Graft polymer, and preparation method and use thereof

A technology of grafted polymers and products, which can be used in pharmaceutical formulations, medical preparations of non-active ingredients, etc., and can solve problems such as poor hydrophilicity, reduced compatibility, and reduced degradation rate.

Inactive Publication Date: 2013-03-06
THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it is poorly hydrophilic and has high crystallinity, which reduces their degradation rate and leads to a decrease in compatibility with soft organs. An effective way to overcome these problems is to introduce biocompatibility into aliphatic polyester segments. The segment with good blood compatibility can greatly improve the performance of aliphatic polyester

Method used

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  • Graft polymer, and preparation method and use thereof
  • Graft polymer, and preparation method and use thereof
  • Graft polymer, and preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0066] Synthesis of chitosan-polylactic acid-dipalmitoylphosphatidylethanolamine graft copolymer

[0067] (1) Disperse 10g of chitosan (molecular weight: 200,000) in water and heat to 75°C. 7ml of 30% H was added dropwise with stirring 2o 2 , Reaction 2h. Cool and filter. Part of the water in the filtrate was rotary evaporated, then precipitated in absolute ethanol, and left overnight. Suction filtration is then obtained to obtain pale yellow soluble chitosan.

[0068] Add 1 g of dried soluble chitosan into 25 ml of dimethyl sulfoxide, and disperse for 1 h, in which nitrogen is passed through for 0.5 h, and vacuum is pumped for 0.5 h. 20 g of lactide (Alfar Aesar company, 97%, analytically pure) was added to the chitosan solution, and dispersed for 1 h under nitrogen protection. Then add 1.5ml of triethylamine, under the protection of nitrogen, react at 85°C for 10h, then precipitate with 300ml of water, wash with water 4 times, dry in a vacuum oven for 24 hours, then ex...

Embodiment 2

[0086]Synthesis of Chitosan-Polyglycolide-Dioleoylphosphatidylethanolamine Copolymer

[0087] (1) Disperse 10g of chitosan (molecular weight: 200,000) in water and heat to 75°C. 7ml of 30% H was added dropwise with stirring 2 o 2 , Reaction 2h. Cool and filter. Part of the water in the filtrate was rotary evaporated, then precipitated in absolute ethanol, and left overnight. Suction filtration is then obtained to obtain light yellow soluble chitosan.

[0088] Add 1 g of dried soluble chitosan into 4 ml of dimethyl sulfoxide, and disperse for 1 h, in which 0.5 h is passed through nitrogen, and 0.5 h is vacuumized. 1 g of glycolide (Alfar Aesar company, 97%, analytically pure) was added to the chitosan solution, and dispersed for 1 h under nitrogen protection. Add 0.1ml of triethylamine, under the protection of nitrogen, react at 70°C for 10h, then precipitate with 300ml of water, wash with water 4 times, dry in a vacuum oven for 24 hours, and then extract with toluene (30...

Embodiment 3

[0094] Synthesis of chitosan-polycaprolactone-distearoylphosphatidylethanolamine graft copolymer

[0095] (1) Disperse 10g of chitosan (molecular weight: 200,000) in water and heat to 75°C. 7ml of 30% H was added dropwise with stirring 2 o 2 , Reaction 2h. Cool and filter. Part of the water in the filtrate was rotary evaporated, then precipitated in absolute ethanol, and left overnight. Suction filtration is then obtained to obtain light yellow soluble chitosan.

[0096] Add 1 g of dried soluble chitosan into 100 ml of dimethyl sulfoxide, and disperse for 1 h, in which nitrogen is passed through for 0.5 h, and vacuum is pumped for 0.5 h. Add 30 g of caprolactone (Alfar Aesar company, 97%, analytically pure) into the chitosan solution, and disperse for 1 h under nitrogen protection. Add 5ml of triethylamine, under the protection of nitrogen, react at 85°C for 15h, then precipitate with 300ml of water, wash with water 4 times, dry in a vacuum oven for 24 hours, and then ex...

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Abstract

The invention provides a chitosan-aliphatic polyester-phosphatidylethanolamine graft polymer, and a preparation method and a use thereof. The structural formula of the graft polymer is represented by formula (I) shown in the specification. The chitosan-aliphatic polyester-phosphatidylethanolamine graft polymer provided by the invention simultaneously comprises a hydrophilic part and a hydrophobic part. Chitosan has a biological degradability and hydrophilicity, and aliphatic polyester and phosphatidylethanolamine have the hydrophobicity, so the nanometer micelle of the amphiphilic chitosan-aliphatic polyester-phosphatidylethanolamine graft polymer has the advantages of effective prolongation of the drug effect, toxicity reduction, and improvement of the biological availability and the biological activity as a drug carrier. The formula (I) is shown in the description.

Description

technical field [0001] The invention relates to a graft polymer and its preparation method and use, in particular to a chitosan-aliphatic polyester-phosphatidylethanolamine graft polymer, its preparation method and its use as a drug carrier. Background technique [0002] Chitosan, whose scientific name is β-(1,4)-2-amino-2-deoxy-D-glucose, is the deacetylation product of chitin, and is the second most abundant hydrophilic polysaccharide in nature. The solubility of chitosan is greatly improved compared with chitin, and its chemical properties are more active. Chitosan is soluble in most dilute acids (such as hydrochloric acid, acetic acid, benzoic acid) to form salts, which are often called soluble chitin. Chitosan has biodegradability, biocompatibility, bioadhesion and permeability-enhancing effects, and has almost no toxic side effects (Agnihotri, S.J., Controlled Release, 2004, 100, 5.). Chitosan has anti-tumor and anti-cancer effects. Chitosan can filter white blood c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G63/91C08B37/08A61K47/36
Inventor 吴雁陈春英李敏苏世帅孙云
Owner THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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