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Co-supported polymer micelle and application thereof in pharmacy

A technology of polymer glue and amphiphilic polymer is applied to polymer micelle and its application in pharmaceuticals, which can solve the problems of large toxic and side effects, low bioavailability, poor water solubility, etc., to avoid toxic and side effects, The effect of improving solubility and improving bioavailability

Inactive Publication Date: 2017-07-21
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, most of these free drugs have defects such as poor water solubility, high toxicity and side effects, and low bioavailability, which greatly affect the therapeutic effect of the pharmaceutical composition on tumors.

Method used

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  • Co-supported polymer micelle and application thereof in pharmacy
  • Co-supported polymer micelle and application thereof in pharmacy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Take 0.1mmol of hyaluronic acid, 0.3mmol of (1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride) and 0.3mmol of N-hydroxyl sulfosuccinimide solution In 10mL formamide, activate at room temperature for half an hour. Dissolve 0.2mmol of octadecylamine in 5mL of N.N-dimethylformamide, drop it into the activated hyaluronic acid solution, continue to react for 24h, use acetone to precipitate the product, redissolve the precipitate with 20mL of distilled water, and place Dialyze in a dialysis bag (MWCO=3500) for 2 days, and freeze-dry to obtain hyaluronic acid-octadecylamine polymer micelles.

Embodiment 2

[0033] Dissolve 0.1mmol of dextran, 0.2mmol of deoxycholic acid and 10mg of 4-dimethylaminopyridine in 10mL of dimethyl sulfoxide. After reacting for 24 hours at room temperature, the product was precipitated with ethanol, and the precipitate was washed with 20mL of distilled water. Reconstituted, placed in a dialysis bag (MWCO=3500) for dialysis for 2 days, and freeze-dried to obtain dextran-deoxycholic acid polymer micelles.

Embodiment 3

[0035] Get 0.1mmol of chitosan, 0.2mmol of succinic anhydride, 0.3mmol of (1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride) and 0.3mmol of N-hydroxy Thiosuccinimide was dissolved in 10 mL of dimethyl sulfoxide, and after 24 hours of reaction, the product was precipitated with acetone. The precipitate was dissolved in 20 mL of distilled water, dialyzed in a dialysis bag (MWCO=3500) for 2 days, and obtained after lyophilization. Chitosan intermediate with free carboxyl group. Dissolve 0.1mmol of chitosan intermediate and 0.4mmol of octylamine in water and methanol (v / v=1:1), 0.3mmol of (1-(3-dimethylaminopropyl)-3-ethyl Carbodiimide hydrochloride) and 0.3 mmol of N-hydroxyl sulfosuccinimide as a catalyst, reacted for 24h. The methanol was removed by rotary evaporation, placed in a dialysis bag (MWCO=3500) for dialysis for 2 days, and the chitosan-octylamine polymer micelles were obtained after freeze-drying.

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Abstract

The invention belongs to the field of pharmaceutical preparations and discloses co-supported polymer micelle and application thereof in pharmacy. The co-supported polymer micelle employs an amphiphilic polymer as a micelle support to co-support silybin and chemotherapeutic drugs. The polymer micelle preparation is self-assembled in an aqueous solution to form nanoparticles, co-supporting silybin and chemotherapeutic drugs; a tumor part is targeted through intravenous injection, and the drugs are released in sync. Silybin is used to control a tumor micro-environment, the effects of the chemotherapeutic drugs are sensitized, and collaborative treatment is achieved for tumors.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a co-loaded drug polymer micelle and its application in pharmacy, in particular to a polymer micelle co-loaded with silybin and chemotherapeutic drugs and its application in pharmacy. Background technique [0002] Tumor microenvironment (TME), that is, the internal environment in which tumor cells are produced and lived, includes not only tumor cells themselves, but also various cells such as tumor-associated fibroblasts, immune, inflammatory cells, and glial cells around them. It also includes the intercellular matrix, microvessels, and biomolecules infiltrated in the adjacent area. In the past, people's treatment of tumors always limited their thinking to the tumor cells themselves. Until recently, most studies have found that the tumor and the tumor microenvironment are an inseparable whole. The tumor microenvironment is like a small ecological environment, which is ...

Claims

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Application Information

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IPC IPC(8): A61K31/357A61K31/337A61K31/704A61K33/24A61K9/107A61K47/36A61P35/00
CPCA61K31/357A61K9/1075A61K31/337A61K31/704A61K33/24A61K47/36A61K2300/00
Inventor 霍美蓉周建平蔡汉殷婷婕
Owner CHINA PHARM UNIV
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