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Use of micelles formed by polyethylene glycol derivatives in cosmetics

A polyethylene glycol, polyethylene glycol group technology, applied in cosmetics, cosmetic preparations, medical preparations containing active ingredients, etc., can solve the problem that the distribution and number of hydrophobic chains are difficult to precisely control, and reduce tissue penetration. , affecting the precise regulation of the kinetics of hydrophobic compounds, etc.

Active Publication Date: 2020-09-25
天津力博生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, a large number of lipophilic and hydrophilic groups make the size of the block copolymer polymer micelles larger, and the hydration radius can reach more than 100nm, which reduces the tissue penetration
Moreover, it is difficult to precisely control the distribution and number of hydrophobic chains in the copolymer, which affects the precise adjustment of the release kinetics of hydrophobic compounds.

Method used

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  • Use of micelles formed by polyethylene glycol derivatives in cosmetics
  • Use of micelles formed by polyethylene glycol derivatives in cosmetics
  • Use of micelles formed by polyethylene glycol derivatives in cosmetics

Examples

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preparation example Construction

[0110] The preparation method of above-mentioned polyethylene glycol derivative, described method comprises the steps:

[0111] (a) phospholipid compound, (b) polyethylene glycol PEG-(Y) with Y terminal group n , and optionally (c) fatty chain-containing compound R 4 -X 1 Mix and react to obtain the polyethylene glycol derivative.

[0112] In one embodiment of the present invention, the above raw materials are mixed in a solvent, for example, the solvent is selected from N,N-dimethylformamide.

[0113] In one embodiment of the present invention, described method comprises the steps:

[0114] (1) (a) phospholipid compound and optional (c) fatty chain-containing compound R 4 -X 1 Dissolved in a solvent to obtain a mixed solution A;

[0115] (2) the polyethylene glycol PEG-(Y) whose end group is Y in (b) n Dissolved in a solvent to obtain a mixed solution B;

[0116] (3) Mix the mixed solution A and the mixed solution B, and react at room temperature to prepare the polyet...

preparation example 1 3

[0132] Preparation Example 1 The synthesis of three aliphatic chain-polyethylene glycol derivatives (1DSPE, 1 n-octadecyl mercaptan)

[0133] Weigh 50 mg of DSPE in a 10 mL round-bottom glass flask, dissolve it in 100 μL of N,N-dimethylformamide, and add 12 μL of diisopropylethylamine to obtain a solution (1).

[0134] Take by weighing 334mg end group substituted polyethylene glycol OPSS-PEG5000-SCM (average molecular weight 5000Da, end group is the polyethylene glycol of dithiopyridyl and succinimide carboxymethyl ester respectively with 2 milliliters weighing bottle, (purchased from Beijing Jiankai Technology Co., Ltd., product number A5109), and dissolved in 400 μL DMF to obtain solution (2).

[0135]The solution (2) was added into the round-bottomed flask with the solution (1) for mixing, stirred by magnetic force, and reacted at room temperature for 4 hours under the protection of nitrogen. Thereafter, nitrogen protection was removed, and 100 μL of 0.5 M hydrochloric aci...

preparation example 2 3

[0137] Preparation Example 2 The synthesis of three aliphatic chain-polyethylene glycol derivatives (1DSPE, 1 n-octyl mercaptan)

[0138] Weigh 50 mg of DSPE in a 10 mL round bottom glass flask, dissolve it in 100 μL of DMF, add 12 μL of diisopropylethylamine to obtain solution (1).

[0139] Take by weighing 334mg end group substituted polyethylene glycol MAL-PEG5000-SCM (average molecular weight 5000Da, end group is respectively the polyethylene glycol of maleimide and succinimide carboxymethyl ester) with 2 milliliter weighing bottle , purchased from Beijing Jiankai Technology Co., Ltd., product number A5003), which was dissolved in 400 μL DMF to obtain solution (2).

[0140] Add 15 μL of 1-octanethiol (molecular weight 146, purchased from Beijing Bailingwei Technology) to solution (2), and react for 1 hour under nitrogen protection. The obtained reaction liquid was added into the round bottom flask with solution (1) for mixing, stirred by magnetic force, and reacted under ...

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Abstract

The invention relates to a use of micelles formed by polyethylene glycol derivatives in cosmetics, and belongs to the technical field of lipid molecules. The polyethylene glycol derivatives can be dispersed in a solvent to form micelles, and the micelles can be used to efficiently package, deliver, and release effective ingredients of cosmetics. The micelles formed by the polyethylene glycol derivatives have high tissue penetration, long-term stability and controllable release performance. In particular, the polyethylene glycol derivatives contain a phospholipid structure, so that the polyethylene glycol derivatives have outstanding biocompatibility.

Description

technical field [0001] The invention relates to the use of micelles formed by polyethylene glycol derivatives in cosmetics, and belongs to the technical field of lipid molecules. Background technique [0002] The effective ingredients of cosmetics include natural products such as vitamins, lipids, amino acids, polypeptides, proteins, and polysaccharide biomacromolecules, as well as other synthetic functional compounds. They have different solubility in water. In order to improve the skin care effect, active ingredients that are difficult to dissolve in water need to be solubilized by appropriate methods. Ceramide and sphingomyelin are the main components of the cell phospholipid bilayer, distributed in all layers of the skin including the dermis, and have a high content in the stratum corneum of human skin. With the growth of age, the content of ceramide in the stratum corneum of the human body decreases, and an appropriate amount of supplement is needed to maintain the hea...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K8/86A61K8/04A61K8/02A61K8/19A61K8/31A61K8/35A61K8/368A61K8/67A61K8/68A61Q19/00
CPCA61K8/86A61K8/04A61K8/042A61K8/0216A61K8/68A61K8/31A61K8/671A61K8/67A61K8/678A61K8/368A61K8/35A61K8/19A61Q19/00A61K2800/56A61K2800/10
Inventor 王晓
Owner 天津力博生物科技有限公司
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