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Novel macromolecule liposome and preparation method thereof

A polymer and liposome technology, applied in the field of medicine, can solve the problems of limited application and large cell toxicity, and achieve the effect of low cytotoxicity, good stability and high yield

Inactive Publication Date: 2012-07-11
TIANJIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

But owing to containing a large amount of amino groups on the molecular chain of lysine chitosan stearyl quaternary ammonium salt, the polymer liposome of preparation has very strong electropositive property, thereby makes it have very big cytotoxicity, limits its application

Method used

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  • Novel macromolecule liposome and preparation method thereof
  • Novel macromolecule liposome and preparation method thereof
  • Novel macromolecule liposome and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Synthesis of γ-polyglutamic acid stearyl quaternary ammonium salt. Take 2g of γ-polyglutamic acid and 50g of dimethylglycidyl octadecyl ammonium chloride into a four-necked flask, add 150mL of isopropanol to the flask, stir magnetically, heat to 50°C, condense and reflux Reaction for 3 days. After the reaction, the product was evaporated using a rotary evaporator to distill the isopropanol out, and then the product was placed in a dialysis bag of 8000-14000 for 7 days, the lower layer of gel was removed, filtered and lyophilized to obtain γ-polyglutamic acid Octadecyl quaternary ammonium salt. Such as figure 1 Infrared analysis test results show that 3,398.90 peaks have broad bands, which are the result of -OH hydrogen bonding; 1,639.41 peaks prove that the sample contains -NH-CO-, derived from γ-polyglutamic acid; 1073.37 peaks It proves that the tested sample contains -CO- and is ester; and the peak at 721.48 proves that the sample contains (CH 2 ) n (n≥4), derived...

Embodiment 2

[0035] Synthesis of γ-polyglutamic acid stearyl quaternary ammonium salt. Take 4g of γ-polyglutamic acid and 150g of dimethylglycidyl octadecylammonium chloride into a four-necked flask, add 200mL of isopropanol to the flask, stir magnetically, heat to 60°C, condense and reflux Reaction for 5 days. After the reaction, the product was evaporated using a rotary evaporator to distill the isopropanol out, and then the product was placed in a dialysis bag of 8000-14000 for dialysis for 3 days, the lower layer of gel was removed, filtered and lyophilized to obtain γ-polyglutamic acid Octadecyl quaternary ammonium salt.

Embodiment 3

[0037] Synthesis of γ-polyglutamic acid stearyl quaternary ammonium salt. Take 4g of γ-polyglutamic acid and 200g of dimethylglycidyl octadecylammonium chloride into a four-necked flask, add 250mL of isopropanol to the flask, stir magnetically, heat to 70°C, condense and reflux Reaction for 1 day. After the reaction is over, use a rotary evaporator to distill the isopropanol out, then put the product into a dialysis bag of 8000-14000 for 10 days, remove the lower layer of gel, filter and freeze-dry to obtain γ-polyglutamic acid Octadecyl quaternary ammonium salt.

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Abstract

The invention relates to a novel macromolecule liposome and a preparation method thereof. The preparation method comprises the steps of: preparing an amphiphilic macromolecule gamma-polyglutamate octadecyl alkylammonium salt through the reaction of dimethyl glycidyl octadecyl ammonium chloride with gamma-polyglutamate; and secondly, dissolving the gamma-polyglutamate octadecyl alkylammonium salt and cholesterol into dichloromethane according to different mass ratios, and preparing the macromolecule liposome according to a reverse-phase evaporation process or film dispersing process. Compared with the traditional product and the prior art, the invention has the characteristic of simple preparation process and is suitable for industrialized production. The prepared product has the characteristics of uniform and controllable particle diameter, effective particle diameter of 70-130nm, Zeta potential of 6-8mV, good preparation stability, simple preparation process and the like.

Description

Technical field [0001] The invention relates to a novel polymer liposome and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Liposomes are composed of phospholipids or other lipid compound bilayer membranes. When amphiphilic molecules such as phospholipids and sphingolipids are dispersed in the water phase, the hydrophobic tails of the molecules tend to gather together and avoid the water phase. The hydrophilic head is exposed to the water phase to form a closed vesicle with a bilayer structure. Liposomes are currently one of the common preparation methods used as drug gene carriers. However, conventional liposomes prepared from traditional lecithin and cholesterol are mostly swallowed by the reticuloendothelial system (RES) in the body and have a shorter residence time in the blood circulation. In addition, its physical and chemical stability is poor, fusion and aggregation are prone to occur during storage and applicat...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K47/34C08G69/48C08G69/10
Inventor 常津王生苏文雅王汉杰廖振宇
Owner TIANJIN UNIV
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