CN108852865A - A kind of fullerene topical composition - Google Patents

Abstract

The invention discloses an oil-soluble fullerene external composition and its preparation method and application. The oil-soluble fullerene external composition contains an oil-soluble auxiliary agent and fullerene dissolved in the oil-soluble auxiliary agent. The composition It has a cosmetic effect.

Description

A kind of fullerene composition for external application

technical field

The invention relates to the field of daily chemicals, in particular to an external composition with cosmetic effect.

Background technique

In 1985, scientists Kroto, Smalley, Curl and others discovered C60 fullerene when studying carbon elements in deep space. In 1996, they won the Nobel Prize in Chemistry for this. Fullerene, diamond and graphite are allotropes of carbon. C60 is a spherical molecule composed of 60 carbon atoms, consisting of 12 pentagons and 20 hexagons. Each carbon atom and the adjacent ^three carbon atoms form bonds through SP2 hybridization. It is named for its shape like a football. Called CITE. A series of molecules with a caged carbon atom cluster structure are collectively referred to as molecules are collectively referred to as caged Note><Cite><Auene derivatives and heterocyclic fullerenes. Common C60, C70, C76, C84 and other types.

The large π-bonded conjugated system composed of multiple P orbitals of fullerene makes it have a strong ability to accept electrons. Because of its unique structure and physical and chemical properties, it has excellent free radical scavenging performance, known as The "free radical sponge" also exhibits excellent antioxidant properties. It has been widely concerned in cosmetic materials, biomedicine and other aspects.

By embedding C60 into surfactants, C60 can still eliminate reactive oxygen species in cells, inhibit mitochondrial depolarization, activation of cysteine proteases, exposure of phosphatidylserine on cell membranes, and DNA cleavage, and C60 exhibits Protect cells from oxidative apoptosis. C60 liposome complex plays an anti-oxidant role by defending against UVA damage to skin structure, cell nucleus and collagen fibers, and penetrating into human skin tissue. It is 172 times that of vitamin C and can affinity free radicals.

Professor Fathi Moussa has been engaged in the research on the properties of C60 for a long time. As the first person to study dissolving fullerene in olive oil, they fed mice 10-17 months every two weeks (feeding 4 mg richerene per kg body weight) Fullerene), the mice in the control group died within 17-38 months, while the life span of the experimental group was extended to 59-66 months. It was found that fullerene has a longevity health care function. During the period, regardless of body weight, there was no abnormality in physiological performance, and no toxicity or biological heredity of C60 was found. On the contrary, a certain amount of C60 has the ability to scavenge free radicals, thereby protecting animals from the harm of excessive free radicals.

As an external product, fullerene-related products have been reported in patents, such as C60-PVP, application numbers: 200480005008.1, 200580049615.2. Due to the limitations of the preparation process and the composite characteristics of PVP and C60, the content of C60 in this composite is not high. More than 1%, in addition, PVP has obvious film-forming properties, and excessive application on the surface of the skin will hinder the performance of certain cosmetics. C60-squalane, application number 201510427642.4, but the solubility of C60 in squalane is limited, and squalane is an oil solution, which limits the use of this series of products. Fullerene nano-suspension CN201510971343.7, but this component is a fullerene component with large particles, which will affect the stability, appearance and use comfort of the formula after being added to the formula, and the fullerene component with large particles is difficult to remove The skin plays a repairing role and can only adhere to the surface layer of the skin to act as a barrier.

Fullerene is a non-polar molecule with strong hydrophobicity and can only be dissolved in non-polar organic solvents such as toluene, benzene, cyclohexane, and chloroform that are harmful to organisms. The hydrophobic nature of fullerene itself directly affects its biological activity. In order to better promote absorption, fullerene is made into a solution type that is easy for the skin to absorb quickly and is in a molecular state. Fullerene is compounded with a skin-friendly type components have not been studied.

The fullerene-containing composition invented by the patent of the present invention ensures that the fullerene is dispersed in the selected solvent in a molecular state, and the obtained fullerene-containing composition has stable properties and can be used in any external formulation. The fullerene in the composition of the present invention is in a dissolved state, and as an external product component, it can better act on the skin.

Contents of the invention

The purpose of the present invention is to provide a fullerene composition, in which the fullerene is in a dissolved state and absorbed quickly, and has the effects of whitening and removing spots, removing wrinkles, anti-acne, and preventing hair loss and solidification.

In one aspect, the present invention provides a fullerene composition comprising an oil solubility aid and fullerene dissolved or dispersed in the oil solubility aid.

In one aspect, the present invention provides a fullerene dispersion system, the system contains fullerene and oil solubility additives, characterized in that more than 50% of the dispersion system, such as 60%, 70%, 80% , 90%, 95%, 99% or more of the particle size is less than 5nm.

In one aspect, the present invention provides a method for preparing a fullerene composition or dispersion system, which is characterized in that it comprises the following steps: taking fullerene powder and an oil-soluble additive, mixing them uniformly, and putting them into a high-pressure homogenizer In, 50-500MPa, preferably 100-300MPa, more preferably 200MPa homogeneous 1-10 times, preferably 3-8 times, more preferably 5 times, then control the temperature of the material at 0-25°C, preferably 5-20°C, further Stir preferably at 10-15°C for 1-20h, preferably 5-15h, more preferably 12h, then centrifuge and/or filter to obtain the product.

In one aspect, the invention provides a fullerene composition or dispersion prepared using the method of the invention.

According to any one of the foregoing aspects, the present invention provides a fullerene composition, which is characterized in that, in addition to the oil-soluble additive and fullerene, it also contains at least one antioxidant.

According to any one of the aforementioned aspects, the present invention provides a fullerene composition, which is characterized in that, in addition to the oil-soluble additive and fullerene, it also contains at least one other active ingredient.

According to any one of the foregoing aspects, the present invention provides an application of a fullerene composition in the preparation of cosmetic or cosmetic products.

According to any one of the foregoing aspects, the present invention provides an application of a fullerene composition in the preparation of a device for beauty or cosmetic use.

According to any of the foregoing aspects, the present invention provides a cosmetic method, the method comprising administering to a subject an effective amount of the composition of the present invention or a medicament comprising the composition of the present invention, optionally, the cosmetic effect includes At least one of whitening, anti-freckle, anti-wrinkle, anti-acne, anti-hair loss.

According to any of the aforementioned aspects, the composition of the present invention can also be used together with other auxiliary materials.

According to any of the preceding aspects, the compositions of the invention may be used together with a surfactant.

According to any of the preceding aspects, the composition of the invention may be incorporated into a cosmetic or pharmaceutical delivery system and/or a sustained release system.

According to any of the foregoing aspects, the oil-soluble auxiliary agent is selected from at least one of: jojoba oil, capric acid triglyceride, isooctyl palmitate, isopropyl palmitate, and myristyl myristate , preferably, the oil-soluble additive is at least one of jojoba oil, caprylic triglyceride, and isooctyl palmitate.

According to any of the foregoing aspects, the fullerene is one or more of hollow fullerenes, metal fullerenes, heterocyclic fullerenes and embedded fullerenes. Including but not limited to fullerenes C _2n , M@C _2n , M ₂ @C _2n , MA@C _2n , M ₃ N@C _2n , M ₂ C ₂ @C _2n , M ₂ S@C _2n , M ₂ Any of O@C _2n and M _x A _3-x N@C _2n , wherein M and A are metal elements, and the M and A are selected from any of Sc, Y and lanthanide metal elements One; 30≤n≤60; 0≤x≤3, preferably, the fullerene is any one of C60, C70, C76, C84, Gd@C82 and its derivatives or a mixture thereof, more preferably Preferably, the fullerene is C60.

The composition of the present invention can be in the form of a liquid preparation, for example, an oily suspension, a solution, or a dry product that can be reconstituted with water or other suitable carriers before use. Such liquid preparations may contain conventional additives such as suspending agents, for example sorbitol, methylcellulose, gelatin, hydroxyethylcellulose, carboxymethylcellulose, aluminum stearate gel or hydrogenated edible fats; solutions It is usually prepared by dissolving the active substance in a carrier and filter sterilizing before filling into a suitable vial or ampoule, which is then hermetically sealed.

In one aspect, the present invention provides a method for preparing an aqueous solution from a fullerene composition: mix the fullerene composition with water in proportion, stir evenly, and then homogenize well, then add preservatives and flavors to obtain the aqueous solution.

The composition of the present invention is prepared in the form of an emulsion, which may contain conventional emulsifiers, co-emulsion agents, surfactants and the like.

In one aspect, the present invention provides a method for preparing an emulsion from a fullerene composition: mixing the fullerene composition with an emulsifier in proportion, then homogenizing, forming an emulsion or paste, adding preservatives and essences to obtain an emulsion .

In one aspect, the invention provides the use of a composition or dispersion according to the invention for the preparation of a cosmetic or cosmetic product.

In one aspect, the invention provides the use of a composition or dispersion according to the invention for the manufacture of a cosmetic or make-up device.

According to any one of the foregoing aspects, the beauty or cosmetic product is used for whitening and removing spots, removing wrinkles, anti-acne, anti-haze, hair growth and strengthening, etc.

Description of drawings

Figure 1: Electron microscope experiment results.

Figure 2: Acne removal experiment.

Figure 3: Quantitative results of the acne removal experiment.

Figure 4: Whitening experiment results.

Figure 5: Anti-haze experiment results.

Detailed ways

The specific embodiments of the present invention will be described in detail below in conjunction with the accompanying drawings, but it should be understood that the protection scope of the present invention is not limited by the specific embodiments.

Unless expressly stated otherwise, throughout the specification and claims, the term "comprise" or variations thereof such as "includes" or "includes" and the like will be understood to include the stated elements or constituents, and not Other elements or other components are not excluded.

In one embodiment, the present invention provides a fullerene composition, which contains oil-soluble additives and fullerenes dissolved or dispersed in oil-soluble additives, optionally, the fullerene concentration 0.01-5 mg/ml, preferably 0.05-3 mg/ml, more preferably 0.1-2 mg/ml, further preferably 1 mg/ml.

In one embodiment, the present invention provides a fullerene dispersion system, the system contains fullerene and oil solubility additives, characterized in that more than 50% of the dispersion system, such as 60%, 70%, 80%, 90%, 95%, 99% or more of the particle size is less than 5nm.

In one embodiment, the present invention provides a method for preparing a fullerene composition or dispersion system, which is characterized in that it includes the following steps: take fullerene powder, oil-soluble additives, mix them uniformly, and put them into a high-pressure homogeneous In the quality machine, 50-500MPa, preferably 100-300MPa, more preferably 200MPa homogenize 1-10 times, preferably 3-8 times, more preferably 5 times, and then control the temperature of the material at 0-25°C, preferably 5-20°C , further preferably at 10-15°C, stirring for 1-20h, preferably 5-15h, more preferably 12h, and then centrifuging and/or filtering to obtain the product.

In one embodiment, the present invention provides a fullerene composition characterized in that, in addition to oil-soluble additives and fullerenes, it also contains at least one antioxidant selected from superoxidized dismutase, mannitol, histidine, tryptophan, bilirubin, quercetin, quercetin, polyphenols, proanthocyanidins, tocotrienols, catechin, catechin derivatives, rutin and Its derivatives, gallic acid and its derivatives, ubiquinone, astaxanthin, carotene, and other carotenoids and their derivatives and their salts, vitamin B and their derivatives and their salts, At least one of vitamin Ds and their derivatives and their salts, vitamin Es and their derivatives and their salts, dibutylhydroxytoluene and butylhydroxyanisole.

In one embodiment, the present invention provides a fullerene composition, characterized in that, in addition to oil-soluble additives and fullerenes, it also contains at least one additional active ingredient, which includes but Not limited to: matrix metalloelastase inhibitors, melanin synthesis stimulators or inhibitors, whitening or depigmenting agents, chromogen formers, self-tanning agents, antiaging agents, NO-synthase inhibitors, antioxidants, free Base scavengers and/or anti-air pollution agents, anti-glycation agents, emulsifiers, emollients, organic solvents, liquid propellants, skin conditioning agents such as humectants, moisture-retaining substances, alpha hydroxy acids, beta hydroxy acids, moisturizing agents, epidermal hydrolytic enzymes, vitamins, pigments or coloring agents, dyes, gel polymers, thickening agents, surfactants, emollients, anti-wrinkle agents, agents capable of reducing or treating bags under the eyes, exfoliating agents, antimicrobial agents, Fungicide, antifungal agent, bactericide, bacteriostatic agent, dermal or epidermal macromolecular synthesis stimulator and/or agent capable of preventing or inhibiting dermal or epidermal macromolecular degradation, collagen synthesis stimulator, elastin synthesis stimulator agent, decorin synthesis stimulator, laminin synthesis stimulator, defensin synthesis stimulator, molecular chaperone synthesis stimulator, aquaporin synthesis stimulator, hyaluronic acid synthesis stimulator, lipids and components of the stratum corneum Synthesis stimulator, ceramide synthesis stimulator, collagen degradation inhibitor, elastin degradation inhibitor, fibroblast proliferation stimulator, keratinocyte proliferation stimulator, adipocyte proliferation stimulator, melanocyte proliferation stimulator, keratin Formation cell differentiation stimulator, adipocyte differentiation stimulator, acetylcholinesterase inhibitor, skin relaxant, glycosaminoglycan synthesis stimulator, DNA repair agent, DNA protection agent, antipruritic agent, for the treatment and/or care of sensitive Skin agent, curing agent, anti-atrophic striae agent, astringent, agent for regulating sebum production, lipolysis stimulator, anti-cellulite agent, healing stimulator, healing auxiliary adjuvant, re-epithelialization stimulator, re-epithelialization Auxiliary adjuvants, cytokine growth factors, sedatives, anti-inflammatory agents, agents acting on capillary circulation and/or microcirculation, angiogenesis stimulators, vascular permeability inhibitors, agents acting on cell metabolism, for improving dermis - Epidermal junction agents, agents that promote hair growth, agents that inhibit or delay hair growth, preservatives, fragrances, chelating agents, plant extracts, essential oils, marine extracts, agents from biological fermentation processes, mineral salts, cells Extracts and sunscreens (organic or mineral photoprotectants acting against UVA and/or UVB), or mixtures thereof.

In one embodiment, the present invention provides an application of a fullerene composition in the preparation of cosmetic or cosmetic products.

In one embodiment, the cosmetic or cosmetic dosage forms include, but are not limited to, solutions, suspensions, emulsions, ointments, gels, creams, lotions, powders, soaps, surfactant-containing cleansers, oils , powder foundations, lotions, foundations, wax foundations, sprays, liniments, pastes and poultices in any dosage form, such as creams, complex emulsions, anhydrous compositions, aqueous dispersions, oils, Lotions, balms, foams, lotions, gels, cream gels, hydroalcoholic solutions, water glycol solutions, liniments, saline solutions, soaps, shampoos, conditioners, serums, ointments, mousses, ointments powder, stick, pen, spray, aerosol, capsule, gelatin capsule, tablet, sugar-coated tablet, powder, granular form, chewing gum, solution, suspension, emulsion, syrup, polysaccharide film, jelly Gel, gelatin, ointment, cream, softening lotion, nourishing lotion, mask, essence, hair tonic, shampoo, rinse, conditioner, hair conditioner, gel, skin lotion, skin softener , toner, astringent, lotion, milk lotion, moisturizing lotion, nourishing lotion, massage cream, nourishing cream, moisturizing cream, hand cream, foundation cream, nourishing essence, sunscreen, soap, cleansing foam, cleansing milk, cleansing cream, Body lotions and body cleansers, eye bag removers, makeup foundations, makeup remover lotions, makeup remover lotions, eye shadows, lipsticks, lip glosses and lip powders; the effects of said beauty or cosmetic products include but are not limited to: skin whitening, pigmentation improvement, Treatment of acne, improvement of wrinkles, improvement of rough skin, improvement of oily skin, improvement of dry skin, shrinking pores, treatment of scars, treatment of flushing, treatment of hair loss, promotion of hair growth, treatment of burns, skin sterilization, skin killing mites, improvement of skin pits, anti At least one of acne and haze prevention.

In one embodiment, the present invention provides an application of a fullerene composition in the preparation of devices for cosmetic or make-up purposes, including but not limited to, disinfectant wipes, sterile cotton swabs, sterile packs, medical Dressing wet wipes, nursing solutions, cleaning solutions, dressings, liquid dressings, band-aids; the application may be that the composition of the present invention is attached to a specific material, and the materials include but are not limited to: cotton swabs, wet wipes, towels, paper towels, gauze , cotton swabs, non-woven fabrics, polymer materials, medical dressings, non-stick gauze for plastic models, vaseline oiled gauze, semi-permeable membranes, foam accessories, etc.

In one embodiment, the composition of the present invention can also be used together with other auxiliary materials, which include hyaluronic acid, oils, surfactants, preservatives, spices, adhesives, thickeners, complexing agents, PH regulator.

In one embodiment, the compositions of the present invention may be used with a surfactant selected from the group consisting of: anionic surfactants, cationic surfactants, amphoteric surfactants, lipophilic nonionic surfactants, lipophilic At least one of water-based nonionic surfactants and natural surfactants.

In one embodiment, examples of anionic surfactants include soap raw materials, fatty acid soaps such as sodium laurate and sodium palmitate, higher alkyl sulfates such as sodium lauryl sulfate and potassium lauryl sulfate, polyoxyethylene (POE)-Triethanolamine lauryl sulfate, POE-Alkyl ether sulfate salts such as sodium lauryl sulfate, N-acyl sarcosine such as sodium lauroyl sarcosinate, N-myristoyl-N-methyl taurine Higher fatty acid amide sulfonates such as sodium coconut oil fatty acid methyl taurate, sodium lauryl methyl taurate, POE-sodium oleyl ether phosphate, POE-stearyl ether phosphoric acid and other phosphate ester salts, Di-2-Ethylhexyl Sodium Sulfosuccinate, Sodium Monolauroyl Monoethanolamide Polyoxyethylene Sulfosuccinate, Sodium Lauryl Polypropylene Glycol Sulfosuccinate, etc. Sulfosuccinates, Linear Lauryl Sodium benzenesulfonate, triethanolamine linear dodecylbenzenesulfonate, linear dodecylbenzenesulfonic acid and other alkylbenzenesulfonates, monosodium N-lauroyl glutamate, N-stearyl glutamate N-acyl glutamic acid salts such as disodium phosphate, monosodium N-myristoyl-L-glutamate, etc., high fatty acid ester sulfates such as hardened coconut oil fatty acid glycerin sodium sulfate, sulfated oils such as Turkish red oil , POE-alkyl ether carboxylic acid, POE-alkyl allyl ether carboxylate, α-olefin sulfonate, higher fatty acid ester sulfonate, secondary alcohol sulfate, higher fatty acid alkyl alcohol amide sulfate Salt, sodium lauroyl monoethanolamide succinate, N-palmitoyl aspartic acid di-triethanolamine, and sodium caseinate.

In one embodiment, as the cationic surfactant, for example, alkyltrimethylammonium salts such as stearyltrimethylammonium chloride and lauryltrimethylammonium chloride, distearyldimethylammonium chloride, etc. Ammonium chloride dialkyldimethylammonium salt, poly(N,N'-dimethyl-3,5-methylenepiperidinium chloride), cetylpyridinium chloride and other alkylpyridinium salts, Alkyl quaternary ammonium salts, alkyl dimethyl benzyl ammonium salts, alkyl isoquinolinium salts, dialkylmorpholinium salts, POE-alkylamines, alkylamine salts, polyamine fatty acid derivatives, ammonium At least one of alcohol fatty acid derivatives, benzalkonium chloride and benzethonium chloride.

In one embodiment, as the amphoteric surfactant, for example, 2-undecyl-N,N,N-(hydroxyethylcarboxymethyl)-2-imidazolinium sodium, 2-cocoyl-2 -imidazoline hydroxide-1-carboxyethoxy disodium salt and other imidazoline amphoteric surfactants, 2-heptadecyl-N-carboxymethyl-N-hydroxyethylimidazolinium betaine, lauryl At least one of betaine-based amphoteric surfactants such as dimethylaminoacetic acid betaine, alkyl betaine, amido betaine, and sultaine.

In one embodiment, examples of lipophilic nonionic surfactants include sorbitan monooleate, sorbitan monoisostearate, sorbitan monolaurate, sorbitan Alcohol monopalmitate, sorbitan monostearate, sorbitan sesquioleate, sorbitan trioleate, penta-2-ethylhexanoic acid diglyceryl sorbitan , tetra-2-ethylhexanoic acid diglyceride sorbitan esters and other sorbitan fatty acid esters, mono-cottonseed oil fatty acid glycerides, monoerucic acid glycerides, sesquioleic acid glycerides, glyceryl monostearate Fatty acid glycerides such as esters, α, α'-oleic acid pyroglutamic acid glyceryl ester, glyceryl monostearate, polyglyceryl fatty acid such as monoisostearic acid diglyceride, diisostearic acid diglyceride At least one of esters, propylene glycol fatty acid esters such as propylene glycol monostearate, hardened castor oil derivatives, and glycerin alkyl ethers.

In one embodiment, examples of the hydrophilic nonionic surfactant include POE-sorbitan monooleate, POE-sorbitan monostearate, POE-sorbitan monooleate Ester, POE-sorbitan tetraoleate and other POE-sorbitan fatty acid esters, POE-sorbitol monolaurate, POE-sorbitol monooleate, POE-sorbitol five Oleate, POE-sorbitol monostearate and other POE-sorbitol fatty acid esters, POE-glycerol monostearate, POE-glycerol monoisostearate, POE-glycerol triisostearate Ester, etc. POE-glycerin fatty acid esters, POE-monooleate, POE-distearate, POE-monooleate, distearic acid ethylene glycol ester, etc. POE-fatty acid esters, POE- Lauryl ether, POE-oleyl ether, POE-stearyl ether, POE-behenyl ether, POE-2-octyl dodecyl ether, POE-cholestanol ether, etc. POE-alkyl ethers Classes, Pluronic (addition polymer of polypropylene glycol and ethylene oxide) and other Pluronic types, POE·POP-cetyl ether, POE·POP-2-decyl tetradecyl ether, POE·POP-monobutyl ether, POE・POP-hydrogenated lanolin, POE・POP-glycerin ether, etc. POE・POP-alkyl ethers, POE-castor oil, POE-hardened castor oil, POE-hardened castor oil monoisostearate, POE-hardened castor Sesame oil triisostearate, POE-hardened castor oil monopyrglutamate monoisostearate, POE-hardened castor oil maleic acid, etc. POE-castor oil hardened castor oil derivatives, POE-sorbitol Beeswax and other POE-beeswax and lanolin derivatives, coconut oil fatty acid diethanolamide, lauric acid monoethanolamide, fatty acid isopropanolamide and other alkanolamides, POE-propylene glycol fatty acid ester, POE-alkylamine, POE-fatty acid At least one of amide, sucrose fatty acid ester, POE-nonylphenyl formaldehyde condensate, alkyl ethoxy dimethyl amine oxide, and trioleyl phosphoric acid.

In one embodiment, examples of natural surfactants include at least one of lecithins such as soybean lecithin, hydrogenated soybean lecithin, lecithin, hydrogenated egg yolk lecithin, soybean saponin, and the like.

In one embodiment, the composition of the invention may be incorporated into a cosmetic or pharmaceutical delivery system and/or sustained release system selected from the group consisting of liposomes , mixed liposomes, millimeter microcapsules, microcapsules, nanocapsules, sponges, cyclodextrins, vesicles, micelles, surfactant mixed micelles, phospholipid-surfactant mixed micelles, millimeter microspheres, micro spheres, nanospheres, lipospheres, microemulsions, nanoemulsions, millimeter particles, microparticles, nanoparticles and solid lipid nanoparticles.

In one embodiment, the oily auxiliary agent can be selected from at least one of liquid oil, solid oil, wax, hydrocarbon oil, higher fatty acid, higher alcohol, ester oil, and silicone oil.

In one embodiment, examples of liquid fats and oils include avocado oil, camellia oil, turtle oil, macadamia oil, corn oil, sunflower oil, mink oil, olive oil, rapeseed oil, egg oil, sesame oil, almond oil , wheat germ oil, camellia oil, castor oil, linseed oil, safflower oil, grape seed oil, cottonseed oil, perilla seed oil, soybean oil, peanut oil, tea seed oil, coconut oil, rice bran oil, paulownia oil, Japan At least one of tung oil, jojoba oil, germ oil, evening primrose oil, glyceryl tricaprylate, and glyceryl triisopalmitate. In addition, the liquid fats and oils here refer to fats and oils that are liquid at room temperature.

In one embodiment, examples of solid fats include cocoa butter, coconut oil, tallow, suet, horse tallow, palm kernel oil, lard, bovine tallow, tree wax oil, tallow tallow, tree wax, hardened At least one of coconut oil, hardened palm oil, hardened tallow, hardened oil, hardened castor oil, and the like.

In one embodiment, examples of waxes include beeswax, candelilla wax, cotton wax, palm wax, bayberry wax, insect wax, spermaceti wax, montan wax, rice bran wax, kapok wax, sugarcane wax, lanolin, Lanolin acetate, liquid lanolin, isopropyl lanolin fatty acid ester, reduced lanolin, hard lanolin, hexyl laurate, jojoba wax, shellac wax, POE lanolin alcohol ether, POE lanolin alcohol acetate At least one of esters, POE cholesteryl ether, lanolin fatty acid polyethylene glycol, and POE hydrogenated lanolin alcohol ether.

In one embodiment, examples of hydrocarbon oils include liquid paraffin, isoparaffin, heavy liquid isoparaffin, paraffin, ozokerite, squalane, vegetable squalane, pristane, ceresin, At least one of squalene, petrolatum, microcrystalline wax, paraffin wax, montan wax, olefin oligomers, polyisobutylene, polybutene, and hydrogenated polybutene.

In one embodiment, examples of higher fatty acids include lauric acid, myristic acid, palmitic acid, stearic acid, behenic acid, oleic acid, undecylenic acid, tall oleic acid, isohard At least one of fatty acid, linoleic acid, linolenic acid, eicosapentaenoic acid (EPA), and docosahexaenoic acid (DHA).

In one embodiment, examples of higher alcohols include linear alcohols such as lauryl alcohol, cetyl alcohol, stearyl alcohol, behenyl alcohol, myristyl alcohol, oleyl alcohol, and cetearyl alcohol; monostearyl glycerin At least one of branched chain alcohols such as ether (bakelyl alcohol), 2-decyltetradecanol, lanolin alcohol, cholesterol, phytosterol, hexyldodecanol, isostearyl alcohol, and octyldodecanol A sort of.

In one embodiment, as the ester oil, for example, isopropyl myristate, cetyl isooctanoate, octyldodecyl myristate, isopropyl palmitate, isooctyl palmitate, stearic acid Butyl, Hexyl Laurate, Myristyl Myristate, Decyl Oleate, Caprylic Triglyceride, Hexyldecyl Dimethyl Caprylate, Cetyl Lactate, Myristyl Lactate, Octyldodecyl Lactate Alkyl esters, lanolin acetate, isocetyl stearate, isocetyl isostearate, cholesterol 12-hydroxystearate, phytosteryl 12-hydroxystearate, phytosteryl oleate, -Ethylene glycol 2-ethylhexanoate, propylene glycol dicaprate, dipentaerythritol fatty acid ester, N-alkyl glycol monoisostearate, neopentyl glycol dicaprate, diisomalate Stearyl esters, glyceryl di-2-heptylundecanoate, trimethylolpropane tri-2-ethylhexanoate, trimethylolpropane triisostearate, tetrakis-2-ethyl Pentaerythritol caproate, Glyceryl tri-2-ethylhexanoate, Glyceryl tris(caproyl caprate), Glycerin tris(caproyl tricaprate Trimyristate stearate) Esters, Trimethylolpropane Triisostearate, Cetyl 2-Ethylhexanoate, 2-Ethylhexyl Palmitate, Glyceryl Trimyristate, Tri-2-Heptyl Undecanoate Glyceryl esters, polyglyceryl diisostearate, polyglyceryl triisostearate, polyglyceryl tetraisostearate, diglyceryl triisostearate, diglyceryl tetraisostearate, three 2 - Erythritol Ethylhexanoate, Ditrimethylolpropane Tris-2-Ethylhexanoate, (Isostearic/Sebacic) Ditrimethylolpropane Oligoester, Castor Oil Fatty Acid ester, oleyl oleate, glyceryl acetate, 2-heptyl undecyl palmitate, diisobutyl adipate, (adipate·2-ethylhexanoate·stearic acid) glycerol oligomerization Ester, (2-hexylcapric acid sebacic acid) diglyceride oligoester, N-lauroyl-L-glutamic acid-2-octyldodecyl ester, di-2-heptyldecyl adipate Monoalkyl esters, ethyl laurate, di-2-ethylhexyl sebacate, 2-hexyldecyl myristate, 2-hexyldecyl palmitate, 2-hexyldecyl adipate, sebacic acid At least one of diisopropyl, 2-ethylhexyl succinate, ethyl acetate, butyl acetate, and triethyl citrate.

In one embodiment, examples of the silicone oil include chain polysiloxanes such as dimethylpolysiloxane, methylphenylpolysiloxane, and methylhydrogenpolysiloxane, octamethylcyclotetrasilicon, and the like. Oxane, decamethylcyclopentasiloxane, dodecamethylcyclohexasiloxane, tetrahydrotetramethylcyclotetrasiloxane and other cyclic polysiloxanes and polyoxyethylene polyalkylsiloxanes, etc. at least one of the

In one embodiment, the oil-soluble additive is selected from at least one of: jojoba oil, caprylic triglyceride, isooctyl palmitate, isopropyl palmitate, and myristyl myristate , preferably, the oil-soluble additive is at least one of jojoba oil, caprylic triglyceride, and isooctyl palmitate.

In one embodiment, jojoba oil, caprylic triglyceride, and isooctyl palmitate in the oil-soluble additives have a mass ratio of (1-7): (1-7): (1 -7), for example, 7:2:1, 5:4:1, 3:6:1, 6:1:3, 4:1:5, 2:1:7 is preferably 4:1:5.

In one embodiment, the fullerene is one or more of hollow fullerenes, metal fullerenes, heterocyclic fullerenes and internal fullerenes. Including but not limited to fullerenes C _2n , M@C _2n , M ₂ @C _2n , MA@C _2n , M ₃ N@C _2n , M ₂ C ₂ @C _2n , M ₂ S@C _2n , M ₂ Any of O@C _2n and M _x A _3-x N@C _2n , wherein M and A are metal elements, and the M and A are selected from any of Sc, Y and lanthanide metal elements One; 30≤n≤60; 0≤x≤3, preferably, the fullerene is any one of C60, C70, C76, C84, Gd@C82 and its derivatives or a mixture thereof, more preferably Preferably, the fullerene is C60.

In one embodiment, the composition of the present invention may be in the form of a liquid preparation, such as an oily suspension, a solution, or a dry product that can be reconstituted with water or other suitable carriers before use. Such liquid preparations may contain conventional additives such as suspending agents, for example sorbitol, methylcellulose, gelatin, hydroxyethylcellulose, carboxymethylcellulose, aluminum stearate gel or hydrogenated edible fats; solutions It is usually prepared by dissolving the active substance in a carrier and filter sterilizing before filling into a suitable vial or ampoule, which is then hermetically sealed.

In one embodiment, the present invention provides a method for preparing an aqueous solution of a fullerene composition: after mixing the fullerene composition of the present invention with water in proportion, stirring evenly, and then homogenizing well, adding preservatives and Fragrances get water solutions.

In one embodiment, the composition of the present invention is in the form of an emulsion, which may contain conventional emulsifiers, co-emulsion agents, surfactants and the like.

In one embodiment, the present invention provides a method for preparing an emulsion from a fullerene composition: mix the fullerene composition of the present invention with an emulsifier in proportion, then homogenize, form an emulsion or paste, add Preservatives and fragrances get emulsions.

In one embodiment, the invention provides the use of a composition or dispersion according to the invention for the preparation of a cosmetic or cosmetic product.

In one embodiment, the invention provides the use of a composition or dispersion according to the invention for the preparation of a cosmetic or make-up device.

Example

The present invention is further explained below with reference to examples. The descriptions of specific exemplary embodiments of the present invention have been presented for purposes of illustration and description. These descriptions are not intended to limit the invention to the precise forms disclosed, and obviously many modifications and variations are possible in light of the teachings of the present specification. The exemplary embodiments were chosen and described in order to explain the specific principles of the invention and its practical application, thereby enabling others skilled in the art to make and use various exemplary embodiments of the invention, as well as various Choose and change.

Example 1:

Take fullerene powder and oil-soluble additives, mix their mixture evenly, put it into a micro-jet high-pressure homogenizer, homogenize it for 5 times at 200MPa, then control the temperature of the material at 15 degrees, stir for 12 hours, and centrifugally filter to obtain a combination things.

The state of the fullerene composition was observed with a transmission electron microscope, and the presence of particles was not detected at a magnification of 250,000 times, indicating that the fullerene was dissolved in the auxiliary material. The results are shown in Figure 1.

Example 2:

anti wrinkle firming eye cream

Example 3:

Anti-Wrinkle Brightening Cream

Example 4:

anti hair loss shampoo

Embodiment 5: skin transmittance experiment

The fullerene composition of the present invention is prepared according to Example 1.

Control group: application number: 200480005008.1 Fullerene complex coated with micelles disclosed in Example 1.

Experimental method: select suckling pigskin as the experimental object, respectively mix the fullerene composition (in which jojoba oil: capric acid triglyceride: isooctyl palmitate ratio is 4:5:1) and micelles-coated Fullerene complexes were compared in transdermal experiments. Drug permeability analysis was performed by LC-MS.

The results show that after 6 hours, the fullerene composition has a transmittance of 80%, and the compound coated with micelles has a transmittance of only 20%.

Conclusion: the fullerene-containing composition of the present invention is bright purple, wherein fullerene is in a dissolved state, and the obtained fullerene-containing composition is stable in properties, can be used for any external formulation, and is very easy to penetrate the stratum corneum of the skin. It is easy to absorb and utilize, and the efficacy is easier to exert.

Embodiment 6: the preparation of oil-soluble auxiliary agent

Take fullerene powder and oil-soluble additives, mix their mixture evenly, put it into a micro-jet high-pressure homogenizer, homogenize it for 5 times at 200MPa, then control the temperature of the material at 15 degrees, stir for 12 hours, and centrifugally filter to obtain a combination thing.

Solubility of fullerenes in single excipients

The content of fullerene in the liquid phase calibration is 1 mg/ml, which shows that fullerene is effectively soluble in the above-mentioned ratio of oil-soluble additives.

Jojoba oil is a vegetable oil. Although it is much more stable than other vegetable oils such as olive oil and linseed oil, it still has a certain degree of instability. Caprylic Capric Triglyceride: A high-strength, odorless oil derived from palm oil or coconut oil, which is extracted using thermal fractionation. Due to its compatibility with human skin, it has a non-greasy texture, which can be added to creams or lotions to improve its extensibility, lubricate and soften the skin. And it has the function of filtering ultraviolet light. It is an extract from coconut and used as emollient and solvent in cosmetics. Isooctyl Palmitate: It has a certain transdermal property and is mild in nature. Comprehensively inspecting the above compositions with different ratios, it is found that under the ratio of jojoba oil: capric acid triglyceride: isooctyl palmitate 4:5:1, the stability of the composition is better, and the skin absorbability is better. Optimum, with a milder skin feel.

Embodiment 7: Whitening and Freckle Removing Effect

Experimental method: After the mice were anesthetized with 2.5% pentobarbital sodium, the model group was intramuscularly injected with 0.4% progesterone injection at a dose of 0.02 g/kg in the hind limbs of the mice, 6 times a week for 4 consecutive weeks. The normal group was injected intramuscularly with sterile water for injection at 0.02g/kg. Take 60 healthy female mice, 3 dosage groups, and divide them into 6 groups randomly, 10 in each group. Normal group, model group, and a group of fullerene compositions (in which jojoba oil: caprylic triglyceride: isooctyl palmitate is 4:5:1) externally applied 3 dosage groups (0.10, 0.20, 0.40 mg/ml)), 3% hydroquinone positive control group (0.69mg/ml). A group of 3 doses of the treatment group were administered externally on the skin of mice on the day of modeling, once a day, for 30 consecutive days. The normal group and the model group were given local application of distilled water at the corresponding time; the 3% hydroquinone positive drug control group started topical application on the day of modeling, and the time and course of treatment were the same as those of the fullerene group. After 30 days of administration, the mice were killed by cervical dislocation, and the hair on the back was removed. Two pieces of liver tissue and two pieces of skin tissue were quickly taken from the drug-applied site, one of which was washed with ice-cold normal saline to remove blood, blotted dry with filter paper, and the liver and skin were cut out. Put 0.5g each into a beaker of 2.0ml pre-cooled normal saline, cut the tissue into pieces, then pour it into a test tube, and homogenize twice with a high-speed disperser at 10r/min, each time for 10 seconds; then at a speed of 3500r/rain Centrifuge for 15 minutes and take the supernatant for testing.

Result: Table 2 below

Table 2

Conclusion: As shown in Table 2 above, the normal group is without modeling, the model group is treated with drugs after modeling, and the positive group is hydroquinone, which is known to have excellent whitening effects. After successful modeling, the number of melanocytes in the model group increased significantly, the number of dermal inflammatory cells increased, and the number of dermal blood vessels decreased. Compared with the low, medium, and high administration groups, the number of melanocytes and dermal inflammatory cells were significantly higher than those in the model group. Low, the number of dermal blood vessels increased significantly, indicating that both have a certain whitening effect, and there is a certain concentration-dependent relationship. The composition of the invention has remarkable effects on the model group and the positive control group, and the composition of the invention has the effect of whitening and removing spots.

Example 8: anti-oxidation and anti-wrinkle

Experimental method: 6-week-old nude mice were used in the experiment, and were divided into two groups, 10 in each group. The experimental group applied an oil-soluble fullerene composition (jojoba oil: capric acid triglyceride capric acid) to the back of the right ear of the nude mice. Esters: isooctyl palmitate (4:5:1), twice a day, about 0.5g each time, the control group did not administer. Under the conditions of clean, ventilated, dry, room temperature 22±2°C, the same feed was fed. After 60 days of medication, 8 rats were taken respectively, and after being killed by cervical dislocation, the skin of the drug-acting part and the corresponding part of the contralateral side were taken for detection. Observe the effect of the water-soluble fullerene external composition in the experimental group for 60 days on the ratio of skin collagen to the area of the dermis. Result: See Table 3, after 60 days, the composition of the present invention has a significant effect on the increase of dermis collagen.

Table 3 The influence of oil-soluble fullerene composition for external application on skin collagen accounted for dermis layer area ratio

Example 9: Evaluation of the effect of the fullerene composition formulation of the present invention on human body for external use

The composition is added into conventional emulsion to prepare a new emulsion product.

Anti-acne experiment: Gender randomized, 20 subjects aged 18-55 with mild, moderate and severe facial acne, used the product for 14 days, the results are shown in Figures 2 and 3.

Fade fine line experiment: 20 women aged 35-55, with obvious wrinkles at the corners of the eyes, use the product for 30 days

Skin color improvement experiment: 20 women aged 35-55 with dull complexion used the face cream containing 3% fullerene of this patented ingredient for 4 consecutive weeks, once a day in the morning and evening. Data were obtained through questionnaire survey and photo analysis. It can be seen that the face cream added with 3% fullerene has obvious skin brightening and whitening effects. The result is shown in Figure 4

Spot lightening experiment: 20 women aged 35-55, with light brown spots locally, used the product for 30 days

Anti-hair loss experiment: People with hair loss problems, regardless of gender, use the product for 30 days

Anti-smog effect: the patented fullerene composition (wherein jojoba oil: caprylic triglyceride: isooctyl palmitate is 4:5:1) was used to treat skin explants for 5 days, and then exposed to pollution Environment. The result shows that the state of the skin cells treated with the ingredients of this patent has almost no difference from the blank group. The skin damaged by haze showed a significant increase in damaged cells, the results are shown in Figure 5.

result:

group Acne fine line changes skin tone improvement Blemish hair loss prevention 80% 65% 70% 50% 60%

Conclusion: the fullerene composition of the present invention has a cosmetic effect, can remove acne, eliminate fine lines, and improve the effect of skin lightening.

In summary the beneficial effects of the present invention

1. The fullerene in the fullerene-containing composition of the present invention is in molecular state, and the particle size is small, so it is easier to release in the formulation and then be absorbed and utilized.

2. The preparation method of the fullerene-containing composition of the present invention is simple and easy, and is suitable for mass production.

3. The fullerene-containing composition of the present invention has stable properties and is suitable for the preparation of any external formulation.

4. The fullerene-containing composition of the present invention has the functions of whitening, freckle removing and wrinkle removing.

Claims (10)

1. A fullerene composition comprising an oil-soluble additive and fullerene dissolved or dispersed in the oil-soluble additive. 2. A fullerene dispersion system, said system contains fullerene and oil-soluble additives, characterized in that more than 50% of said dispersion system, such as 60%, 70%, 80%, 90%, 95% , More than 99% of the particle size is less than 5nm. 3. Composition or dispersion according to any one of the preceding claims, characterized in that, in addition to oil solubility aids and fullerenes, at least one antioxidant is present. 4. Composition or dispersion according to any one of the preceding claims, characterized in that, in addition to the oil solubility assistant and the fullerenes, it contains at least one further active ingredient. 5. Composition or dispersion according to any one of the preceding claims, characterized in that the composition or dispersion can be incorporated into cosmetic or pharmaceutical delivery systems and/or sustained release systems. 6. A preparation method of a fullerene composition or a dispersion system and a preparation product thereof, characterized in that, the method comprises the steps of: taking fullerene powder and an oil-soluble auxiliary agent, after mixing uniformly, passing through a high-pressure homogenization After mechanical treatment, centrifuge and/or filter to obtain the product; optionally, the high-pressure homogenizer is homogenized at 50-500MPa, preferably 100-300MPa, more preferably 200MPa for 1-10 times, preferably 3-8 times, and more preferably 5 times, and then control the material temperature at 0-25°C, preferably 5-20°C, more preferably 10-15°C, and stir for 1-20h, preferably 5-15h, more preferably 12h. 7. The composition or dispersion system or method according to any one of the preceding claims, wherein the oil-soluble auxiliary agent is selected from the group consisting of: jojoba oil, capric triglyceride, isooctyl palmitate, isopropyl palmitate , Myristyl Myristate, Cocoyl Caprylate/Caprate, Decyl Cocoate, Methyl Cocoate, Isodecyl Cocoate, Stearyl Behenate, Stearin At least one of alcohol citrate, stearyl lactate, stearyl caprylate, stearyl palmitate, fish oil glycerin mixed esters, sucrose polyoleate, preferably jojoba oil, caprylic acid At least one of capric triglyceride, isooctyl palmitate, isopropyl palmitate, and myristyl myristate, more preferably, the oil-soluble auxiliary agent is jojoba oil, capric glycerin caprylate At least one of triesters, isooctyl palmitate, most preferably, the oil-soluble auxiliary agent is jojoba oil, caprylic triglyceride, isooctyl palmitate, and its mass proportion is (1 -7):(1-7):(1-7), for example, 7:2:1, 5:4:1, 3:6:1, 6:1:3, 4:1:5, 2: 1:7, 4:5:1, preferably 4:5:1. 8. The composition or dispersion system or method according to any one of the preceding claims, wherein the fullerene is at least one of a hollow fullerene, a metal fullerene, a heterocyclic fullerene and an endofullerene , including but not limited to fullerenes C _2n , M@C _2n , M ₂ @C _2n , MA@C _2n , M ₃ N@C _2n , M ₂ C ₂ @C _2n , M ₂ S@C _2n , M Any one of ₂ O@C _2n and M _x A _3-x N@C _2n or a mixture thereof, wherein M and A are metal elements, and both M and A are selected from Sc, Y and lanthanide metals Any one of the elements; 30≤n≤60; 0≤x≤3, preferably, the fullerene is any one of C60, C70, C76, C84, Gd@C82 and its derivatives or mixture, further preferably, the fullerene is C60. 9. Use of the composition or dispersion system according to any one of the preceding claims in the preparation of cosmetic or cosmetic products, optionally, said cosmetic or cosmetic products are used for whitening, anti-wrinkle, anti-acne, anti-haze or hair growth fixation Hair at least one. 10. Use of the composition or dispersion system according to any one of the preceding claims in the preparation of an instrument for beauty or make-up, optionally, the beauty or cosmetic product is used for whitening and anti-freckle, anti-wrinkle, anti-acne, anti-haze Or at least one of hair growth and fixation.