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A kind of high skin retention ceramide nano composition and its preparation method and use

A nano-composite, ceramide technology, applied in skin care preparations, pharmaceutical formulations, cosmetic preparations, etc., can solve the problem of slowing the absorption of active ingredients, hindering the transdermal absorption of ceramides, and the lack of skin care effects of emulsions and gels. It can improve the solubility and water dispersibility, improve the skin permeability, and improve the skin permeability.

Active Publication Date: 2019-12-20
WUHAN BEST CARRIER NANO TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] However, the application of ceramide in cosmetics has the following three defects and deficiencies: one is that ceramide is a highly crystalline substance with low solubility and poor water dispersibility, which leads to a high drug loading capacity of ceramide emulsion or gel in the prior art. Low, the content of ceramide in the emulsion or gel is generally 0.5%, or even 0.05%, resulting in poor skin care effect of emulsion and gel; the second is that ceramide has poor transdermal property, which affects the skin care effect; the third is ceramide emulsion or The gel is easy to crystallize out during the placement process, which reduces the stability of ceramide cosmetics
[0005] However, the above-mentioned patents still have obvious defects and deficiencies: although the Chinese invention patent CN 104546516A adopts nano-liposome technology, the content of ceramide VI in the prepared composite ceramide liposome is 0.1% to 0.5%, and ceramide The content of ⅢB is 0.1% to 0.6%, the content of active ingredients is very low, and the skin care effect is limited. Secondly, the prepared composite ceramide liposome has a large particle size, which hinders the transdermal absorption of ceramide; the Chinese invention patent CN101214198A formula contains The excipients are phospholipids, glycerin, and water. The formula lacks components that promote skin absorption, which will slow down the absorption of active ingredients. Secondly, the particle size of the prepared ceramide liposomes is below 100nm, and there is no limit to the lower limit of the particle size , only considering the correlation between particle size and transdermal property, not comprehensively considering the correlation between particle size and transdermal property and retention, as well as the influence of cosmetic components on retention, the prerequisite for ceramide cosmetics to work And the material basis is that ceramide can penetrate the skin and stay in the skin for a long time at a high concentration. The appropriate particle size of cosmetics is also one of the important prerequisites for skin care effects

Method used

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  • A kind of high skin retention ceramide nano composition and its preparation method and use
  • A kind of high skin retention ceramide nano composition and its preparation method and use
  • A kind of high skin retention ceramide nano composition and its preparation method and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] (1) Prepare the oil phase: melt 3.0% egg yolk phospholipid, 2.0% cholesterol, and 0.5% octyldodecanol in a 65°C water bath, add 0.5% ceramide I after melting, mix well, and set aside;

[0043] (2) Prepare the water phase: add 5.0% vitamin E polyethylene glycol succinate and 15.0% 1,3-butanediol to 74.0% water, stir and dissolve in a water bath at 65°C;

[0044] (3) Preparation of micron-scale dispersion: drop the oil phase prepared in step (1) into the water phase prepared in step (2) and keep stirring, then emulsify at a high speed of 4000rpm for 10min to prepare a micron-scale dispersion;

[0045] (4) Preparation of nano-composition: heat the nano-dispersion prepared in step (3) at 45° C., and then circulate through high-pressure homogenization at 500 bar for 10 times to obtain a ceramide nano-composition. The particle diameter of the ceramide nano composition is 59.3nm, and the encapsulation efficiency is 84.7%.

Embodiment 2

[0047] (1) Prepare the oil phase: melt 5.0% soybean lecithin, 3.0% cholesterol, and 1.0% octyldodecanol in a water bath at 90°C, then add 0.5% ceramide I and 0.5% ceramide II after melting, and mix well ,spare;

[0048] (2) Prepare the water phase: add 3.0% vitamin E polyethylene glycol succinate, 10.0% polyethylene glycol 400, and 20.0% propylene glycol into 57.0% water, stir and dissolve in a water bath at 90°C;

[0049] (3) Preparation of micron-scale dispersion: drop the oil phase prepared in step (1) into the water phase prepared in step (2) and keep stirring, then emulsify at 6000rpm high-speed shear for 5min to make a micron-scale dispersion;

[0050] (4) Preparation of nano-composition: heat the nano-dispersion prepared in step (3) at 70° C., and then cycle through high-pressure homogenization at 1800 bar twice to obtain a ceramide nano-composition. The particle diameter of the ceramide nano composition is 72.8nm, and the encapsulation efficiency is 90.5%.

Embodiment 3

[0052] (1) Prepare the oil phase: put 2.0% egg yolk phospholipids, 5.0% dipalmitoylphosphatidylcholine, 1.0% distearoylphosphatidylcholine, 5.0% octyldodecanol, 5.0% cholesterol in a water bath at 70°C Make it melt; add 1.0% ceramide III A after melting, mix well, set aside;

[0053] (2) Prepare the water phase: add 0.5% vitamin E polyethylene glycol succinate and 10% propylene glycol to 70.5% water, stir and dissolve in a 70°C water bath;

[0054] (3) Preparation of micron-scale dispersion: drop the oil phase prepared in step (1) into the water phase prepared in step (2) and keep stirring, then emulsify at 8000rpm high-speed shear for 3min to make a micron-scale dispersion;

[0055] (4) Preparation of nano-composition: heat the nano-dispersion prepared in step (3) at 50° C., and then cycle 7 times through high-pressure homogenization at 500 bar to obtain a ceramide nano-composition. The particle diameter of the ceramide nano composition is 79.3nm, and the encapsulation effic...

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Abstract

The invention relates to a high skin retention ceramide nano composition, and a preparation method and applications thereof. The high skin retention ceramide nano composition is composed of, by mass, 0.5 to 8.0% of ceramide, 3.0 to 10.0% of phospholipid, 0.5 to 5.0% of cholesterol, 0.5 to 5.0% of octyldodecanol, 0.5 to 5.0% of D-alpha-tocopheryl polyethylene glycol 1000 succinate, 10.0 to 30.0% of a polyalcohol, and the balance purified water. According to the preparation method, an oil phase prepared from ceramide, phospholipid, cholesterol, and octyldodecanol is added into a water phase prepared from D-alpha-tocopheryl polyethylene glycol 1000 succinate, the polyalcohol, and purified water dropwise; and an obtained mixture is subjected to high speed shear emulsification and high pressure homogenization or high pressure microfluidic equipment treatment. Drug loading capacity of the high skin retention ceramide nano composition is large; transdermal delivery of ceramide, and high concentration long time retention are promoted; stability and safety are high; the preparation method is simple, and is convenient to control; and the preparation method is suitable for industrialized production.

Description

technical field [0001] The invention belongs to the technical field of cosmetics, and in particular relates to a high skin retention ceramide nanocomposite and its preparation method and application. Background technique [0002] The chemical name of ceramide is N-fatty acyl sphingosine, which is formed by the covalent combination of long-chain sphingosine and fatty acid through amide bond, in which the carbon chain length, degree of saturation and number of hydroxyl groups of sphingosine and fatty acid can vary. According to the difference of sphingosine and fatty acid chain in its structure, ceramide can be divided into ceramide Ⅰ, ceramide Ⅱ, ceramide ⅢA, ceramide ⅢB and ceramide Ⅵ. Among them, ceramide Ⅰ has the functions of repairing the sebum membrane, improving the barrier function of the skin surface, and reducing water loss; ceramide Ⅱ has the functions of balancing moisture and enhancing the skin's self-protection function; ceramide ⅢA has long-term moisturizing ef...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K8/86A61K8/63A61K8/55A61K8/42A61K8/37A61K8/34A61Q19/00
CPCA61K8/342A61K8/37A61K8/42A61K8/553A61K8/63A61K8/86A61K2800/413A61K2800/49A61K2800/591A61Q19/00
Inventor 刘卫许琦郭凤凤杨达峰
Owner WUHAN BEST CARRIER NANO TECH
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