad); high-speed refrigerated centrifuge MIKRO 220R ( Hittich); positive pipette M25 (Gilson); 50 mL continuous pipette tip Multipette plus (Eppendorf); skin punch (area 0.38 cm 2 ).
2.实验方法:2. Experimental method:
3D重组表皮模型接收及复苏3D reconstructed epidermis model reception and recovery
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。Receive the 3D epidermal remodeling model, check the integrity of the package, check the number of models, check the maintenance medium, and detect the color and volume of the medium. After confirming that it is correct, start model recovery.
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。 Perform resuscitation operations in a biological safety cabinet. Take a certain number of 12-well plates, add 2 ml/well of maintenance medium to the first row, then take out the 3D recombinant epidermal model with tweezers, carefully remove the surface gel with a cotton swab, and put it into the well containing maintenance medium , recovery for 24 hours. One 12-well plate can recover 4 3D reconstructed epidermal models. Culture conditions: 5% CO 2 , cultured in a constant temperature incubator at 37°C.
3D重组表皮模型样品处理3D Reconstructed Epidermis Model Sample Processing
将模型分为实施例1-9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)。The model was divided into sample groups of Examples 1-9 (3 repetitions for each sample) and a positive control group (rosiglitazone, 3 repetitions).
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。First add 2 ml/well of maintenance medium to the second row of the 12-well plate, and then use tweezers to transfer the 3D recombinant epidermal model located in the first row to the corresponding second row.
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。 Use a piston displacement pipette (M25) to add 15 microliters of rosiglitazone solution (100 micromoles, dissolved in 1×DPBS) to the positive control group, add 15 microliters of samples to the sample group, and Gently spread the sample evenly on the surface of the skin model, and each sample was repeated three times. All models were placed in a cell culture incubator and cultured for 24 hours. Culture conditions: 5% CO 2 , cultured in a constant temperature incubator at 37°C.
3D重组表皮模型收集总RNA样品3D Reconstituted Epidermis Model to Collect Total RNA Samples
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。 Use a 50ml continuous pipette to absorb 1×DPBS, rinse off the sample on the surface of the model (do not flush directly at the sample, but aim at the side wall of the skin model support frame), and then use a cotton swab to absorb the residual liquid. Cut the epidermal tissue with a hole punch, and separate the epidermal tissue from the underlying collagen base with two small elbow tweezers, put the epidermal tissue into an EP tube containing 1 ml of total RNA extraction reagent (TRIzol), and use Pipette the epidermal tissue repeatedly with a 1 ml RNase-free pipette until only the transparent stratum corneum remains. Subsequently, 0.2 ml of chloroform was added to the original EP tube, shaken vigorously, and centrifuged at low temperature and high speed for 15 minutes. Use an RNase-free pipette nozzle to take 500 microliters of the upper aqueous phase, then add an equal volume of pre-cooled (minus 20 degrees) isopropanol, mix by inversion, and centrifuge at low temperature and high speed for 10 minutes. After centrifugation, the RNA forms a white pellet at the bottom of the EP tube. Rinse twice with 75% ethanol, remove residual ethanol with a centrifuge and a suction nozzle, and open the lid to dry at room temperature until it becomes transparent. Dissolve with 40 µl RNase-free H 2 O and mix well. The 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.
RT-qPCR法定量检测皮肤屏障相关基因Quantitative detection of skin barrier-related genes by RT-qPCR
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。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.
反转录体系如下:The reverse transcription system is as follows:
Figure PCTCN2022125279-appb-000003
Figure PCTCN2022125279-appb-000003
反转录程序如下:25℃,5分钟;42℃,30分钟;85℃,5分钟。The reverse transcription program was as follows: 25°C, 5 minutes; 42°C, 30 minutes; 85°C, 5 minutes.
用荧光实时定量聚合酶链式反应(PCR)试剂iTaq TM Universal
Figure PCTCN2022125279-appb-000004
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。
Fluorescent real-time quantitative polymerase chain reaction (PCR) reagent iTaq TM Universal
Figure PCTCN2022125279-appb-000004
Green Supermix performs fluorescence real-time quantitative detection to analyze the expression of barrier-related gene messenger RNA (mRNA).
反应体系如下:The reaction system is as follows:
Figure PCTCN2022125279-appb-000005
Figure PCTCN2022125279-appb-000005
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)。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).
本实施例所用引物序列设计如下:The primer sequences used in this example are designed as follows:
Figure PCTCN2022125279-appb-000006
Figure PCTCN2022125279-appb-000006
Figure PCTCN2022125279-appb-000007
Figure PCTCN2022125279-appb-000007
采用2 -ΔΔCt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。 The 2 -ΔΔCt method was used to analyze the gene expression changes of the sample group of the example and the positive control group (rosiglitazone) relative to the control group of Example 1.
3.结果判断3. Result judgment
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。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.
表2:各组样品处理后的皮肤屏障因子表达情况Table 2: Expression of skin barrier factors in each group of samples after treatment
Figure PCTCN2022125279-appb-000008
Figure PCTCN2022125279-appb-000008
如表2所示,实施例1样品(微藻油0%+乳木果油0%)作为对照,其基因相对表达量为100%,实施例2、3、4、5、6、7、8和9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。As shown in Table 2, the sample of Example 1 (microalgae oil 0%+shea butter 0%) is used as a control, and its gene relative expression is 100%. The gene expression of samples 8 and 9 and the positive control sample were compared to obtain the corresponding percentages.
具体来说,屏障因子FLG在实施例2样品(乳木果油5%)、实施例3 样品(微藻油5%)、实施例4样品(微藻油1%+乳木果油8%)、实施例5样品(微藻油3%+乳木果油6%)、实施例6样品(微藻油4.5%+乳木果油4.5%)、实施例7样品(微藻油6%+乳木果油3%)、实施例8样品(微藻油7%+乳木果油2%)、实施例9样品(微藻油8%+乳木果油1%)和阳性对照(罗格列酮)处理后,与实施例1样品(微藻油0%+乳木果油0%)相比,分别为222%、340%、381%、439%、767%、457%、381%、340%和362%。Specifically, the barrier factor FLG in the sample of Example 2 (shea butter 5%), the sample of Example 3 (microalgae oil 5%), the sample of Example 4 (microalgae oil 1%+shea butter 8% ), Example 5 sample (microalgae oil 3%+shea butter 6%), embodiment 6 sample (microalgae oil 4.5%+shea butter 4.5%), embodiment 7 sample (microalgae oil 6% + shea butter 3%), Example 8 sample (microalgae oil 7%+shea butter 2%), embodiment 9 sample (microalgae oil 8%+shea butter 1%) and positive control ( Rosiglitazone) after treatment, compared with Example 1 sample (microalgae oil 0%+shea butter 0%), respectively 222%, 340%, 381%, 439%, 767%, 457%, 381%, 340%, and 362%.
具体来说,屏障因子LOR在实施例2样品(乳木果油5%)、实施例3样品(微藻油5%)、实施例4样品(微藻油1%+乳木果油8%)、实施例5样品(微藻油3%+乳木果油6%)、实施例6样品(微藻油4.5%+乳木果油4.5%)、实施例7样品(微藻油6%+乳木果油3%)、实施例8样品(微藻油7%+乳木果油2%)、实施例9样品(微藻油8%+乳木果油1%)和阳性对照(罗格列酮)处理后,与实施例1样品(微藻油0%+乳木果油0%)相比,分别为240%、319%、422%、504%、839%、544%、422%、323%和351%。Specifically, the barrier factor LOR in the sample of embodiment 2 (shea butter 5%), the sample of embodiment 3 (microalgae oil 5%), the sample of embodiment 4 (microalgae oil 1%+shea butter 8% ), Example 5 sample (microalgae oil 3%+shea butter 6%), embodiment 6 sample (microalgae oil 4.5%+shea butter 4.5%), embodiment 7 sample (microalgae oil 6% + shea butter 3%), Example 8 sample (microalgae oil 7%+shea butter 2%), embodiment 9 sample (microalgae oil 8%+shea butter 1%) and positive control ( Rosiglitazone) after treatment, compared with Example 1 sample (microalgae oil 0%+shea butter 0%), respectively 240%, 319%, 422%, 504%, 839%, 544%, 422%, 323%, and 351%.
具体来说,屏障因子IVL在实施例2样品(乳木果油5%)、实施例3样品(微藻油5%)、实施例4样品(微藻油1%+乳木果油8%)、实施例5样品(微藻油3%+乳木果油6%)、实施例6样品(微藻油4.5%+乳木果油4.5%)、实施例7样品(微藻油6%+乳木果油3%)、实施例8样品(微藻油7%+乳木果油2%)、实施例9样品(微藻油8%+乳木果油1%)和阳性对照(罗格列酮)处理后,与实施例1样品(微藻油0%+乳木果油0%)相比,分别为113%、75%、116%、132%、120%、129%、116%、113%和103%。Specifically, the barrier factor IVL in Example 2 sample (shea butter 5%), embodiment 3 sample (microalgae oil 5%), embodiment 4 sample (microalgae oil 1%+shea butter 8% ), Example 5 sample (microalgae oil 3%+shea butter 6%), embodiment 6 sample (microalgae oil 4.5%+shea butter 4.5%), embodiment 7 sample (microalgae oil 6% + shea butter 3%), Example 8 sample (microalgae oil 7%+shea butter 2%), embodiment 9 sample (microalgae oil 8%+shea butter 1%) and positive control ( Rosiglitazone) after treatment, compared with Example 1 sample (microalgae oil 0%+shea butter 0%), respectively 113%, 75%, 116%, 132%, 120%, 129%, 116%, 113%, and 103%.
具体来说,屏障因子TGM1在实施例2样品(乳木果油5%)、实施例3样品(微藻油5%)、实施例4样品(微藻油1%+乳木果油8%)、实施例5样品(微藻油3%+乳木果油6%)、实施例6样品(微藻油4.5%+乳木果油4.5%)、实施例7样品(微藻油6%+乳木果油3%)、实施例8样品(微藻油7%+乳木果油2%)、实施例9样品(微藻油8%+乳木果油1%)和阳性对照(罗格列酮)处理后,与实施例1样品(微藻油0%+乳木果油 0%)相比,分别为134%、134%、178%、211%、246%、195%、178%、149%和161%。Specifically, the barrier factor TGM1 in the sample of embodiment 2 (shea butter 5%), the sample of embodiment 3 (microalgae oil 5%), the sample of embodiment 4 (microalgae oil 1%+shea butter 8% ), Example 5 sample (microalgae oil 3%+shea butter 6%), embodiment 6 sample (microalgae oil 4.5%+shea butter 4.5%), embodiment 7 sample (microalgae oil 6% + shea butter 3%), Example 8 sample (microalgae oil 7%+shea butter 2%), embodiment 9 sample (microalgae oil 8%+shea butter 1%) and positive control ( Rosiglitazone) after treatment, compared with Example 1 sample (microalgae oil 0%+shea butter 0%), respectively 134%, 134%, 178%, 211%, 246%, 195%, 178%, 149%, and 161%.
具体来说,屏障因子CASP14在实施例2样品(乳木果油5%)、实施例3样品(微藻油5%)、实施例4样品(微藻油1%+乳木果油8%)、实施例5样品(微藻油3%+乳木果油6%)、实施例6样品(微藻油4.5%+乳木果油4.5%)、实施例7样品(微藻油6%+乳木果油3%)、实施例8样品(微藻油7%+乳木果油2%)、实施例9样品(微藻油8%+乳木果油1%)和阳性对照(罗格列酮)处理后,与实施例1样品(微藻油0%+乳木果油0%)相比,分别为188%、316%、300%、485%、667%、424%、300%、279%和330%。Specifically, the barrier factor CASP14 in the sample of embodiment 2 (shea butter 5%), the sample of embodiment 3 (microalgae oil 5%), the sample of embodiment 4 (microalgae oil 1%+shea butter 8% ), Example 5 sample (microalgae oil 3%+shea butter 6%), embodiment 6 sample (microalgae oil 4.5%+shea butter 4.5%), embodiment 7 sample (microalgae oil 6% + shea butter 3%), Example 8 sample (microalgae oil 7%+shea butter 2%), embodiment 9 sample (microalgae oil 8%+shea butter 1%) and positive control ( Rosiglitazone) after treatment, compared with Example 1 sample (microalgae oil 0%+shea butter 0%), respectively 188%, 316%, 300%, 485%, 667%, 424%, 300%, 279%, and 330%.
具体来说,屏障因子HMGCR在实施例2样品(乳木果油5%)、实施例3样品(微藻油5%)、实施例4样品(微藻油1%+乳木果油8%)、实施例5样品(微藻油3%+乳木果油6%)、实施例6样品(微藻油4.5%+乳木果油4.5%)、实施例7样品(微藻油6%+乳木果油3%)、实施例8样品(微藻油7%+乳木果油2%)、实施例9样品(微藻油8%+乳木果油1%)和阳性对照(罗格列酮)处理后,与实施例1样品(微藻油0%+乳木果油0%)相比,分别为170%、281%、291%、326%、450%、342%、291%、284%和229%。Specifically, the barrier factor HMGCR in the sample of embodiment 2 (shea butter 5%), the sample of embodiment 3 (microalgae oil 5%), the sample of embodiment 4 (microalgae oil 1%+shea butter 8% ), Example 5 sample (microalgae oil 3%+shea butter 6%), embodiment 6 sample (microalgae oil 4.5%+shea butter 4.5%), embodiment 7 sample (microalgae oil 6% + shea butter 3%), Example 8 sample (microalgae oil 7%+shea butter 2%), embodiment 9 sample (microalgae oil 8%+shea butter 1%) and positive control ( Rosiglitazone) after treatment, compared with Example 1 sample (microalgae oil 0%+shea butter 0%), respectively 170%, 281%, 291%, 326%, 450%, 342%, 291%, 284%, and 229%.
具体来说,屏障因子AQP3在实施例2样品(乳木果油5%)、实施例3样品(微藻油5%)、实施例4样品(微藻油1%+乳木果油8%)、实施例5样品(微藻油3%+乳木果油6%)、实施例6样品(微藻油4.5%+乳木果油4.5%)、实施例7样品(微藻油6%+乳木果油3%)、实施例8样品(微藻油7%+乳木果油2%)、实施例9样品(微藻油8%+乳木果油1%)和阳性对照(罗格列酮)处理后,与实施例1样品(微藻油0%+乳木果油0%)相比,分别为112%、131%、151%、197%、204%、167%、151%、171%和131%。Specifically, the barrier factor AQP3 in the sample of embodiment 2 (shea butter 5%), the sample of embodiment 3 (microalgae oil 5%), the sample of embodiment 4 (microalgae oil 1%+shea butter 8% ), Example 5 sample (microalgae oil 3%+shea butter 6%), embodiment 6 sample (microalgae oil 4.5%+shea butter 4.5%), embodiment 7 sample (microalgae oil 6% + shea butter 3%), Example 8 sample (microalgae oil 7%+shea butter 2%), embodiment 9 sample (microalgae oil 8%+shea butter 1%) and positive control ( Rosiglitazone) after treatment, compared with Example 1 sample (microalgae oil 0%+shea butter 0%), respectively 112%, 131%, 151%, 197%, 204%, 167%, 151%, 171%, and 131%.
具体来说,屏障因子ZO-1在实施例2样品(乳木果油5%)、实施例3样品(微藻油5%)、实施例4样品(微藻油1%+乳木果油8%)、实施例5样品(微藻油3%+乳木果油6%)、实施例6样品(微藻油4.5%+乳木 果油4.5%)、实施例7样品(微藻油6%+乳木果油3%)、实施例8样品(微藻油7%+乳木果油2%)、实施例9样品(微藻油8%+乳木果油1%)和阳性对照(罗格列酮)处理后,与实施例1样品(微藻油0%+乳木果油0%)相比,分别为143%、214%、314%、318%、402%、303%、314%、240%和246%。Specifically, the barrier factor ZO-1 in the sample of embodiment 2 (shea butter 5%), the sample of embodiment 3 (microalgae oil 5%), the sample of embodiment 4 (microalgae oil 1%+shea butter 8%), Example 5 sample (microalgae oil 3%+shea butter 6%), embodiment 6 sample (microalgae oil 4.5%+shea butter 4.5%), embodiment 7 sample (microalgae oil 6%+shea butter 3%), Example 8 sample (microalgae oil 7%+shea butter 2%), example 9 sample (microalgae oil 8%+shea butter 1%) and positive After the control (rosiglitazone) was treated, it was 143%, 214%, 314%, 318%, 402%, 303%, respectively, compared with the sample of Example 1 (microalgae oil 0%+shea butter 0%) %, 314%, 240%, and 246%.
综上,实施例2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3样品(微藻油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4样品(微藻油1%+乳木果油8%)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5样品(微藻油3%+乳木果油6%)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6样品(微藻油4.5%+乳木果油4.5%)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7样品(微藻油6%+乳木果油3%)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8样品(微藻油7%+乳木果油2%)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(微藻油8%+乳木果油1%)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。In summary, the sample in Example 2 (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. Protective effect. The sample of Example 3 (microalgae oil 5%) promotes the expression of FLG, LOR, 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 repair. The sample of Example 4 (microalgae oil 1%+shea butter 8%) 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. The sample of Example 5 (microalgae oil 3%+shea butter 6%) 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 6 (microalgae oil 4.5%+shea butter 4.5%) 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. The sample of Example 7 (microalgae oil 6%+shea butter 3%) 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 8 (microalgae oil 7%+shea butter 2%) 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 (microalgae oil 8%+shea butter 1%) 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.
应用例Application example
本发明所述的包含微生物油脂和植物油脂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。The compositions comprising microbial oils and vegetable oils of the present invention can be used as intermediate raw materials or functional additives for the preparation of medicines or external skin preparations, and the external skin preparations are preferably cosmetic compositions, including but not limited to creams, Preparation of lotion, gel, lotion, essence, mask, eye cream, aerosol (cleaning foam), spray, shower gel, massage oil, facial cleanser and other dosage forms.
本发明所述包含微生物油脂和植物油脂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);更优选的重量百分比为0.01%-40%(w/w)。The weight percent of the composition comprising microbial oil and vegetable oil in the skin external preparation of the present invention is 0.001%-100% (w/w); the preferred weight percent is 0.01%-60% (w/w); more The preferred weight percentage is 0.01%-40% (w/w).
以下是实施例3-6和8获得的包含微生物油脂和植物油脂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:The following are specific application examples of the compositions containing microbial oils and vegetable oils obtained in Examples 3-6 and 8 in external skin preparations, as well as the formulations and preparation methods of these dosage forms. Specific application examples are as follows:
应用例1:面霜的制备Application example 1: Preparation of face cream
Figure PCTCN2022125279-appb-000009
Figure PCTCN2022125279-appb-000009
应用例2:乳液的制备Application Example 2: Preparation of Emulsion
Figure PCTCN2022125279-appb-000010
Figure PCTCN2022125279-appb-000010
应用例3:眼霜的制备Application example 3: Preparation of eye cream
Figure PCTCN2022125279-appb-000011
Figure PCTCN2022125279-appb-000011
Figure PCTCN2022125279-appb-000012
Figure PCTCN2022125279-appb-000012
应用例4:面膜的制备Application Example 4: Preparation of facial mask
Figure PCTCN2022125279-appb-000013
Figure PCTCN2022125279-appb-000013
Figure PCTCN2022125279-appb-000014
Figure PCTCN2022125279-appb-000014
应用例5:精华液的制备Application Example 5: Preparation of Essence
Figure PCTCN2022125279-appb-000015
Figure PCTCN2022125279-appb-000015
Figure PCTCN2022125279-appb-000016
Figure PCTCN2022125279-appb-000016
应用例6:本发明中的实施例2-9也可以单独作为皮肤外用剂单独使用。Application example 6: Examples 2-9 in the present invention can also be used alone as skin external preparations.

Claims (12)

  1. 一种油脂组合物,所述油脂包括微生物油脂和植物油脂,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%的油脂。An oil composition, the oil includes microbial oil and vegetable oil, wherein, based on the total weight of the composition, the composition contains at least 0.5% by weight of oil.
  2. 如权利要求1所述的组合物,所述微生物油脂与所述植物油脂的重量比为1:8至8:1。The composition according to claim 1, the weight ratio of the microbial oil to the vegetable oil is 1:8 to 8:1.
  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。The composition according to claim 1, wherein the composition also comprises a natural surfactant selected from the group consisting of: lecithin, cholesterol, lanolin, tea saponin, protein, saponins, Sugars, alkyl polyglycosides or combinations thereof.
  4. 如权利要求2所述的组合物,其中,所述天然表面活性剂是氢化卵磷脂。The composition of claim 2, wherein said natural surfactant is hydrogenated lecithin.
  5. 如权利要求3或4所述的组合物,其中,所述油脂与所述天然表面活性剂的重量比为1:1至20:1。The composition according to claim 3 or 4, wherein the weight ratio of the oil to the natural surfactant is 1:1 to 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。The composition according to claim 5, wherein the weight ratio of the vegetable oil to the natural surfactant is 10:1 to 20:1.
  7. 如权利要求1所述的组合物,其中,所述植物油脂为植物种子油脂、植物果实油脂或它们的组合,其中,所述植物种子油脂选自: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、白羽扇豆籽油或它们的组合,其中,所述植物果实油脂选自: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。The composition according to claim 1, wherein the vegetable oil is plant seed oil, plant fruit oil or their combination, wherein the plant seed oil is selected from the group consisting of jojoba seed oil, safflower seed oil, white pool 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 Hard Walnut Seed Oil, Grass Cotton Seed Oil, Tea Seed Oil, Millet Seed Oil, Papaya Seed Oil, Raspberry Seed Oil, Baobab Seed Oil, Gold Calendula seed oil, oleifera seed oil, Moringa seed oil, American hickory seed oil, perilla seed oil, babassu seed oil, white lupine seed oil or their combination, wherein the plant fruit oil is selected from 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, Rosa Dogtooth Fruit Oil, Pepper Fruit Oil, Brazil Nectarine Fruit Oil, Pimento Fruit Oil, Anise Fruit Oil, Mauritius Fruit Oil, Juniper Fruit Oil, Litsea Pepper Fruit Oil, Wenzhou Satsuma Fruit Oil, Star Fruit Palm Fruit oil, rosehip oil, coriander fruit oil, or a combination thereof.
  8. 如权利要求1所述的组合物,其中所述微生物油脂选自:微藻油、雨生红球藻油、长耳齿状藻油或它们的组合。The composition according to claim 1, wherein the microbial oil is selected from the group consisting of microalgae oil, Haematococcus pluvialis oil, Dentate algae oil or their combination.
  9. 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。Application of the composition as claimed in claim 1 in enhancing the skin barrier function.
  10. 如权利要求9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。The application according to claim 9, wherein said enhancement of skin barrier function is achieved by enhancing the vitality of the skin barrier and/or promoting the expression of skin barrier-related factors.
  11. 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。Application of the composition as claimed in claim 1 in the preparation of medicines and/or skin external preparations for enhancing skin barrier function.
  12. 如权利要求11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。The use according to claim 11, the medicine and/or skin external preparation comprises 0.001-100% by weight of the composition.
PCT/CN2022/125279 2021-12-14 2022-10-14 Composition containing microbial oil and vegetable oil and use thereof WO2023109290A1 (en)

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CN114146027A (en) * 2021-12-14 2022-03-08 上海家化联合股份有限公司 Composition containing microbial oil and vegetable oil and application thereof
CN114796024B (en) * 2022-04-14 2023-06-20 珠海金肽生物科技有限公司 Bionic sebum composition for skin barrier repair, and preparation method and application thereof

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