CN107638304B - Alpha-arbutin composition with high skin cell permeability and preparation method and application thereof - Google Patents
Alpha-arbutin composition with high skin cell permeability and preparation method and application thereof Download PDFInfo
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- CN107638304B CN107638304B CN201711056114.8A CN201711056114A CN107638304B CN 107638304 B CN107638304 B CN 107638304B CN 201711056114 A CN201711056114 A CN 201711056114A CN 107638304 B CN107638304 B CN 107638304B
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- BJRNKVDFDLYUGJ-ZIQFBCGOSA-N alpha-Arbutin Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1OC1=CC=C(O)C=C1 BJRNKVDFDLYUGJ-ZIQFBCGOSA-N 0.000 title claims abstract description 163
- 229940033280 alpha-arbutin Drugs 0.000 title claims abstract description 162
- 239000000203 mixture Substances 0.000 title claims abstract description 127
- 210000004927 skin cell Anatomy 0.000 title claims abstract description 109
- 230000035699 permeability Effects 0.000 title claims abstract description 77
- 238000002360 preparation method Methods 0.000 title claims abstract description 15
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 88
- 108010073771 Soybean Proteins Proteins 0.000 claims abstract description 36
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- 239000000787 lecithin Substances 0.000 claims abstract description 24
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- 229940067606 lecithin Drugs 0.000 claims abstract description 24
- 150000005846 sugar alcohols Polymers 0.000 claims abstract description 20
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- PUPZLCDOIYMWBV-UHFFFAOYSA-N (+/-)-1,3-Butanediol Chemical compound CC(O)CCO PUPZLCDOIYMWBV-UHFFFAOYSA-N 0.000 claims description 42
- LRHPLDYGYMQRHN-UHFFFAOYSA-N N-Butanol Chemical compound CCCCO LRHPLDYGYMQRHN-UHFFFAOYSA-N 0.000 claims description 36
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- JLPULHDHAOZNQI-ZTIMHPMXSA-N 1-hexadecanoyl-2-(9Z,12Z-octadecadienoyl)-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCC\C=C/C\C=C/CCCCC JLPULHDHAOZNQI-ZTIMHPMXSA-N 0.000 claims description 26
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Abstract
The invention provides an alpha-arbutin composition with high skin cell permeability and preparation and application thereof. The alpha-arbutin composition comprises the following components in percentage by mass: 1.0-15.0% of alpha-arbutin, 1.0-15.0% of lecithin, 0.4-6.0% of quaternized soybean protein, 15.0-50.0% of polyhydric alcohol, 2.0-10.0% of auxiliary emulsifier, 0.1-1.5% of stabilizer and the balance of water. The alpha-arbutin composition with high skin cell permeability provided by the invention has the advantages of good skin permeability, high skin retention, good stability and large drug-loading rate, can efficiently promote the alpha-arbutin to reach a skin-care target site through a skin barrier, and has remarkable whitening and freckle-removing effects. Meanwhile, the preparation method is simple and easy to control, green and environment-friendly, and is suitable for industrial production.
Description
Technical Field
The invention relates to an alpha-arbutin composition, in particular to an alpha-arbutin composition with high skin cell permeability and a preparation method and application thereof.
Background
Alpha-arbutin is an epimer of beta-arbutin and has the chemical name of 4-hydroxyphenyl-alpha-D-glucopyranoside. The molecular structure of the alpha-arbutin has two structural functional groups: glucose residues and phenolic hydroxyl groups. The glucose residue has hydrophilicity, and the phenolic hydroxyl has melanin synthetase inhibiting effect, so that the alpha-arbutin can play a role in moisturizing and whitening to a certain extent, and can be used as a whitening agent to be added into cosmetics to play a role in whitening and removing freckles.
Research shows that the alpha-arbutin can effectively inhibit the activity of tyrosinase in the skin and block the formation of melanin while not influencing the growth of skin cells, and the decomposition and excretion of the melanin are accelerated by the combination of the alpha-arbutin and the tyrosinase, so that the skin pigmentation is reduced, and color spots and freckles are removed. Compared with beta-arbutin, the alpha-arbutin has the characteristics of safety, stability and high efficiency, and the intensity of inhibiting tyrosinase is greatly superior to that of the widely used beta-arbutin.
However, alpha-arbutin has strong hydrophilicity and poor skin permeability, and is difficult to penetrate through skin barriers and enter melanocytes to exert the whitening effect. Therefore, the low skin retention of α -arbutin limits its effective use in cosmetics.
Disclosure of Invention
The invention aims to provide an alpha-arbutin composition with high skin retention and high skin cell penetration, and a preparation method and application thereof.
In order to achieve the above object, the present invention provides the following technical solutions:
the invention provides an alpha-arbutin composition with high skin cell permeability, which is prepared from the following raw material components in percentage by mass:
preferably, the lecithin includes one or more of soybean lecithin, egg yolk lecithin, hydrogenated soybean lecithin and hydrogenated egg yolk lecithin.
Preferably, the quaternized soy protein comprises hydroxypropyltrimethylammonium chloride hydrolyzed soy protein and/or lauryl dimethylammonium hydroxypropyl hydrolyzed soy protein.
Preferably, the polyhydric alcohol comprises one or more of 1, 2-propylene glycol, dipropylene glycol, glycerol, 1, 2-hexanediol, 1, 3-butanediol, 1, 2-pentanediol, octyldodecanol, sorbitol and octylene glycol.
Preferably, the coemulsifier comprises one or more of diethylene glycol monoethyl ether, butanol polyether-9, butanol polyether-12, butanol polyether-26, butanol polyether-35, PPG-26-butanol polyether-26 and poloxamer.
Preferably, the stabilizer comprises one or more of xanthan gum, carboxyethyl cellulose, gelatin, arabic gum and carbomer.
Preferably, the alpha-arbutin composition with high skin cell permeability further comprises 0.01-4.0% of preservative.
The invention also provides a preparation method of the alpha-arbutin composition with high skin cell permeability, which comprises the following steps:
mixing alpha-arbutin, quaternized soy protein, a stabilizer and water to obtain a water phase;
mixing lecithin, polyhydric alcohol and a co-emulsifier to obtain an oil phase;
mixing the water phase with the oil phase to obtain a mixed solution;
homogenizing the mixed solution to obtain the alpha-arbutin composition with high skin cell permeability.
Preferably, the oil phase further comprises a preservative.
The invention also provides application of the alpha-arbutin composition with high skin cell permeability in cosmetics.
The invention provides an alpha-arbutin composition with high skin cell permeability, which is prepared from the following raw material components in percentage by mass: 1.0-15.0% of alpha-arbutin, 1.0-15.0% of lecithin, 0.4-6.0% of quaternized soybean protein, 15.0-50.0% of polyhydric alcohol, 2.0-10.0% of auxiliary emulsifier, 0.1-1.5% of stabilizer and the balance of water. The alpha-arbutin in the alpha-arbutin composition with high skin cell permeability can ensure proper drug loading, and the lecithin in the alpha-arbutin composition is a component of cell membranes and has good biocompatibility, so that the alpha-arbutin can be wrapped in a phospholipid bilayer to promote the alpha-arbutin to penetrate through the skin cuticle and enter deep tissues; the quaternized soybean protein has positive charges, good cell affinity and strong intracellular permeability, can help alpha-arbutin to penetrate through cell membranes to act on target substances in cells, and better exerts the beautifying effect; co-emulsifier and stabilizerThe fixative maintains the long-term stability of the system. Therefore, the alpha-arbutin composition with high skin cell penetration provided by the invention is large in drug loading, good in skin penetration, high in skin retention, good in stability and good in biocompatibility, has high-efficiency whitening, freckle removing and skin tendering effects, and can be used in the field of cosmetic preparation. The results of the examples show that the alpha-arbutin composition with high skin cell penetration provided by the invention can reach 1554.2 mu g/cm in 12h of skin cumulative penetration2The accumulated retention of the skin can reach 167.8 mu g/cm after 12 hours2As described above, the composition has excellent skin permeability and retention; under the condition of safe dosage, the compound has obvious inhibition effect on B-16 melanoma cell proliferation and tyrosinase activity, and has more efficient and obvious whitening and freckle removing effects; after being placed for 30 days, the product properties and the particle size are not obviously changed, and the stability is good.
The invention also provides a preparation method of the alpha-arbutin composition with high skin cell permeability, the method is simple to operate, and the obtained alpha-arbutin composition with high skin cell permeability is more uniform and stable in system. The invention also provides application of the alpha-arbutin composition with high skin cell permeability in cosmetics, and the composition can be directly added into the cosmetics and has good effects of whitening, removing freckles and tendering skin.
Drawings
FIG. 1 shows in vitro transdermal test results of samples prepared in examples 2 to 5 and comparative examples 1 and 2;
FIG. 2 is a graph showing the results of the inhibition of the proliferation of B-16 melanoma cells by the samples prepared in example 2, comparative example 1 and comparative example 2;
FIG. 3 shows the results of the inhibition of tyrosinase activity by the samples prepared in example 2, comparative example 1 and comparative example 2;
FIG. 4 is a graph showing a distribution of particle sizes of the high skin cell permeation α -arbutin composition obtained in example 7.
Detailed Description
The invention provides an alpha-arbutin composition with high skin cell permeability, which is prepared from the following raw material components in percentage by mass:
in the present invention, all the raw material components are commercially available products well known to those skilled in the art unless otherwise specified.
The alpha-arbutin composition with high skin cell permeability provided by the invention comprises 1.0-15.0% of alpha-arbutin, preferably 2.0-12.0%, and more preferably 5.0-10.0%.
In the invention, the alpha-arbutin can effectively inhibit the activity of tyrosinase in the skin and block the formation of melanin while not influencing the growth of skin cells, and the decomposition and excretion of the melanin are accelerated by the combination of the alpha-arbutin and the tyrosinase, so that the skin pigmentation is reduced, and color spots and freckles are removed.
The alpha-arbutin composition with high skin cell penetration provided by the invention comprises 1.0-15.0% of lecithin, preferably 2.0-12.0%, more preferably 5.0-10.0%.
In the invention, the lecithin is preferably one or more of soybean lecithin, egg yolk lecithin, hydrogenated soybean lecithin and hydrogenated egg yolk lecithin; in the present invention, when the lecithin is two or more of the above specific choices, the ratio of each substance is not particularly limited and may be mixed in an arbitrary ratio; in the present invention, the lecithin is preferably 1 to 2 kinds of the above specific choices.
In the invention, when the lecithin is preferably a mixture of egg yolk lecithin and hydrogenated egg yolk lecithin, the mass ratio of the egg yolk lecithin to the hydrogenated egg yolk lecithin is preferably (1-5): specifically, 1 may be 2:1, 3:1 or 4: 1.
In the present invention, when the lecithin is preferably a mixture of soybean lecithin and hydrogenated soybean lecithin, the mass ratio of the soybean lecithin to the hydrogenated soybean lecithin is preferably 1: (1-4), specifically 1:1, 1:2, 1:3.
In the present invention, when the lecithin is preferably a mixture of egg yolk lecithin and hydrogenated soybean lecithin, the mass ratio of the egg yolk lecithin to the hydrogenated soybean lecithin is preferably (2-4): 1, specifically 2:1, 7:3, 3: 1.
In the present invention, when the lecithin is preferably a mixture of soybean lecithin and hydrogenated egg yolk lecithin, the mass ratio of the soybean lecithin to the hydrogenated egg yolk lecithin is preferably (0.5 to 3): 1, specifically, it may be 0.5:1, 1: 1. 2: 1.
In the present invention, when the lecithin is preferably a mixture of hydrogenated soybean lecithin and hydrogenated egg yolk lecithin, the mass ratio of the hydrogenated soybean lecithin to the hydrogenated egg yolk lecithin is preferably (0.5 to 3): 1, specifically, it may be 0.5:1, 1: 1. 2: 1.
The alpha-arbutin composition with high skin cell permeability provided by the invention comprises 0.4-6.0% of quaternized soybean protein, preferably 0.6-5.0%, more preferably 1.0-4.0%.
In the present invention, the quaternized soy protein is preferably one or both of hydroxypropyltrimethylammonium chloride hydrolyzed soy protein, lauryl dimethylammonium hydroxypropyl hydrolyzed soy protein.
In the present invention, when the quaternized soy protein is preferably a mixture of hydroxypropyltrimethylammonium chloride hydrolyzed soy protein and lauryl dimethylammonium hydroxypropylhydrolyzed soy protein, the mass ratio of hydroxypropyltrimethylammonium chloride hydrolyzed soy protein to lauryl dimethylammonium hydroxypropylhydrolyzed soy protein may specifically be 5:3, 2:3, 1: 3.5.
The alpha-arbutin composition with high skin cell penetration provided by the invention comprises 15.0-50.0% of polyhydric alcohol by mass, preferably 20.0-40.0%, and more preferably 25.0-35.0%.
In the invention, the polyalcohol is preferably one or more of 1, 2-propylene glycol, dipropylene glycol, glycerol, 1, 2-hexanediol, 1, 3-butanediol, 1, 2-pentanediol, octyldodecanol, sorbitol and octylene glycol; in the present invention, when the polyhydric alcohols are two or more of the above specific choices, the proportions of the respective substances are not particularly limited and may be mixed in an arbitrary proportion; in the present invention, the polyol is preferably 2 to 3 of the above specific choices;
in the invention, when the polyhydric alcohol is preferably a mixture of 1, 3-butanediol and sorbitol, the mass ratio of the 1, 3-butanediol to the sorbitol is preferably (0.1-4): 1, specifically 1:2, 1:1, 3: 1.
In the invention, when the polyhydric alcohol is preferably a mixture of 1, 2-propylene glycol and octyl dodecanol, the mass ratio of the 1, 2-propylene glycol to the octyl dodecanol is preferably (5-11): 1, specifically 6:1, 8:1, 10: 1.
In the present invention, when the polyhydric alcohol is preferably 1, 2-propanediol, a mixture of glycerin and 1, 3-butanediol, the mass ratio of 1, 2-propanediol, glycerin and 1, 3-butanediol may be specifically 1:2:2, 1:1:2, 1:2: 1.
In the present invention, when the polyhydric alcohol is preferably a mixture of dipropylene glycol, 1, 2-hexanediol, and 1, 3-butanediol, the mass ratio of dipropylene glycol, 1, 2-hexanediol, and 1, 3-butanediol may be specifically 1:1:2, 1:2: 1.
In the present invention, when the polyol is preferably a mixture of glycerol, 1, 2-pentanediol and octyldodecanol, the mass ratio of glycerol, 1, 2-pentanediol and octyldodecanol may be specifically 15:5:1, 1:2:5, 10:5: 1.
In the present invention, when the polyhydric alcohol is preferably a mixture of 1, 2-propanediol, 1, 2-hexanediol and 1, 3-butanediol, the mass ratio of 1, 2-propanediol, 1, 2-hexanediol and 1, 3-butanediol may be specifically 8:2:5, 8:3:1, 1:2: 1.
In the present invention, when the polyhydric alcohol is preferably a mixture of glycerin, 1, 3-butanediol and 1, 2-pentanediol, the mass ratio of glycerin, 1, 3-butanediol and 1, 2-pentanediol may be specifically 2:10:3, 1:4:1, 2:10: 5.
In the present invention, when the polyhydric alcohol is preferably 1, 2-propanediol, a mixture of glycerol and octaethylene glycol, the mass ratio of 1, 2-propanediol, glycerol and octaethylene glycol may be specifically 4:5:1, 1:1:2, 1:2: 1.
In the present invention, when the polyhydric alcohol is preferably a mixture of 1, 2-hexanediol, 1, 3-butanediol and sorbitol, the mass ratio of 1, 2-hexanediol, 1, 3-butanediol and sorbitol may be specifically 2:15:2, 1:5:2, 1:2: 4.
In the present invention, when the polyol is preferably 1, 2-propanediol, a mixture of dipropylene glycol and glycerin, the mass ratio of 1, 2-propanediol, dipropylene glycol and glycerin is 2:2:15, 1:3:2, 1:7: 3.
The alpha-arbutin composition with high skin cell permeability provided by the invention comprises 2.0-10.0% by mass of a co-emulsifier, preferably 3.0-8.0%, and more preferably 4.0-7.0%.
In the invention, the coemulsifier is preferably one or more of diethylene glycol monoethyl ether, butanol polyether-9, butanol polyether-12, butanol polyether-26, butanol polyether-35, PPG-26-butanol polyether-26 and poloxamer; in the present invention, when the coemulsifier is two or more of the above specific choices, the ratio of each substance is not particularly limited and may be mixed in an arbitrary ratio; in the present invention, the co-emulsifier is preferably 1 to 3 of the above specific choices.
In the invention, when the coemulsifier is preferably a mixture of butyether-26 and PPG-26-butyether-26, the mass ratio of the butyether-26 to the PPG-26-butyether-26 can be 3:2, 1:1 or 1: 2.
In the present invention, when the co-emulsifier is preferably a mixture of diethylene glycol monoethyl ether and butyether-12, the mass ratio of diethylene glycol monoethyl ether to butyether-12 may be specifically 1:5, 3:2, 3: 1.
In the present invention, when the co-emulsifier is preferably a mixture of ethylene glycol monoethyl ether and PPG-26-butanol polyether-26, the mass ratio of the ethylene glycol monoethyl ether to PPG-26-butanol polyether-26 may be specifically 1:1, 1:3, 2: 5.
In the invention, when the coemulsifier is preferably a mixture of butyether-9 and poloxamer, the mass ratio of the butyether-9 to the poloxamer can be specifically 5:1, 3:2 and 1: 1.
In the present invention, when the coemulsifier is preferably a mixture of buteth-12 and buteth-35, the mass ratio of buteth-12 to buteth-35 may be specifically 4:3, 2:5, 3: 1.
In the invention, when the coemulsifier is preferably a mixture of butyether-9 and PPG-26-butyether-26, the mass ratio of the butyether-9 to the PPG-26-butyether-26 can be specifically 5:1, 1:2 and 3: 1.
In the invention, when the number of the co-emulsifier is 3, the co-emulsifier is preferably a mixture of butyether-26, butyether-35 and PPG-26-butyether-26, and the mass ratio of the butyether-26, the butyether-35 and the PPG-26-butyether-26 can be 3:3:2, 2:5:3 and 1:2: 3.
The alpha-arbutin composition with high skin cell penetration provided by the invention comprises 0.1-1.5% of stabilizer by mass, preferably 0.3-1.2%, and more preferably 0.5-1.0%.
In the present invention, the stabilizer preferably comprises one or more of xanthan gum, carboxyethyl cellulose, gelatin, acacia and carbomer; in the present invention, when the stabilizer is two or more of the above specific choices, the ratio of each substance is not particularly limited and may be mixed in an arbitrary ratio; in the present invention, the stabilizer is preferably 1 to 2 of the above specific choices.
In the present invention, when the number of the stabilizers is 2, the stabilizer is preferably a mixture of gelatin and carbomer, and the mass ratio of the gelatin to the carbomer is preferably 2:1, 1:1 or 2: 3.
In the present invention, when 1 stabilizer is used, the stabilizer is preferably carboxyethyl cellulose.
The alpha-arbutin composition with high skin cell permeability provided by the invention comprises the balance of water, and the water is preferably purified water.
In the present invention, the particle size of the alpha-arbutin composition with high skin cell penetration is preferably 80 to 350nm, more preferably 100 to 250nm, and most preferably 120 to 200 nm.
In the present invention, the particle size of the high skin cell permeation α -arbutin composition is the particle size of particles formed by dispersing the high skin cell permeation α -arbutin composition in water; the particles comprise all the components of the composition, and the components form the particles through mutual physical interaction.
In the present invention, the Zeta potential of the alpha-arbutin composition with high skin cell permeability is preferably 0 to +60mV, more preferably +10 to +40mV, and most preferably +10 to +20 mV.
The alpha-arbutin composition with high skin cell permeability provided by the invention preferably further comprises 0.01-4.0% of preservative, more preferably 0.05-3.0%, and most preferably 0.1-1.0%.
In the invention, the preservative is preferably one or more of phenoxyethanol, methylisothiazolinone, potassium sorbate, DMDM hydantoin, imidazolidinyl urea and ethylhexyl glycerin; in the present invention, when the preservatives are two or more of the above specific choices, the proportions of the respective substances are not particularly limited and may be mixed in any proportion; in the present invention, the preservative is preferably 1 to 2 of the above specific choices.
In the invention, when the number of the preservatives is 2, the preservatives are preferably a mixture of phenoxyethanol and ethylhexyl glycerol, and the mass ratio of the phenoxyethanol to the ethylhexyl glycerol can be 1:1, 4:1, 7:3 and 1: 5.
The invention also provides a preparation method of the alpha-arbutin composition with high skin cell permeability, which comprises the following steps:
mixing alpha-arbutin, quaternized soy protein, a stabilizer and water to obtain a water phase;
mixing lecithin, polyhydric alcohol and a co-emulsifier to obtain an oil phase;
mixing the water phase with the oil phase to obtain a mixed solution;
homogenizing the mixed solution to obtain the alpha-arbutin composition with high skin cell permeability.
The invention mixes alpha-arbutin, quaternized soy protein, stabilizer and water to obtain water phase. In the invention, the mixing temperature is preferably 50-70 ℃, more preferably 55-70 ℃, and most preferably 55-65 ℃. The mixing time is not particularly limited, and all the raw materials can be uniformly mixed. The manner and rate of heating to the mixing temperature is not particularly limited in the present invention, and may be by solution heating as is well known to those skilled in the art.
In the present invention, the mixing process is preferably performed under stirring conditions. The stirring speed is not particularly limited, and all the components can be fully dissolved to obtain a water phase.
The oil phase is obtained by mixing lecithin, polyhydric alcohol and an auxiliary emulsifier. In the invention, the mixing temperature is preferably 50-70 ℃, more preferably 55-70 ℃, and most preferably 55-65 ℃. The mixing time is not particularly limited, and all the raw materials can be uniformly mixed. The manner and rate of heating to the mixing temperature is not particularly limited in the present invention, and may be by solution heating as is well known to those skilled in the art.
In the present invention, the mixing process is preferably performed under stirring conditions. The stirring speed is not particularly limited, and all the components can be fully dissolved to obtain the oil phase.
In the present invention, the oil phase preferably further comprises a preservative component, and the mixing is preferably performed by mixing the preservative with lecithin, polyol and co-emulsifier.
The present invention does not require any order of preparation of the aqueous phase and the oil phase, and the aqueous phase and the oil phase may be prepared in any order.
After obtaining the water phase and the oil phase, the invention mixes the water phase and the oil phase to obtain a mixed solution. In the invention, the mixing temperature of the oil phase and the water phase is preferably 50-70 ℃, more preferably 55-70 ℃, and most preferably 55-65 ℃. The manner and rate of heating to the mixing temperature is not particularly limited in the present invention, and may be by solution heating as is well known to those skilled in the art.
In the present invention, the mixing of the aqueous phase and the oil phase is preferably performed under stirring conditions; the stirring time is preferably 20-40 min, more preferably 20-35 min, and most preferably 25-30 min. The stirring speed is not particularly limited in the present invention, and the raw materials can be uniformly mixed by using the method well known to those skilled in the art.
After the mixed solution is obtained, the invention carries out homogenization treatment on the mixed solution to obtain the alpha-arbutin composition with high skin cell permeability. In the invention, the number of homogenization treatment is preferably 2-6, more preferably 3-5, and most preferably 4; the time of single homogenization treatment is preferably 4-12 min independently, more preferably 5-10 min, and most preferably 6-8 min; the temperature of the homogenization treatment is preferably 60-85 ℃, more preferably 65-80 ℃, and most preferably 70-75 ℃; the homogenization treatment is preferably high-pressure homogenization treatment; the pressure of the homogenization treatment is preferably 500 to 1500bar, more preferably 600 to 1200bar, and most preferably 800 to 1000 bar.
In the present invention, the homogenization treatment makes the alpha-arbutin composition system with high skin cell penetration more uniform and stable.
The invention also provides the application of the alpha-arbutin composition with high skin cell permeability or the alpha-arbutin composition with high skin cell permeability prepared by the preparation method in cosmetics. The application of the alpha-arbutin composition with high skin cell permeability in cosmetics is not particularly limited, and the alpha-arbutin composition can be directly added into the cosmetics for use. In the present invention, the alpha-arbutin composition with high skin cell permeability is preferably added in an amount ranging from 5 to 50% by mass, more preferably from 10 to 30% by mass, and most preferably from 10 to 20% by mass in the cosmetic.
In the present invention, the product form of the high skin cell penetration α -arbutin composition is preferably a cream, aqua, emulsion, spray or gel.
In the present invention, the alpha-arbutin composition with high skin cell permeability can be added into cosmetics to effectively inhibit the activity of tyrosinase in the skin, block the formation of melanin, accelerate the decomposition and excretion of melanin, thereby reducing skin pigmentation and removing stains and freckles. The alpha-arbutin composition with high skin cell permeability provided by the invention has the advantages of good skin permeability, high skin retention and remarkable whitening and freckle removing effects, and can be widely applied to cosmetics, especially whitening, freckle removing and skin tendering cosmetics.
The high skin cell penetration α -arbutin composition provided by the present invention, and the preparation method and use thereof are described in detail below with reference to examples, but they should not be construed as limiting the scope of the present invention.
Example 1
Adding 1% of alpha-arbutin, 0.4% of lauryl dimethyl ammonium hydroxypropyl hydrolyzed soybean protein, 1% of xanthan gum and 0.5% of carbomer into 43.1% of water, and stirring and dissolving at 50 ℃ in water bath to obtain a water phase for later use;
dissolving 1% hydrogenated soybean lecithin, 10% 1,2 propylene glycol, 20% glycerol, 20% 1, 3-butanediol, 2% diethylene glycol monoethyl ether, 0.5% phenoxyethanol and 0.5% ethylhexyl glycerol in 50 deg.C water bath under stirring to obtain oil phase;
mixing the water phase and the oil phase, and continuously stirring for 20min at 50 deg.C in water bath to obtain alpha-arbutin mixed solution with high skin cell permeability;
homogenizing the alpha-arbutin mixed solution with high skin cell permeability under the conditions of 500bar pressure and 60 ℃ for 4min, and circulating for 6 times to obtain the alpha-arbutin composition with high skin cell permeability. The alpha-arbutin composition with high skin cell penetration has the particle size of 80.1nm and the Zeta potential of +0.1 mV.
Example 2
Adding 2% of alpha-arbutin, 0.5% of hydroxypropyl trimethyl ammonium chloride hydrolyzed soybean protein and 0.5% of gelatin into 67% of water, and stirring and dissolving at 55 ℃ in a water bath to obtain a water phase for later use;
stirring and dissolving 1% of soybean lecithin, 1% of hydrogenated soybean lecithin, 5% of dipropylene glycol, 5% of 1, 2-hexanediol, 10% of 1, 3-butanediol, 1% of octaethylene glycol, 2% of butyether-9, 1% of poloxamer and 4% of potassium sorbate in a water bath at 55 ℃ to obtain an oil phase for later use;
mixing the water phase and the oil phase, and continuously stirring for 25min at 55 deg.C in water bath to obtain alpha-arbutin mixed solution with high skin cell permeability;
homogenizing the alpha-arbutin mixed solution with high skin cell permeability under the conditions of pressure of 800bar and temperature of 70 ℃ for 6min, and circulating for 5 times to obtain the alpha-arbutin composition with high skin cell permeability. The alpha-arbutin composition with high skin cell permeability has the particle size of 123.6nm and the Zeta potential of +3.1 mV.
Example 3
Adding 4% of alpha-arbutin, 0.5% of hydroxypropyl trimethyl ammonium chloride hydrolyzed soybean protein, 0.3% of lauryl dimethyl ammonium hydroxypropyl hydrolyzed soybean protein and 0.5% of Arabic gum into 65.2% of water, and stirring and dissolving at 60 ℃ in a water bath to obtain a water phase for later use;
stirring and dissolving 2% of egg yolk lecithin, 1% of hydrogenated egg yolk lecithin, 15% of glycerol, 5% of 1, 2-pentanediol, 1% of octyldodecanol, 3% of butanol polyether-26, 2% of PPG-26-butanol polyether-26 and 0.5% of imidazolidinyl urea in a water bath condition at 60 ℃ to obtain an oil phase for later use;
mixing the water phase and the oil phase, and continuously stirring for 30min at 60 deg.C in water bath to obtain alpha-arbutin mixed solution with high skin cell permeability;
homogenizing the alpha-arbutin mixed solution with high skin cell permeability under the conditions of 1000bar pressure and 75 ℃ for 8min, and circulating for 4 times to obtain the alpha-arbutin composition with high skin cell permeability. The alpha-arbutin composition with high skin cell penetration has the particle size of 159.2nm and the Zeta potential of +6.9 mV.
Example 4
Adding 8% of alpha-arbutin, 4% of lauryl dimethyl ammonium hydroxypropyl hydrolyzed soybean protein and 0.3% of xanthan gum into 50.7% of water, and stirring and dissolving in a water bath at 65 ℃ to obtain a water phase for later use;
stirring 10% soybean lecithin, 15% 1, 3-butanediol, 5% sorbitol, 1% diethylene glycol monoethyl ether, 5% butanol polyether-12, and 1% phenoxyethanol in water bath at 65 deg.C to obtain oil phase;
mixing the water phase and the oil phase, and continuously stirring for 35min at 65 deg.C in water bath to obtain alpha-arbutin mixed solution with high skin cell permeability;
homogenizing the alpha-arbutin mixed solution with high skin cell permeability under the conditions of pressure of 1200bar and temperature of 80 ℃ for 10min, and circulating for 3 times to obtain the alpha-arbutin composition with high skin cell permeability. The alpha-arbutin composition with high skin cell permeability has the particle size of 173.8nm and the Zeta potential of +17.6 mV.
Example 5
Adding 12% of alpha-arbutin, 5% of hydroxypropyl trimethyl ammonium chloride hydrolyzed soybean protein and 0.2% of carbomer into 44.3% of water, and stirring and dissolving in a water bath at 65 ℃ to obtain a water phase for later use;
stirring and dissolving 12% of egg yolk lecithin, 3% of hydrogenated egg yolk lecithin, 8% of 1, 2-propylene glycol, 2% of 1, 2-hexanediol, 5% of 1, 3-butanediol, 3% of butanol polyether-26, 3% of butanol polyether-35, 2% of PPG-26-butanol polyether-26 and 0.5% of DMDM hydantoin in a water bath condition at 65 ℃ to obtain an oil phase for later use;
mixing the water phase and the oil phase, and continuously stirring for 25min at 65 deg.C in water bath to obtain alpha-arbutin mixed solution with high skin cell permeability;
homogenizing the alpha-arbutin mixed solution with high skin cell permeability under the conditions of 1400bar pressure and 80 ℃ for 6min, and circulating for 3 times to obtain the alpha-arbutin composition with high skin cell permeability. The alpha-arbutin composition with high skin cell permeability has the particle size of 324.7nm and the Zeta potential of +22.8 mV.
Example 6
Adding 15% of alpha-arbutin, 6% of lauryl dimethyl ammonium hydroxypropyl hydrolyzed soybean protein and 0.1% of carboxyethyl cellulose into 38.89% of water, and stirring and dissolving in a water bath at 70 ℃ to obtain a water phase for later use;
stirring and dissolving 5% of soybean lecithin, 10% of hydrogenated soybean lecithin, 2% of glycerol, 10% of 1, 3-butanediol, 3% of 1, 2-pentanediol, 5% of diethylene glycol monoethyl ether, 5% of PPG-26-butanol polyether-26 and 0.01% of methylisothiazolinone in a water bath at 70 ℃ to obtain an oil phase for later use;
mixing the water phase and the oil phase, and continuously stirring for 40min at 70 deg.C in water bath to obtain alpha-arbutin mixed solution with high skin cell permeability;
homogenizing the alpha-arbutin mixed solution with high skin cell permeability under 1500bar pressure and 85 deg.C for 12min, and circulating for 2 times to obtain alpha-arbutin composition with high skin cell permeability. The alpha-arbutin composition with high skin cell permeability has the particle size of 349.8nm and the Zeta potential of +59.8 mV.
Example 7
Adding 10% of alpha-arbutin, 2% of hydroxypropyl trimethyl ammonium chloride hydrolyzed soybean protein, 3% of lauryl dimethyl ammonium hydroxypropyl hydrolyzed soybean protein and 0.2% of carboxyethyl cellulose into 48.8% of water, and stirring and dissolving at 60 ℃ in a water bath to obtain a water phase for later use;
stirring and dissolving 7% of egg yolk lecithin, 3% of hydrogenated soybean lecithin, 8% of 1, 2-propylene glycol, 10% of glycerol, 2% of caprylyl glycol, 3% of diethylene glycol monoethyl ether, 2% of PPG-26-butanol polyether-26, 0.7% of phenoxyethanol and 0.3% of ethylhexyl glycerol in a water bath at the temperature of 60 ℃ to obtain an oil phase for later use;
mixing the water phase and the oil phase, and continuously stirring for 25min at 60 deg.C in water bath to obtain alpha-arbutin mixed solution with high skin cell permeability;
homogenizing the alpha-arbutin mixed solution with high skin cell permeability under the conditions of 1000bar pressure and 70 ℃ for 5min, and circulating for 3 times to obtain the alpha-arbutin composition with high skin cell permeability. The alpha-arbutin composition with high skin cell penetration has the particle size of 201.1nm and the Zeta potential of +18.1 mV.
Example 8
Adding 10% of alpha-arbutin, 5% of lauryl dimethyl ammonium hydroxypropyl hydrolyzed soybean protein and 0.2% of carboxyethyl cellulose into 48.8% of water, and stirring and dissolving under the condition of water bath at 60 ℃ to obtain a water phase for later use;
stirring and dissolving 5% of soybean lecithin, 5% of hydrogenated yolk lecithin, 2% of 1, 2-hexanediol, 15% of 1, 3-butanediol, 2% of sorbitol, 5% of butanol polyether-9, 1% of poloxamer, 0.7% of phenoxyethanol and 0.3% of ethylhexyl glycerin in a water bath at 60 ℃ to obtain an oil phase for later use;
mixing the water phase and the oil phase, and continuously stirring for 25min at 60 deg.C in water bath to obtain alpha-arbutin mixed solution with high skin cell permeability;
homogenizing the alpha-arbutin mixed solution with high skin cell permeability under the conditions of 1000bar pressure and 70 ℃ for 5min, and circulating for 3 times to obtain the alpha-arbutin composition with high skin cell permeability. The alpha-arbutin composition with high skin cell permeability has the particle size of 182.3nm and the Zeta potential of +14.5 mV.
Example 9
Adding 10% of alpha-arbutin, 4% of hydroxypropyl trimethyl ammonium chloride hydrolyzed soybean protein and 0.2% of carboxyethyl cellulose into 47.8% of water, and stirring and dissolving under the condition of water bath at 60 ℃ to obtain a water phase for later use;
stirring and dissolving 4% of hydrogenated soybean lecithin, 4% of hydrogenated yolk lecithin, 20% of 1, 2-propylene glycol, 2% of octyldodecanol, 4% of butyether-12, 3% of butyether-35, 0.7% of phenoxyethanol and 0.3% of ethylhexyl glycerin in a water bath at 60 ℃ to obtain an oil phase for later use;
mixing the water phase and the oil phase, and continuously stirring for 25min at 60 deg.C in water bath to obtain alpha-arbutin mixed solution with high skin cell permeability;
homogenizing the alpha-arbutin mixed solution with high skin cell permeability under the conditions of 1000bar pressure and 70 ℃ for 5min, and circulating for 3 times to obtain the alpha-arbutin composition with high skin cell permeability. The alpha-arbutin composition with high skin cell permeability has the particle size of 159.1nm and the Zeta potential of +11.4 mV.
Example 10
Adding 10% of alpha-arbutin, 1% of hydroxypropyl trimethyl ammonium chloride hydrolyzed soybean protein, 3.5% of lauryl dimethyl ammonium hydroxypropyl hydrolyzed soybean protein and 0.2% of carboxyethyl cellulose into 47.3% of water, and stirring and dissolving at 60 ℃ in a water bath to obtain a water phase for later use;
stirring and dissolving 6% of soybean lecithin, 6% of egg yolk lecithin, 2% of 1, 2-propylene glycol, 2% of dipropylene glycol, 15% of glycerol, 5% of butanol polyether-9, 1% of PPG-26-butanol polyether-26, 0.7% of phenoxyethanol and 0.3% of ethylhexyl glycerol in a water bath at 60 ℃ to obtain an oil phase for later use;
mixing the water phase and the oil phase, and continuously stirring for 25min at 60 deg.C in water bath to obtain alpha-arbutin mixed solution with high skin cell permeability;
homogenizing the alpha-arbutin mixed solution with high skin cell permeability under the conditions of 1000bar pressure and 70 ℃ for 5min, and circulating for 3 times to obtain the alpha-arbutin composition with high skin cell permeability. The alpha-arbutin composition with high skin cell penetration has the particle size of 143.8nm and the Zeta potential of +9.6 mV.
Example 11
The α -arbutin compositions with high skin cell permeability obtained in examples 1 to 10 were left in a closed container at room temperature for 30 days, and properties and particle sizes of the samples were examined, and the experimental results are shown in table 1.
TABLE 1 results of stability test of alpha-arbutin compositions with high skin cell penetration in examples 1-10
The stability test result shows that: the alpha-arbutin composition with high skin cell permeability provided by the invention has no aggregation, delamination and precipitation phenomena, the particle size is 80-350 nm, the practical application requirement is met, the aggregation, delamination and precipitation phenomena do not occur after a sample is placed for 30 days, the particle size does not change significantly, the practical application requirement is still met, particularly, the alpha-arbutin composition is still stable under the condition of high active matter concentration, and the phenomena of active matter crystallization precipitation, leakage and the like are not found. Therefore, the alpha-arbutin composition with high skin cell penetration provided by the invention has good stability.
Comparative example 1
The alpha-arbutin cream is prepared according to a conventional cream preparation method: melting 2.0% of alpha-arbutin, 3.0% of stearic acid, 4.5% of glyceryl monostearate, 5.0% of cetostearyl alcohol and 6.0% of polydimethylsiloxane in a water bath at 75 ℃ to obtain an oil phase; dissolving 10.0% of glycerol, 5.0% of 1, 2-propylene glycol, 0.3% of triethanolamine and 64.2% of purified water in a water bath at 75 ℃ to obtain a water phase; mixing the oil phase and the water phase under stirring, emulsifying, and cooling to obtain 2.0% alpha-arbutin cream.
Comparative example 2
A blank cream containing no alpha-arbutin is prepared according to the formula and the method in the comparative example 1, and the blank cream is compounded with the alpha-arbutin composition with high skin cell penetration and the alpha-arbutin concentration of 4.0 percent prepared in the example 3 according to the mass ratio of 1:1 to obtain the cream of the alpha-arbutin composition with high skin cell penetration and the alpha-arbutin content of 2.0 percent as a cream control.
Example 12
And (3) carrying out transdermal test by taking the abdominal skin of the male SD rat with the weight of 160-220 g as a barrier layer of the transdermal test. Securing intact skin between the receiving reservoir and the supply reservoir (skin inner layer facing the receiving reservoir); the diffusion cell parameters were: effective diffusion area 3.14cm2The volume of the receiving pool is about 7.0ml, and the magnetic stirring speed is 600 rpm; filling a receiving pool with 4.5% of ceteareth-20% of ethanol-physiological saline as a release medium, removing bubbles, starting stirring, keeping the temperature to (37.0 +/-0.5) ° C, uniformly coating 1g of a sample on the surface of skin, sucking 0.35ml of receiving liquid for 1h, 2h, 4h, 6h, 8h, 10h and 12h, supplementing 0.35ml of the release medium, filtering the receiving liquid by using a 0.22 mu m organic filter membrane, measuring the concentration of alpha-arbutin in the filtered receiving liquid by using high performance liquid chromatography, and calculating the cumulative transdermal quantity of the medicine at different times.
The cumulative transdermal amount of alpha-arbutin per unit area is calculated according to the following formula:
wherein: qs is the cumulative transdermal mass; s is the effective diffusion area; v is the volume of the physiological saline in the receiving pool; ci is the concentration of the drug in the receiving solution from the 1 st to the last sampling; n is the nth sample volume; cn is the concentration of the drug in the receiving fluid at the time of the sampling.
The samples prepared in examples 2 to 5 and comparative examples 1 and 2 were subjected to the transdermal test in the manner described above, and the skin cumulative permeation amount for 12 hours of the samples of examples 2 to 5 was 721.2. mu.g/cm2、956.4μg/cm2、1243.5μg/cm2、1554.2μg/cm2And the cumulative retention at 12h was 51.9. mu.g/cm2、79.2μg/cm2、106.3μg/cm2、132.5μg/cm2. The result shows that the alpha-arbutin composition with high skin cell penetration provided by the invention has good skin permeability and accumulated retention.
The 12h cumulative permeation of the sample of comparative example 2 was 264.6. mu.g/cm2Comparative example 1 had a cumulative permeation of only 97.1. mu.g/cm for 12h2. The 12h cumulative retention of the comparative example 2 sample was 167.8. mu.g/cm2Comparative example 1 had a cumulative retention of only 21.2. mu.g/cm in 12 hours2. The results show that the comparative example 2 sample has a skin cumulative permeation amount and a cumulative retention amount significantly higher than those of the comparative example 1, and thus it can be known that the application of the α -arbutin composition to a cosmetic cream has better skin permeation and cumulative retention amount than free α -arbutin. The alpha-arbutin composition with high skin cell permeability provided by the invention can penetrate through the skin barrier and deeply penetrate to the skin care target part and be retained at high concentration, so that the cosmetic effect is efficiently exerted.
Example 13
B-16 melanoma cells were selected in the logarithmic growth phase and seeded at a density of 2X 104 cells/mL in 96-well plates at 200. mu.L/well in 37 ℃ with 5% CO2Culturing in saturated humidity environment. After 24h, the medium was replaced once with fresh medium to which the test drug (example 2, comparative example 1, comparative example 2, respectively) was added. Each set 5 dose groups with final concentration of 10, 20, 40, 60, 80 mug/mL, each dose group set three multiple wells, control group without drug, blank group without cell inoculation. And continuously incubating for 48 h. Adding 20 μ L of 5g/L MTT solution into each well 4h before finishing, discarding supernatant after 4h, and adding dimethyl sulfoxide into each wellSulfone 150. mu.L, 490nm wavelength was selected to measure absorbance in each well on an ELISA detector and zeroed with blank.
Cell viability inhibition ═ 1 — (average absorbance value per concentration/average absorbance value of control group) × 100%
B-16 melanoma cell viability assay experiments were conducted in the above-described manner using example 2, comparative example 1, and comparative example 2 as test drugs, and the inhibitory effects of example 2, comparative example 1, and comparative example 2 on the proliferation of B-16 melanoma cells were investigated, and the results of the experiments are plotted in fig. 2.
As can be seen from the results of FIG. 2, after 48 hours of drug action, the inhibition rates of example 2 and comparative example 2 at a concentration of 10. mu.g/mL were 42.1% and 15.3%, respectively, and the inhibition rates of example 2 and comparative example 2 at a concentration of 20. mu.g/mL were 89.4% and 49.5%, respectively, for B-16 melanoma cell proliferation, whereas the inhibition effects of comparative example 1 at concentrations of 10. mu.g/mL and 20. mu.g/mL were insignificant for B-16 melanoma cell proliferation. The experimental result shows that the alpha-arbutin composition with high skin cell permeability provided by the invention is easier to penetrate cell membranes to enter B-16 melanoma cells to exert the drug effect, and can also play a role in inhibiting the proliferation of the B-16 melanoma cells even at a very low concentration.
Example 14
Selection of logarithmic growth phase B-16 melanoma cells at 2X 104The cells were inoculated into 6-well plates at a density of 2.5mL per well, incubated at 37 ℃ with 5% CO2Culturing in saturated humidity environment. After 24h, the medium was replaced once with fresh medium to which the test drug (example 2, comparative example 1, comparative example 2, respectively) was added. The final concentration of each of the 5 dose groups was 10, 20, 40, 60, and 80. mu.g/mL, and no drug was added to the control group. Cells were harvested after further incubation for 72 h. Digesting with 0.25% pancreatin, collecting about 107 cells, washing twice with PBS, adding 1mL of 0.5% sodium deoxycholate solution, shaking to dissolve the cells, preparing cell lysate containing active tyrosinase, placing the tube in ice bath for 15min, adding 3mL of 0.1% L-dopa solution immediately, incubating for 10min, and measuring the absorbance at 475 nm.
Tyrosinase activity inhibition rate (1-A addition group/A control group)
The tyrosinase activity assay test was carried out by the above-described method using example 2, comparative example 1, and comparative example 2 as the test drugs, and the inhibitory effects on the tyrosinase activity of example 2, comparative example 1, and comparative example 2 were examined, and the results of the test are shown in fig. 3.
As can be seen from the results of FIG. 3, example 2, comparative example 1 and comparative example 2 all showed concentration-dependent inhibition of tyrosinase activity. Example 2 and comparative example 2 have stronger inhibitory effects on tyrosinase activity than comparative example 1. The alpha-arbutin composition with high skin cell penetration provided by the invention has more effective and obvious whitening and freckle removing effects compared with free alpha-arbutin.
Example 15
An artificial light source of a sunlight simulator is adopted, and a skin blackening model is induced on the inner sides of the upper arms of 20 healthy subjects by continuous ultraviolet rays (the wave band is 290-400 nm) with 2.0 times of minimum erythema dose (2 MED). Each of 10 subjects applied the sample of example 2 and the sample of comparative example 1 once in the morning and at night, and after 30 days, the melanin values before and after the comparison were carried out. And (3) testing the melanin value of the inner side of the upper arm by adopting a spectrocolorimeter (CM-2600d) instrument, and evaluating the skin whitening effect of the sample according to the change of the front and rear values.
Table 2 results of skin melanin values before and after the experiment (n ═ 10)
| Time of day | Example 2 | Comparative example 1 |
| |
267.6 | 281.2 |
| 30 days | 201.0 | 249.7 |
| Rate of change (%) | 24.9 | 11.2 |
As can be seen from the results in table 2, the decrease tendency of the melanin value of example 2 is significantly better than that of comparative example 1. The alpha-arbutin composition with high skin cell permeability can penetrate through the skin cuticle to enter the basal layer and enter the melanocyte to efficiently exert the whitening effect, so that the whitening effect of the alpha-arbutin is more obvious.
Example 16
Taking the alpha-arbutin composition sample with high skin cell penetration prepared in the example 2, and compounding the alpha-arbutin composition sample with the blank cream in the comparative example 1 according to the mass ratio of 1:1 to obtain the cream.
Example 17
Taking the alpha-arbutin composition sample with high skin cell penetration prepared in the example 3, and compounding the alpha-arbutin composition sample with the blank cream in the comparative example 1 according to the mass ratio of 1:1 to obtain the cream.
Example 18
Taking the alpha-arbutin composition sample with high skin cell penetration prepared in the example 4, and compounding the alpha-arbutin composition sample with the blank cream in the comparative example 1 according to the mass ratio of 1:1 to obtain the cream.
Example 19
Taking the alpha-arbutin composition sample with high skin cell penetration prepared in the example 5, and compounding the alpha-arbutin composition sample with the blank cream in the comparative example 1 according to the mass ratio of 1:1 to obtain the cream.
Example 20
The creams prepared in examples 16 to 19 and the blank cream were subjected to a skin irritation test:
taking 18 healthy rabbits (2.0 +/-0.2) kg in weight, randomly dividing the weight into 6 groups, removing hairs from two sides of the back skin of the rabbits 24 hours before an experiment, and checking whether the removed skin is injured 24 hours after the hairs are removed, wherein the injured skin is not suitable for a skin irritation test. The cream obtained in examples 16 to 19 was applied 3 times a day for 7 consecutive days while a blank cream (without any drug) was applied for control, and the test results were observed and listed in table 3.
According to the test results in table 3, it can be seen that neither the cream obtained in examples 16-19 nor the blank cream has congestion and red swelling after being applied to the skin of rabbits, indicating that the high skin cell penetration α -arbutin composition provided by the present invention has no irritation to the skin.
Table 3 skin irritation observations of compositions 16-19 and blanks of examples 16
"+" rabbit skin congestion, red swelling; "+ +" indicates that the congestion and red swelling still exist, but there is an increasing trend; "-" indicates no hyperemia or redness and swelling.
As can be seen from the above examples, the alpha-arbutin composition with high skin cell penetration provided by the invention has large drug-loading rate, and the maximum concentration of the active ingredient alpha-arbutin can reach 15.0%; the cumulative skin permeability can reach 1554.2 mug/cm after 12 hours2The accumulated retention of the skin can reach 167.8 mu g/cm after 12 hours2As described above, the composition has excellent skin permeability and retention; under the condition of safe dosage, the compound has obvious inhibition effect on B-16 melanoma cell proliferation and tyrosinase activity, and has more efficient and obvious whitening and freckle removing effects; after being placed for 30 days, the product properties and the grain diameter are not obviousThe change and the stability are good.
The foregoing is merely a preferred embodiment of the invention and is not intended to limit the invention in any manner. It should be noted that, for those skilled in the art, without departing from the principle of the present invention, several improvements and modifications can be made, and these improvements and modifications should also be construed as the protection scope of the present invention.
Claims (5)
1. The alpha-arbutin composition with high skin cell permeability is obtained by the following raw material components in percentage by mass:
1.0-15.0% of alpha-arbutin
Lecithin 1.0% -15.0%
0.4-6.0% of quaternized soybean protein
15.0 to 50.0 percent of polyhydric alcohol
2.0 to 10.0 percent of auxiliary emulsifier
0.1 to 1.5 percent of stabilizer
The balance of water;
the quaternized soy protein comprises hydroxypropyl trimethyl ammonium chloride hydrolyzed soy protein and/or lauryl dimethyl ammonium hydroxypropyl hydrolyzed soy protein;
the lecithin comprises one or more of soybean lecithin, yolk lecithin, hydrogenated soybean lecithin and hydrogenated yolk lecithin;
the polyhydric alcohol comprises one or more of 1, 2-propylene glycol, dipropylene glycol, glycerol, 1, 2-hexanediol, 1, 3-butanediol, 1, 2-pentanediol, sorbitol and caprylyl glycol;
the auxiliary emulsifier comprises one or more of diethylene glycol monoethyl ether, butanol polyether-9, butanol polyether-12, butanol polyether-26, butanol polyether-35, PPG-26-butanol polyether-26 and poloxamer;
the stabilizer comprises one or more of xanthan gum, carboxyethyl cellulose, gelatin, acacia and carbomer.
2. The high skin cell penetration α -arbutin composition according to claim 1, further comprising 0.01-4.0% of a preservative.
3. A method for preparing the high skin cell penetration α -arbutin composition of claim 1 comprising the steps of:
mixing alpha-arbutin, quaternized soy protein, a stabilizer and water to obtain a water phase;
mixing lecithin, polyhydric alcohol and a co-emulsifier to obtain an oil phase;
mixing the water phase with the oil phase to obtain a mixed solution;
homogenizing the mixed solution to obtain the alpha-arbutin composition with high skin cell permeability.
4. The method of claim 3, wherein the oil phase further comprises a preservative.
5. Use of the alpha-arbutin composition with high skin cell permeability according to claim 1 or 2 or the alpha-arbutin composition with high skin cell permeability prepared by the preparation method according to claim 3 or 4 in cosmetics.
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| JP2004359587A (en) * | 2003-06-03 | 2004-12-24 | Audein Pyuuchaazu:Kk | Method for producing stable emulsified nanoparticle using arbutin and cosmetic composition containing emulsified nanoparticle |
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Denomination of invention: A type of high skin cell penetration a- Arbutin composite and its preparation method and application Effective date of registration: 20231124 Granted publication date: 20201229 Pledgee: Jieyang Branch of Guangdong Nanyue Bank Co.,Ltd. Pledgor: GUANGDONG LUCKERKONG BIOTECH CO.,LTD. Registration number: Y2023980067460 |