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Preparation method and purpose of oxidation-reduction response chitosan-lipidosome

A chitosan and liposome technology, which can be used in liposome delivery, other methods of inserting foreign genetic materials, and medical preparations with inactive ingredients, etc. Application prospect, high biocompatibility, effect of improving biocompatibility and blood stability

Active Publication Date: 2017-11-28
DALIAN NATIONALITIES UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The liposome structure is easily damaged by components such as high-density lipoprotein in serum, resulting in the leakage of encapsulated drugs

Method used

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  • Preparation method and purpose of oxidation-reduction response chitosan-lipidosome
  • Preparation method and purpose of oxidation-reduction response chitosan-lipidosome
  • Preparation method and purpose of oxidation-reduction response chitosan-lipidosome

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034]Dissolve 0.5 g of chitosan (CSO) with a molecular weight of 5 kDa in 100 mL of water, and sonicate for 30 min to fully dissolve it. Under the stirring state, add the chitosan aqueous solution dropwise to the DMSO solution of dithiobisuccinimidyl propionate, and after reacting at 30°C for 2 hours, continue to drop 0.5 g of 1,2 -Ethanol solution of dioleoylphosphatidylethanolamine, reacted at 30°C for 2h, the reaction solution was rotary evaporated, dialyzed and freeze-dried to prepare redox responsive 1,2-dioleoylphosphatidylethanolamine chitosan.

[0035] Prepare a 1mg / mL redox response 1,2-dioleoylphosphatidylethanolamine chitosan aqueous solution, take 100uL, mix it with 1mL of DOTAP cationic liposomes containing SPIO by ultrasound, then let it stand for 1h, and then insert it into the In the way of assembly, liposomes are modified to obtain liposome drug carriers with redox-responsive chitosan brushes on the surface.

Embodiment 2

[0037] Dissolve 0.5 g of chitosan (CSO) with a molecular weight of 5 kDa in 100 mL of water, and sonicate for 30 min to fully dissolve it. Under the stirring state, add the chitosan aqueous solution dropwise to the DMSO solution of dithiobisuccinimidyl propionate, and after reacting at 30°C for 2 hours, continue to drop 0.5 g of 1,2 - An ethanol solution of distearoylphosphatidylethanolamine, reacted at 30° C. for 2 hours, and the reaction solution was rotary evaporated, dialyzed and freeze-dried to prepare redox-responsive 1,2-distearoylphosphatidylethanolamine chitosan.

[0038] Prepare a 1mg / mL redox response 1,2-distearoylphosphatidylethanolamine chitosan aqueous solution, take 100uL, mix it with 1mL of DOTAP cationic liposome containing SPIO by ultrasound, then let it stand for 1h, and then insert In the way of self-assembly, liposomes are modified to obtain liposome drug carriers with redox-responsive chitosan brushes on the surface.

Embodiment 3

[0040] Dissolve 0.5 g of chitosan (CSO) with a molecular weight of 5 kDa in 100 mL of water, and sonicate for 30 min to fully dissolve it. Under the stirring state, add the chitosan aqueous solution dropwise to the DMSO solution of dithiobisuccinimidyl propionate, and after reacting at 30°C for 2 hours, continue to drop 0.5 g of 1,2 -Ethanol solution of dilauroylphosphatidylethanolamine, reacted at 30°C for 2h, the reaction solution was rotary evaporated, dialyzed and freeze-dried to prepare redox responsive 1,2-dilauroylphosphatidylethanolamine chitosan.

[0041] Prepare a 1mg / mL redox response 1,2-dilauroylphosphatidylethanolamine chitosan aqueous solution, take 100uL, mix it with 1mL of DOTAP cationic liposomes containing SPIO by ultrasound, then let it stand for 1h, and then insert it into the In the way of assembly, liposomes are modified to obtain liposome drug carriers with redox-responsive chitosan brushes on the surface.

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Abstract

The invention provides a preparation method and a purpose of oxidation-reduction response chitosan-lipidosome. The method is characterized in that disulfide disuccinimidyl substituted ester is used for synthesizing oxidation-reduction response disulfide bond connected double-aliphatic-chain substituent group phosphatidyl ethanolamine-s-s-chitosan. The synthesized double-aliphatic-chain substituent group phosphatidyl ethanolamine chitosan is used for modifying lipidosome by a back insertion self assembly method; the double-aliphatic-chain substituent group phosphatidyl ethanolamine chitosan-lipidosome medicine carrier with oxidation-reduction response chitosan brushes on the surface is formed through assembly. The assembled chitosan-lipidosome has strong cell adhesion performance and antiserum capability, has the environment response performance at the same time, and is applicable to intravenous injection. The invention also provides application of superparamagnetic ferroferric oxide nanometer particles coated by the chitosan-lipidosome to medicine delivery. High medicine delivery efficiency and high biocompatibility are realized; wide application prospects are realized.

Description

technical field [0001] The present invention relates to a redox responsive chitosan-liposome drug carrier, in particular to a redox responsive double aliphatic chain substituent phosphatidylethanolamine chitosan and its construction and encapsulation with liposome superparamagnetic The invention relates to a drug carrier of iron ferric oxide nanoparticles, which belongs to the preparation method of a novel drug carrier in the field of drug delivery. Background technique [0002] A drug carrier refers to a system that can change the way a drug enters the human body and its distribution in the body, controls the release rate of the drug, and delivers the drug to the target organ. Drug carriers can effectively improve the utilization rate, safety and effectiveness of drugs through controlled release. Chitosan and liposomes are commonly used drug carriers. Chitosan has good biocompatibility and biodegradability. The 2-position amino group and the 6-position hydroxyl group are e...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08B37/08A61K47/69A61K47/61A61K41/00A61K49/18C12N15/88
CPCA61K41/00A61K49/1812A61K9/0009C12N15/88C08B37/003A61K47/6911A61K9/1272A61K9/1278A61K9/1277A61P35/00A61K9/1271
Inventor 张树彪陈会英马羽秦晓利蓝浩铭崔韶晖
Owner DALIAN NATIONALITIES UNIVERSITY
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