Component for effectively promoting skin permeation and preparation method and application thereof

Abstract

The invention discloses a component for effectively promoting skin penetration and a preparation method and application thereof, the component is composed of phospholipid, glycerol glucoside and sodium hyaluronate with low molecular weight, the molecular weight of the sodium hyaluronate is within 10000 Da, and the mass ratio of the phospholipid to the glycerol glucoside to the sodium hyaluronate is 5: (2-5): 1. Through component selection and optimized proportioning, the permeation efficiency of active substances passing through a skin barrier is remarkably improved. Wherein the phospholipid can enhance the compatibility with lipid between skin cells; glycerol glucoside can promote generation of skin aquaporin and strengthen skin deep hydration. The sodium hyaluronate with low molecular weight realizes efficient release of active matters in the deep layer of the skin with excellent permeability and moisturizing performance. The invention is widely applicable to the field of cosmetics, and can effectively improve the absorption efficiency of the product. In addition, the preparation process is simple, mild and safe, and has a wide commercial application prospect.

Description

Technical Field

[0001] The invention relates to the technical field of cosmetics, and in particular to an ingredient that effectively promotes skin penetration, a preparation method and application thereof. Background Art

[0002] In the research of modern skin care products, improving skin permeability has always been an important topic. Due to the complex structure and barrier function of the skin, many active ingredients are difficult to penetrate into the deep layers of the skin, affecting their effects. Therefore, how to improve the skin's ability to penetrate external ingredients has become a technical challenge in the research and development of cosmetics and drugs.

[0003] Traditional penetration enhancement technologies mainly rely on chemical penetration enhancers, physical penetration methods (such as ultrasound, electroporation, etc.) and nanotechnology (such as liposomes, nanoemulsions, etc.). Although these methods have improved the penetration efficiency to a certain extent, they may have problems such as safety, stability or comfort, making them difficult to be widely used. For example, chemical penetration enhancers may damage the skin barrier, causing dryness or allergies; physical penetration methods may cause discomfort and require professional equipment; and although liposomes and nanoemulsions can improve permeability, their formulations and processes are relatively demanding and may be unstable.

[0004] Therefore, developing a safe, effective, and stable penetration-promoting ingredient that can improve permeability without damaging the skin barrier has become an urgent issue to be addressed. Summary of the invention

[0005] The purpose of the present invention is to provide an ingredient that effectively promotes skin penetration, a preparation method and an application thereof. The core ingredients are composed of phospholipids, glyceryl glucoside and low molecular weight sodium hyaluronate. After optimizing the ratio and ingredient selection, the penetration ability of active substances in the skin barrier is significantly improved, which well solves the problems of low penetration efficiency and skin barrier damage in the prior art.

[0006] In order to achieve the above object, the present invention adopts the following technical solutions:

[0007] In a first aspect, the present invention provides an ingredient that effectively promotes skin penetration, which is composed of phospholipids, glyceryl glucoside and low molecular weight sodium hyaluronate, wherein the molecular weight of the sodium hyaluronate is within 10,000 Da, and the mass ratio of the phospholipids, the glyceryl glucoside and the sodium hyaluronate is 5:(2-5):1.

[0008] The ingredients for effectively promoting skin penetration provided by the present invention are composed of phospholipids, glyceryl glucoside and low molecular weight sodium hyaluronate, which significantly improve the penetration efficiency of active ingredients without damaging the skin barrier through synergistic effects. Specifically, the synergistic mechanism of phospholipids, glyceryl glucoside and sodium hyaluronate is:

[0009] (1) Barrier adjustment and channel creation: phospholipids loosen the intercellular lipid structure and enhance the compatibility of the skin with glyceryl glucoside and sodium hyaluronate;

[0010] (2) Improvement of water environment: Glyceryl glucoside optimizes the water flow in the skin and improves skin permeability by promoting the production of aquaporins;

[0011] (3) Deep release and repair: Low molecular weight sodium hyaluronate accelerates the release of active ingredients deep into the skin with its strong penetration ability and moisturizing properties, while protecting and repairing the skin barrier.

[0012] (4) By combining phospholipids, glyceryl glucoside and low molecular weight sodium hyaluronate in a specific ratio, a highly efficient and synergistic permeation-enhancing system is formed, which significantly improves the absorption efficiency of active ingredients while maintaining the health of the skin.

[0013] As an example, the mass ratio of phospholipids, glyceryl glucoside and sodium hyaluronate can be set to 5:2:1 or 5:5:1; of course, the mass ratio of phospholipids, glyceryl glucoside and sodium hyaluronate can also be adjusted to 5:2.5:1 or 5:3:1 or 5:3.3:1 or 5:3.5:1 or 5:4:1 or 5:4.5:1 as needed. The above ratios constitute the ingredients that effectively promote skin penetration, which significantly improve the penetration ability of active substances in the skin barrier.

[0014] Furthermore, the molecular weight of the sodium hyaluronate is 500Da to 10000Da. This configuration allows low molecular weight sodium hyaluronate to have excellent penetration ability, easily penetrate the stratum corneum, penetrate into the dermis, and provide deep moisturizing and barrier repair functions for the skin. The specific features are as follows:

[0015] (1) Deep release of active ingredients: Accurately release other active ingredients deep in the skin and improve their even distribution.

[0016] (2) Enhance skin elasticity: Low molecular weight sodium hyaluronate has strong hygroscopic properties, which can help maintain long-term skin hydration and improve skin elasticity.

[0017] As an example, the molecular weight of sodium hyaluronate is 800 Da to 1000 Da.

[0018] Furthermore, the phospholipid includes at least one of hydrogenated lecithin, phosphatidylcholine and phosphatidylcholine.

[0019] Preferably, the phospholipid is hydrogenated lecithin containing more than 70% hydrogenated phosphatidylcholine, which can form a stable lipid film on the skin surface. Its special structure enhances the compatibility with the lipids in the stratum corneum of the skin, effectively loosens the intercellular gaps, and at the same time improves the stability of the skin barrier, providing a channel for the penetration of other ingredients.

[0020] Furthermore, the glyceryl glucoside is extracted from desert algae that has been optimized through space breeding. The growth rate and active ingredient content of desert algae are improved through gene mutation. The glyceryl glucoside extracted from this type of desert algae has significant penetration-promoting properties. The specific unique advantages are as follows:

[0021] (1) Promote the production of aquaporin: Glyceryl glucoside can effectively activate the production of aquaporin (AQP) and enhance the water transfer efficiency of the skin.

[0022] (2) High stability: The desert algae optimized through space breeding have been endowed with higher purity and biological activity of glyceryl glucoside, making its structure more stable and having excellent stress resistance.

[0023] (3) Mechanism of action: Glyceryl glucoside improves the water environment inside and outside skin cells, reduces skin barrier resistance, enables other active substances to penetrate deeper into the skin more efficiently, and improves skin hydration.

[0024] Furthermore, the preparation method of glyceryl glucoside comprises the following steps: grinding, ultrasonic extraction, centrifugation, reduced pressure evaporation concentration, separation and elution, ultrafiltration purification and cooling-induced crystallization.

[0025] Specifically, the preparation method of glyceryl glucoside comprises the following steps:

[0026] (1) Grinding: Freeze and grind the space-grown desert algae to break the cell walls and release the cell contents to obtain desert algae powder;

[0027] (2) Ultrasonic extraction: first, the desert algae powder obtained in step (1) is mixed with an ethanol solution at a mass ratio of 1:10, wherein the ethanol content in the ethanol solution is 70% to 80%, to obtain a mixed solution; then, the mixed solution is placed in an ultrasonic assisted extraction device for ultrasonic extraction to improve the extraction efficiency, the ultrasonic extraction temperature is set to 30° C. to 40° C., the ultrasonic frequency is 30 kHz, and the extraction is performed for 30 min; the ultrasonic extraction is repeated 3 times to ensure that the glycerol glucoside is completely extracted, and each time the extract is filtered and replaced with a fresh ethanol solution and the filter residue for re-ultrasonic extraction, and the filtered extract is collected;

[0028] (3) Centrifugation: The extract obtained in step (2) is placed in a centrifuge and centrifuged at a speed of 3000 rpm to 10000 rpm for 10 min to remove insoluble impurities and obtain a clarified extract;

[0029] (4) Concentrating by evaporation under reduced pressure: placing the extract after treatment in step (3) in a reduced pressure evaporation device and concentrating at a temperature below 40° C. until the volume of the solution is reduced to 1 / 5 of the original volume, thereby obtaining a concentrated solution; this step helps to remove ethanol and retain the active ingredient of glyceryl glucoside;

[0030] (5) separation and elution: the concentrated solution obtained in step (4) is separated by C18 reverse phase silica gel column chromatography, and gradient elution is performed using pure water, 30% ethanol, 50% ethanol, 70% ethanol and 100% ethanol in turn for elution in separate tubes or bottles, and the eluate containing glycerol glucoside is collected;

[0031] (6) ultrafiltration purification: the eluate obtained in step (5) is placed in an ultrafiltration membrane system with a molecular weight cutoff value of 3000 Da for filtration to remove small molecular impurities and obtain a purified glycerol glucoside solution;

[0032] (7) Cooling to induce crystallization: Finally, the glycerol glucoside solution after ultrafiltration purification in step (6) is cooled to 4°C and allowed to stand for 24 to 48 hours to induce crystallization of glycerol glucoside to obtain high-purity powdered glycerol glucoside. The purity of glycerol glucoside is analyzed by high performance liquid chromatography (HPLC), and the purity reaches more than 95%.

[0033] Furthermore, the desert algae include at least one of Chlorella vulgaris, Microcystis sp., Hasa algae and Cyanobacteria.

[0034] Preferably, the desert algae is Hasa algae.

[0035] In a second aspect, the present invention provides an application of the above-mentioned ingredient that effectively promotes skin penetration, which is applied to the preparation of cosmetics, wherein the added amount of the ingredient that effectively promotes skin penetration is 0.1wt% to 20wt%, and the dosage form of the cosmetics is any one of an aqueous solution, an emulsion, a cream or a gel.

[0036] In a third aspect, the present invention provides a cosmetic comprising ingredients that effectively promote skin penetration, the cosmetic comprising phase A and phase B, wherein phase B comprises at least one of a preservative, a skin conditioner, an antioxidant, and a pH adjuster, and phase A comprises water, the above-mentioned ingredients that effectively promote skin penetration, and at least one of a thickener, a moisturizer, an emollient, a chelating agent, and an emulsifier.

[0037] Preferably, the skin conditioning agent is selected from at least one of niacinamide, collagen, astaxanthin, vitamin C and its derivatives, peptides, and amino acids.

[0038] Preferably, the pH regulator is selected from at least one of arginine, sodium hydroxide, potassium hydroxide, triethanolamine and aminomethyl propanol.

[0039] Preferably, the antioxidant is selected from at least one of vitamin E and its derivatives, ubiquinone and fullerene.

[0040] Preferably, the preservative is selected from at least one of phenoxyethanol, p-hydroxyacetophenone, sodium benzoate, phenoxyethanol, methylparaben, caprylhydroxamic acid, and chlorphenesin.

[0041] Preferably, the moisturizer is selected from at least one of glycerin, 1,3-propylene glycol, butylene glycol, dipropylene glycol, pentylene glycol, sorbitol, erythritol, 1,2-hexanediol, glyceryl polyether-26, and caprylyl glycol.

[0042] Preferably, the thickener is selected from at least one of xanthan gum, acrylic acid (esters) / C10-30 alkyl acrylate cross-linked polymer, carbomer, ammonium acryloyldimethyltaurate / VP copolymer, and sodium acrylate / sodium acryloyldimethyltaurate copolymer.

[0043] Preferably, the chelating agent is selected from at least one of disodium EDTA, tetrasodium EDTA and sodium phytate.

[0044] Preferably, the emulsifier is selected from at least one of PEG-100 stearate, polyglyceryl-3 methyl glucose distearate, potassium cetyl phosphate, cetearyl glucoside, cetearyl olivetate, sodium methyl stearoyl taurate, sodium methyl stearoyl taurate, hydrogenated lecithin, sorbitan olivate, and polyglyceryl-3 distearate.

[0045] Preferably, the emollient is selected from at least one of tri(ethylhexanoin)glyceryl, caprylic / capric triglyceride, pentaerythritol tetra(ethylhexanoin), isononyl isononanoate, hydrogenated polyisobutene, butyloctanol salicylate, diethoxyethyl succinate, isododecane, rice germ oil, hydrogenated palm kernel oil, cocoa butter cetyl ethylhexanoate, isopropyl myristate, isopropyl palmitate, diisopropyl sebacate, polydimethylsiloxane, cetearyl alcohol, dibutyl adipate, C12-15 alcohol benzoate, dicaprylyl carbonate, coconut oil alcohol-caprylate / caprate, polydimethylsiloxane, caprylyl polymethylsiloxane, cyclopentasiloxane, and phenyl trimethicone.

[0046] Furthermore, in terms of weight percentage, the cosmetic comprises a phase A and a phase B, wherein the phase B comprises 0.01wt% to 3wt% of a preservative, 0 to 10wt% of an antioxidant, 0 to 3wt% of a pH adjuster and 0 to 20wt% of a skin conditioner, and the phase A comprises 0 to 20wt% of an emulsifier, 0 to 1wt% of a chelating agent, 0.1wt% to 20wt% of an ingredient that effectively promotes skin penetration, 0.01wt% to 8wt% of a thickener, 0.01wt% to 40wt% of a moisturizer, 0 to 50wt% of an emollient and the remainder being water.

[0047] As an example, by weight percentage, the cosmetic includes phase A and phase B, wherein phase B includes 0.01-3wt% of a preservative and 0-20wt% of a skin conditioner, and phase A includes 0.1-20wt% of an ingredient that effectively promotes skin penetration, 0.01%-8wt% of a thickener, 0.01%-40wt% of a moisturizer, 0-50wt% of an emollient, and the remainder is water.

[0048] Specifically, by weight percentage, the cosmetic includes 0.16wt% to 17.6wt% of ingredients that effectively promote skin penetration, 5wt% of moisturizer, 5wt% of emollient, 0.5wt% of thickener, 1wt% of skin conditioner, 0.5wt% of preservative and the balance of water.

[0049] More specifically, based on 100 parts, the cosmetic includes phase A and phase B, phase B includes 0.5 parts of a preservative and 1 part of a skin conditioner, phase A includes 0.16 to 17.6 parts of an ingredient that effectively promotes skin penetration, 0.5 parts of a thickener, 5 parts of a humectant, 5 parts of an emollient, and the remainder is water; wherein the preservative is phenoxyethanol, the skin conditioner is niacinamide, the thickener is ammonium acryloyldimethyltaurate / VP copolymer, the humectant is glycerin, and the emollient is caprylic / capric triglyceride.

[0050] In a fourth aspect, the present invention further provides a method for preparing the above-mentioned cosmetics containing ingredients that effectively promote skin penetration, comprising the following steps:

[0051] S1. Weigh the cosmetic raw material phase A component and phase B component respectively;

[0052] S2. Add the components of phase A into an emulsifying pot, mix and heat to 75°C to 85°C, stir homogenously at a stirring speed of 3000r / min for 10min, and keep stirring for 10min to 20min;

[0053] S3. Stir and cool to below 45°C, add phase B components, stir homogenously at a speed of 3000r / min for 2min to 5min, and discharge.

[0054] Compared with the prior art, the present invention provides a component that effectively promotes skin penetration, a preparation method and application thereof, and has the following beneficial effects:

[0055] The present invention uses phospholipids, glyceryl glucoside and low molecular weight sodium hyaluronate as core ingredients, and after optimizing the ratio and ingredient selection, significantly improves the penetration efficiency of active substances through the skin barrier. Among them, phospholipids can enhance the compatibility with lipids between skin cells; glyceryl glucoside can promote the production of skin water channel proteins and strengthen the hydration of deep skin layers; low molecular weight sodium hyaluronate has excellent permeability and moisturizing properties, and realizes the efficient release of active substances in the deep layers of the skin.

[0056] The invention is widely applicable to the field of cosmetics and can effectively improve the absorption efficiency of products.

[0057] In addition, the preparation process of the present invention is simple, mild and safe, and has broad commercial application prospects. DETAILED DESCRIPTION

[0058] The technical solution of the present invention will be described clearly and completely below. Obviously, the described embodiments are only part of the embodiments of the present invention, not all of the embodiments. Based on the embodiments of the present invention, all other embodiments obtained by ordinary technicians in this field without creative work are within the scope of protection of the present invention.

[0059] In the embodiments and comparative examples, the experimental methods used are all conventional methods unless otherwise specified. If no specific conditions are specified, the operations can be carried out according to conventional conditions or conditions recommended by the manufacturer. The materials, reagents or instruments used are all conventional commercial products and can be obtained from commercial channels unless otherwise specified.

[0060] The present invention is further described in detail below through detailed examples.

[0061] Example 1

[0062] This embodiment provides an ingredient that effectively promotes skin penetration, including 0.1 parts of phospholipids, 0.04 parts of glyceryl glucoside, and 0.02 parts of low molecular weight sodium hyaluronate.

[0063] The molecular weight of sodium hyaluronate is 800Da-1000Da, the phospholipid is hydrogenated lecithin containing more than 70% hydrogenated phosphatidylcholine, and both hydrogenated lecithin and sodium hyaluronate are commercially available products.

[0064] Glycerol glucoside is prepared by extracting desert algae bred in space, which is also a commercially available product. The specific preparation method of glycerol glucoside includes the following steps:

[0065] (1) Grinding: Freeze and grind the space-grown desert algae (using Hasa algae) to break the cell walls and release the cell contents to obtain desert algae powder;

[0066] (2) Ultrasonic extraction: first, the desert algae powder obtained in step (1) is mixed with an ethanol solution in a mass ratio of 1:10, wherein the ethanol content in the ethanol solution is 75%, to obtain a mixed solution; then, the mixed solution is placed in an ultrasonic assisted extraction device for ultrasonic extraction to improve the extraction efficiency, the ultrasonic extraction temperature is set to 35° C., the ultrasonic frequency is 30 kHz, and the extraction is performed for 30 min; the ultrasonic extraction is repeated 3 times to ensure that the glycerol glucoside is completely extracted, and each time the extract is filtered and replaced with a fresh ethanol solution and the filter residue, and then re-mixed with the ultrasonic extraction, and the filtered extract is collected;

[0067] (3) Centrifugation: The extract obtained in step (2) is placed in a centrifuge and centrifuged at 8000 rpm for 10 min to remove insoluble impurities and obtain a clarified extract;

[0068] (4) Concentrating by evaporation under reduced pressure: placing the extract after treatment in step (3) in a reduced pressure evaporation device and concentrating at a temperature below 40° C. until the volume of the solution is reduced to 1 / 5 of the original volume, thereby obtaining a concentrated solution; this step helps to remove ethanol and retain the active ingredient of glyceryl glucoside;

[0069] (5) separation and elution: the concentrated solution obtained in step (4) is separated by C18 reverse phase silica gel column chromatography, and gradient elution is performed using pure water, 30% ethanol, 50% ethanol, 70% ethanol and 100% ethanol in turn for elution in separate tubes or bottles, and the eluate containing glycerol glucoside is collected;

[0070] (6) ultrafiltration purification: the eluate obtained in step (5) is placed in an ultrafiltration membrane system with a molecular weight cutoff value of 3000 Da for filtration to remove small molecular impurities and obtain a purified glycerol glucoside solution;

[0071] (7) Cooling to induce crystallization: Finally, the glycerol glucoside solution after ultrafiltration purification in step (6) is cooled to 4°C and allowed to stand for 48 hours to induce crystallization of glycerol glucoside to obtain high-purity powdered glycerol glucoside. The purity of glycerol glucoside is analyzed by high performance liquid chromatography (HPLC), and the purity reaches more than 95%.

[0072] Example 2

[0073] This embodiment provides an ingredient that effectively promotes skin penetration, including 0.3 parts of phospholipids, 0.15 parts of glyceryl glucoside, and 0.06 parts of low molecular weight sodium hyaluronate.

[0074] The selection of sodium hyaluronate, phospholipids and glyceryl glucoside is the same as that in Example 1. Compared with Example 1, only the dosage of the components is changed.

[0075] Example 3

[0076] This embodiment provides an ingredient that effectively promotes skin penetration, including 0.5 parts of phospholipids, 0.3 parts of glyceryl glucoside, and 0.1 parts of low molecular weight sodium hyaluronate.

[0077] The selection of sodium hyaluronate, phospholipids and glyceryl glucoside is the same as that in Example 1. Compared with Example 1, only the dosage of the components is changed.

[0078] Example 4

[0079] This embodiment provides an ingredient that effectively promotes skin penetration, including 1 part of phospholipids, 0.66 parts of glyceryl glucoside, and 0.2 parts of low molecular weight sodium hyaluronate.

[0080] The selection of sodium hyaluronate, phospholipids and glyceryl glucoside is the same as that in Example 1. Compared with Example 1, only the dosage of the components is changed.

[0081] Example 5

[0082] This embodiment provides an ingredient that effectively promotes skin penetration, including 1.5 parts of phospholipids, 1.05 parts of glyceryl glucoside and 0.3 parts of low molecular weight sodium hyaluronate.

[0083] The selection of sodium hyaluronate, phospholipids and glyceryl glucoside is the same as that in Example 1. Compared with Example 1, only the dosage of the components is changed.

[0084] Example 6

[0085] This embodiment provides an ingredient that effectively promotes skin penetration, including 3 parts of phospholipids, 2.4 parts of glyceryl glucoside and 0.6 parts of low molecular weight sodium hyaluronate.

[0086] The selection of sodium hyaluronate, phospholipids and glyceryl glucoside is the same as that in Example 1. Compared with Example 1, only the dosage of the components is changed.

[0087] Example 7

[0088] This embodiment provides an ingredient that effectively promotes skin penetration, including 5 parts of phospholipids, 4.5 parts of glyceryl glucoside and 1 part of low molecular weight sodium hyaluronate.

[0089] The selection of sodium hyaluronate, phospholipids and glyceryl glucoside is the same as that in Example 1. Compared with Example 1, only the dosage of the components is changed.

[0090] Example 8

[0091] This embodiment provides an ingredient that effectively promotes skin penetration, including 8 parts of phospholipids, 8 parts of glyceryl glucoside and 1.6 parts of low molecular weight sodium hyaluronate.

[0092] The selection of sodium hyaluronate, phospholipids and glyceryl glucoside is the same as that in Example 1. Compared with Example 1, only the dosage of the components is changed.

[0093] Comparative Example 1

[0094] This comparative example provides a composition comprising 0.5 parts of phospholipids.

[0095] The selection of phospholipids is the same as that in Example 3. Compared with Example 3, glyceryl glucoside and low molecular weight sodium hyaluronate are not contained.

[0096] Comparative Example 2

[0097] This comparative example provides a component including 0.3 parts of glyceryl glucoside.

[0098] The selection of glyceryl glucoside is the same as that in Example 3. Compared with Example 3, phospholipids and low molecular weight sodium hyaluronate are not contained.

[0099] Comparative Example 3

[0100] This comparative example provides a composition including 0.1 parts of low molecular weight sodium hyaluronate.

[0101] The selection of sodium hyaluronate is the same as that in Example 3, but compared with Example 3, it does not contain phospholipids and glyceryl glucoside.

[0102] Comparative Example 4

[0103] This comparative example provides a composition comprising 0.5 parts of phospholipids and 0.3 parts of glyceryl glucoside.

[0104] The selection of phospholipids and glyceryl glucoside is the same as that in Example 3. Compared with Example 3, low molecular weight sodium hyaluronate is not contained.

[0105] Comparative Example 5

[0106] This comparative example provides a composition comprising 0.5 parts of phospholipids and 0.1 parts of low molecular weight sodium hyaluronate.

[0107] The selection of phospholipids and sodium hyaluronate is the same as that in Example 3. Compared with Example 3, glyceryl glucoside is not contained.

[0108] Comparative Example 6

[0109] This comparative example provides a component including 0.3 parts of glyceryl glucoside and 0.1 parts of low molecular weight sodium hyaluronate.

[0110] The selection of glyceryl glucoside and sodium hyaluronate is the same as that in Example 3. Compared with Example 3, phospholipids are not contained.

[0111] Comparative Example 7

[0112] This comparative example provides a composition comprising 0.5 parts of phospholipids, 0.3 parts of glyceryl glucoside and 0.1 parts of sodium hyaluronate.

[0113] The difference from Example 3 is that the phospholipid is lecithin, the glyceryl glucoside is chemically synthesized, and the molecular weight of sodium hyaluronate is greater than 1 million Da, and all three are purchased from conventional raw material manufacturers.

[0114] Comparative Example 8

[0115] This comparative example provides a composition including 0.5 parts of polysorbate-20.

[0116] Wherein, polysorbate-20 is purchased from conventional raw material manufacturers.

[0117] Comparative Example 9

[0118] This comparative example provides a component including 0.3 parts of glyceryl glucoside.

[0119] The difference from Example 3 is that phospholipids and low molecular weight sodium hyaluronate are not contained, and the glyceryl glucoside used is chemically synthesized and can be purchased from conventional raw material manufacturers.

[0120] 1. Preparation of cosmetics

[0121] The ingredients prepared in the above Examples 1 to 8 and Comparative Examples 1 to 9 were respectively used to prepare cosmetics according to the following methods to obtain cosmetics 1 to 17; at the same time, a blank control group (not containing the ingredients prepared in Examples 1 to 8 and Comparative Examples 1 to 9, and replaced with a corresponding amount of deionized water) was set up separately to obtain cosmetic 18.

[0122] 1.1. Formula composition of cosmetics

[0123] The cosmetic (based on 100 parts) includes phase A and phase B, specifically,

[0124] Phase B includes 0.5 part of preservative and 1 part of skin conditioner;

[0125] Phase A comprises 0.5 parts of thickener, 5 parts of moisturizer, 5 parts of emollient, the ingredients prepared in any one of Examples 1 to 8 and Comparative Examples 1 to 9, and the balance of water;

[0126] Among them, the preservative is phenoxyethanol, the skin conditioning agent is niacinamide, the thickener is ammonium acryloyldimethyltaurate / VP copolymer, the moisturizer is glycerin, and the emollient is caprylic / capric triglyceride.

[0127] 1.2. Preparation process of cosmetics

[0128] The preparation method of the cosmetic comprises the following steps:

[0129] S1. Weigh the cosmetic raw material phase A component and phase B component respectively;

[0130] S2. Put the components of phase A into the emulsifying pot, mix and heat to 85°C, stir homogenously at a stirring speed of 3000r / min for 10 minutes, and keep stirring for 10 minutes;

[0131] S3, stirring and cooling to below 45°C, adding phase B components, stirring homogenously at a speed of 3000r / min for 5 minutes, and discharging. The particle diameter of the effective penetration cosmetics is less than 200n.

[0132] 2. Experimental test: Transdermal penetration test

[0133] 1. Test Purpose

[0134] This test used piglet back skin to conduct Franz diffusion cell permeability experiments on niacinamide in samples (cosmetics 1 to 18). The penetration ability of the samples was examined by measuring the cumulative penetration amount of niacinamide in the receiving chamber at different time periods, and the absorption-promoting ability of the penetration-promoting essence was evaluated.

[0135] 2. Test materials and test samples

[0136] 2.1 Test model and test system

[0137] In this test, the back skin of a one-month-old suckling pig was selected as the test model, and the suckling pig skin-Franzcel system was selected as the test system. The cosmetics 1 to 18 prepared above were selected as test samples.

[0138] 2.2 Reagents

[0139] PBS buffer solution, phosphoric acid, acetonitrile.

[0140] 2.3 Equipment

[0141] TK-12D transdermal absorption diffusion instrument, Franz cell diffusion pool, high performance liquid chromatography, KO3200E ultrasonic cleaner, low temperature high speed centrifuge.

[0142] 3. Test steps

[0143] 3.1. Preparation of ex vivo suckling pig skin

[0144] The dorsal skin of suckling pig stored at -20°C was thawed with deionized water at room temperature and repeatedly rinsed with PBS buffer.

[0145] 3.2. Test of the penetration ability of active substances in vitro

[0146] (1) First, fix the skin between the donor chamber and the receiving chamber of the Franz cell diffusion tank, with the stratum corneum of the skin facing the donor chamber and the dermis facing the receiving chamber;

[0147] (2) Add 7.0 mL of receiving solution into the receiving chamber, tighten and fix the suckling pig skin, then add 1.5 mL of receiving solution (PBS) into the receiving chamber through a sampler, exhaust the air, and make the dermis layer of the skin in close contact with the receiving solution;

[0148] (3) Sample loading: Add the sample to the skin surface in the supply chamber. The effective penetration area S is about 3.14 cm 2 . Add the sample to the surface of the pig skin and spread the sample evenly from the center of the skin to the edge. Each sample was repeated 3 times in parallel (three replicates were made from skin from specific parts of independent donors);

[0149] (4) Infiltration: Turn on the electromagnetic stirrer and stir at a speed of 300 pm, maintain a constant temperature water bath of (32±1)°C, and ensure that there are no bubbles in the water bath interlayer;

[0150] (5) Take sample solution at 1 h, 2 h, 6 h, and 24 h respectively, use a sampler to extract 2.0 mL of receiving solution through the sampling tube, and then place it in a 2 mL EP tube. In addition, add an equal amount of receiving solution after each sampling.

[0151] 3.3. Transdermal content test

[0152] After 24 hours of penetration, HPLC was performed on the skin, in the skin and subcutaneously at each time point for different experimental groups.

[0153] 4. Detection method

[0154] After sampling, high performance liquid chromatography (HPLC) was used to detect the concentration of nicotinamide:

[0155] Chromatographic column: C18 reverse phase column.

[0156] Mobile phase: A (methanol 70 mL + isopropanol 20 mL): B (1 g sodium heptane sulfonate dissolved in 910 mL water, pH adjusted to 2.1±0.1 with perchloric acid) = 9:91.

[0157] Detection wavelength: characteristic absorption wavelength of nicotinamide (usually 262 nm).

[0158] 5. Statistics and analysis

[0159] 5.1. Penetration percentage

[0160] P = Q / Po × 100%, where: P is the penetration percentage, Q is the cumulative penetration amount of the sample in the receiving chamber at each time point, and Po is the theoretical content of the sample in the release pool.

[0161] 6. Test results

[0162] 6.1. Penetration percentage results

[0163] According to the calculation formula in 5.1, the permeability percentage of the sample at different time points is obtained. The results are shown in Table 1.

[0164] Table 1 Permeability results

[0165]

[0166] From the data in Table 1, the permeability of cosmetics 1 to 8 (i.e., corresponding to Examples 1 to 8) is much higher than that of cosmetics 9 to 18 (i.e., corresponding to Examples 1 to 8 and the blank control group), especially when the time is extended to 6h and 24h, the difference is more significant. As the proportion content of hydrogenated lecithin, glyceryl glucoside and low molecular weight sodium hyaluronate increases, the permeability of niacinamide gradually increases, which shows that the synergistic effect and the ratio of ingredients have a significant promoting effect on transdermal absorption. The permeability of cosmetics 9 to 17 (i.e., corresponding to Examples 1 to 9) has a limited increase, and has not significantly improved transdermal absorption, indicating that its permeability-promoting effect is insufficient. Cosmetic 8 (i.e., corresponding to Example 8) has the best performance, and the permeability is significantly better than other cosmetic samples at each time point, especially reaching 55.03% at 24 hours, which is the cosmetic sample with the best transdermal absorption effect.

[0167] From the data of cosmetics 15 to 17 (i.e. corresponding to Examples 7 to 9), the combination of lecithin, chemically synthesized glycerol glucoside, and high molecular weight sodium hyaluronate has a significantly lower penetration-enhancing effect than cosmetics 1 to 8 (i.e. corresponding to Examples 1 to 8). Chemically synthesized glycerol glucoside may have poor affinity with the skin due to its different structure and cannot significantly promote the transdermal absorption of nicotinamide. Although lecithin is used in cosmetics 15 (i.e. corresponding to Example 7), it cannot effectively form a dense skin-affinity lipid layer; high molecular weight sodium hyaluronate (usually with a molecular weight of >1000 kDa) is difficult to penetrate the stratum corneum due to its large molecular volume, and can only form a moisturizing effect on the surface, but cannot penetrate deep, and compared with low molecular weight sodium hyaluronate (within 10000Da), the penetration-enhancing effect is poor.

[0168] It can be seen that through the above raw material selection and ratio optimization setting, the present invention can significantly improve the penetration efficiency of active substances through the skin barrier.

[0169] The above embodiments are merely illustrative of the concept and technical solution of the present invention, and are not intended to limit the present invention. Anyone familiar with the technology may modify or change the above embodiments without violating the spirit and scope of the present invention. Therefore, all equivalent modifications or changes made by a person with ordinary knowledge in the technical field without departing from the spirit and technical ideas disclosed by the present invention should still be covered by the claims of the present invention.

[0170] In addition, it should be understood that although the present specification is described according to implementation modes, not every implementation mode contains only one independent technical solution. This narrative method of the specification is only for the sake of clarity. Those skilled in the art should regard the specification as a whole. The technical solutions in each implementation mode may also be appropriately combined to form other implementation modes that can be understood by those skilled in the art.

Claims

1. An ingredient that effectively promotes skin penetration, characterized in that: It is composed of phospholipids, glyceryl glucoside and low molecular weight sodium hyaluronate, the molecular weight of the sodium hyaluronate is within 10000Da, and the mass ratio of the phospholipids, the glyceryl glucoside and the sodium hyaluronate is 5:(2-5):

1.

2. The composition effective in promoting skin penetration according to claim 1, characterized in that: The molecular weight of the sodium hyaluronate is 500Da to 10000Da.

3. The composition effective in promoting skin penetration according to claim 1, characterized in that: The phospholipid includes at least one of hydrogenated lecithin, phosphatidylcholine and phosphatidylcholine.

4. The composition effective in promoting skin penetration according to claim 1, characterized in that: The glycerol glucoside is prepared by extracting desert algae optimized by space breeding. The preparation method of the glycerol glucoside comprises the following steps: grinding, ultrasonic extraction, centrifugation, reduced pressure evaporation concentration, separation elution, ultrafiltration purification and cooling-induced crystallization.

5. The composition effective in promoting skin penetration according to claim 4, characterized in that: The desert algae include at least one of Chlorella vulgaris, Microcystis sp., Hasa algae and Cyanobacteria.

6. A use of a component effective in promoting skin penetration as claimed in any one of claims 1 to 5, characterized in that: When applied to the preparation of cosmetics, the added amount of the component that effectively promotes skin penetration is 0.1wt% to 20wt%, and the dosage form of the cosmetics is any one of water, emulsion, cream or gel.

7. A cosmetic comprising an ingredient effective in promoting skin penetration, characterized in that: The cosmetic comprises a phase A and a phase B, wherein the phase B comprises at least one of a preservative, a skin conditioner, an antioxidant, and a pH adjuster, and the phase A comprises water, an ingredient effective in promoting skin penetration as recited in any one of claims 1 to 5, and at least one of a thickener, a moisturizer, an emollient, a chelating agent, and an emulsifier.

8. The cosmetic comprising an ingredient effective in promoting skin penetration according to claim 7, characterized in that: In terms of weight percentage, the cosmetic comprises a phase A and a phase B, wherein the phase B comprises 0.01wt% to 3wt% of a preservative, 0 to 10wt% of an antioxidant, 0 to 3wt% of a pH adjuster and 0 to 20wt% of a skin conditioner, and the phase A comprises 0 to 20wt% of an emulsifier, 0 to 1wt% of a chelating agent, 0.1wt% to 20wt% of an ingredient that effectively promotes skin penetration, 0.01wt% to 8wt% of a thickener, 0.01wt% to 40wt% of a moisturizer, 0 to 50wt% of an emollient and the remainder of water.

9. The cosmetic comprising an ingredient effective in promoting skin penetration according to claim 7, characterized in that: Include at least one of the following (1) to (9): (1) The skin conditioning agent is selected from at least one of niacinamide, collagen, astaxanthin, vitamin C and its derivatives, peptides, and amino acids; (2) the pH regulator is selected from at least one of arginine, sodium hydroxide, potassium hydroxide, triethanolamine, and aminomethyl propanol; (3) The antioxidant is selected from at least one of vitamin E and its derivatives, ubiquinone, and fullerene; (4) the preservative is at least one selected from phenoxyethanol, p-hydroxyacetophenone, sodium benzoate, phenoxyethanol, methylparaben, caprylhydroxamic acid, and chlorphenesin; (5) The moisturizing agent is at least one selected from glycerin, 1,3-propylene glycol, butylene glycol, dipropylene glycol, pentylene glycol, sorbitol, erythritol, 1,2-hexanediol, glyceryl polyether-26, and caprylyl glycol; (6) The thickener is at least one selected from xanthan gum, acrylic acid (ester) / C10-30 alkyl acrylate cross-linked polymer, carbomer, ammonium acryloyldimethyl taurate / VP copolymer, sodium acrylate / sodium acryloyldimethyl taurate copolymer; (7) The chelating agent is at least one selected from disodium EDTA, tetrasodium EDTA, and sodium phytate; (8) The emulsifier is at least one selected from PEG-100 stearate, polyglyceryl-3 methyl glucose distearate, potassium cetyl phosphate, cetearyl glucoside, cetearyl olivetate, sodium methyl stearoyl taurate, sodium methyl stearoyl taurate, hydrogenated lecithin, sorbitan olivate, and polyglyceryl-3 distearate; (9) The emollient is selected from at least one of tri(ethylhexanoin)glyceryl, caprylic / capric triglyceride, pentaerythritol tetra(ethylhexanoin), isononyl isononanoate, hydrogenated polyisobutene, butyloctyl salicylate, diethoxyethyl succinate, isododecane, rice germ oil, hydrogenated palm kernel oil, cocoa butter cetyl ethylhexanoate, isopropyl myristate, isopropyl palmitate, diisopropyl sebacate, polydimethylsiloxane, cetearyl alcohol, dibutyl adipate, C12-15 alcohol benzoate, dicaprylyl carbonate, coconut oil caprylate / caprate, polydimethylsiloxane, caprylyl polymethicone, cyclopentasiloxane, and phenyl trimethicone.

10. A method for preparing a cosmetic comprising an ingredient effective in promoting skin penetration as claimed in claim 7, characterized in that: The following steps are involved: S1. Weigh the cosmetic raw material phase A component and phase B component respectively; S2. Add the components of phase A into an emulsifying pot, mix and heat to 75°C to 85°C, stir homogenously at a stirring speed of 3000r / min for 10min, and keep stirring for 10min to 20min; S3. Stir and cool to below 45°C, add phase B components, stir homogenously at a speed of 3000r / min for 2min to 5min, and discharge.

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