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Polymer liposomes based on polyamino acid and quaternary ammonium salt and preparation method for polymer liposomes

A polyamino acid and polymer technology, applied in the field of medicine, can solve the problems of easy fusion and aggregation, short residence time, and poor physical and chemical stability during storage and application, and achieve the effects of short preparation cycle, simple operation, and low cost

Active Publication Date: 2012-11-28
南通药享科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, conventional liposomes prepared from traditional lecithin and cholesterol are mostly swallowed by the reticuloendothelial system in the body, and the residence time in the blood circulation is relatively short.
Moreover, its physical and chemical stability is poor, and it is prone to fusion and aggregation during storage and application.

Method used

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  • Polymer liposomes based on polyamino acid and quaternary ammonium salt and preparation method for polymer liposomes
  • Polymer liposomes based on polyamino acid and quaternary ammonium salt and preparation method for polymer liposomes
  • Polymer liposomes based on polyamino acid and quaternary ammonium salt and preparation method for polymer liposomes

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Synthesis of polyglutamic acid octadecyl quaternary ammonium salt. Take 2g of polyglutamic acid and 50g of dimethylglycidyloctadecylammonium chloride into a four-necked flask, add 200mL of isopropanol into the flask, stir with magnetic force, heat to 70°C, condense and reflux for 3 sky. After the reaction, use a rotary evaporator to distill the isopropanol out of the product, then place the product in a dialysis bag at 8000-14000 for dialysis for 7 days, remove the lower layer of gel, filter and lyophilize, and obtain polyglutamic acid octadecamate Alkyl quaternary ammonium salt. Such as figure 1 As shown in the nuclear magnetic resonance analysis test results, the appearance of Ha, Hc, Hd, and Hf peaks proves that the long chain of quaternary ammonium salt is successfully connected to the main chain of polyglutamic acid, and proves that the synthesis of polyglutamic acid octadecyl quaternary ammonium salt is successful.

Embodiment 2

[0037] Synthesis of polylysine octadecyl quaternary ammonium salt. Take 4g of polylysine and 150g of dimethylglycidyloctadecylammonium chloride into a four-neck flask, add 250mL of isopropanol into the flask, stir with magnetic force, heat to 50°C, condense and reflux for 5 sky. After the reaction, use a rotary evaporator to distill the isopropanol out of the product, then place the product in a dialysis bag at 8000-14000 for dialysis for 3 days, remove the lower layer of gel, filter and freeze-dry to obtain polylysine octadecadecane Alkyl quaternary ammonium salt.

Embodiment 3

[0039] Synthesis of polyarginine octadecyl quaternary ammonium salt. Take 4g of polyarginine and 200g of dimethylglycidyloctadecylammonium chloride into a four-neck flask, add 150mL of isopropanol into the flask, stir with a magnetic force, heat to 30°C, condense and reflux for 1 sky. After the reaction, use a rotary evaporator to distill the isopropanol out of the product, then place the product in a dialysis bag of 8000-14000 for dialysis for 10 days, remove the lower layer of gel, filter and lyophilize, and obtain polyarginine octadecyl Alkyl quaternary ammonium salt.

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Abstract

The invention relates to polymer liposomes based on polyamino acid and quaternary ammonium salt and a preparation method for the polymer liposomes. The preparation method comprises the following steps of: reacting dimethyl epoxypropyl octadecyl ammonium chloride with polyamino acid to obtain amphiphilic polymer polyamino acid octodecyl quaternary ammonium salt; and dissolving the amphiphilic polymer polyamino acid octodecyl quaternary ammonium salt and cholesterol in dichloromethane in different mass ratios, and preparing the polymer liposomes by using a reverse-phase evaporation method or a film dispersion method. Compared with the conventional products and technologies, the invention has the characteristics that: the whole preparation process is simple, and suitable for industrial production; the prepared product has uniform and controllable grain size and the effective grain size of 50-200nm; and a preparation is high in stability, the preparation process is simple and the like.

Description

technical field [0001] The invention relates to a class of polymer liposomes based on polyamino acids and quaternary ammonium salts and a preparation method thereof, belonging to the technical field of medicines. Background technique [0002] Amphiphilic polymers refer to polymers that have both hydrophilic and lipophilic units in the same polymer. Amphiphilic polymers have many excellent properties, such as easy post-modification, special surface properties, and the ability to form micelles or microemulsions in certain solvents. Amphiphilic polymers have important applications in medicine. They can be used to manufacture biomedical materials such as artificial blood vessels, artificial skin, and heart valves. They can also be used as drug gene carriers by preparing amphiphilic polymers into micelles or polymer liposomes. , and can endow it with functions such as targeting, long circulation and sustained release. [0003] Liposome is currently one of the common preparation...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08G69/48C08G69/10A61K47/34A61K9/127
Inventor 常津王生苏文雅王汉杰康世胤
Owner 南通药享科技有限公司
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