两亲性聚乙二醇接枝聚乳酸胶束的制备及特性  

Preparation and Characterization of Amphiphilic Polyethyleneglycol-graft-poly(lactic acid)(PPLA)Copolymer Micelles

作　　者：张晓喜[1] 潘君[1] 严好[1] 糜丽[1] 江伟民[1] 任慧卿[1] 王润光[1] 

机构地区：[1]重庆大学生物工程学院生物材料与仿生工程研究中心,重庆400044

出　　处：《精细化工》2010年第6期584-588,共5页Fine Chemicals

基　　金：国家自然科学基金资助项目(30870609);重庆市自然科学基金重点资助项目(CSTC2009BA4025)~~

摘　　要：制备聚乙二醇接枝聚乳酸(PPLA)聚合物胶束,探讨其作为药物载体的可行性和稳定性。溶剂挥发法制备PPLA胶束并对其表征。萘普生为模型药物,单因素考察了投药量、丙酮用量、加样顺序对包封率的影响。结果表明,PPLA临界胶束质量浓度(CMC)低,为3×10-4g/L;胶束呈球形、平均粒径小于200nm;在室温、稀释、碱性条件下稳定;最佳载药条件为:材料与药物同时溶于丙酮后滴入水中、丙酮与水的体积比1∶10,萘普生与PPLA质量比0.8∶10,PPLA胶束质量浓度1.0g/L。37℃时载药胶束在磷酸盐缓冲液(PBS)中可缓慢持续释放5d以上。结果证明,制备的聚乙二醇接枝改性聚乳酸聚合物胶束可用作疏水性药物的缓释给药载体。A new polymer namely polyethyleneglycol-graft-poly（lactic acid）（PPLA）polymeric micelle was prepared and explore for its potential application to drug delivery.The rotary evaporation method was applied for the preparation graft copolymer micelle which was characterized.With naproxen as the model drug,the effect of several factors including acetone volume,naproxen feed amount and the additional sequence of material were investigated on the entrapment efficiency by single-factorial experiments.The critical micelle concentration was 3×10-4 g/L.Distributing in a narrow range,the spherical-shaped micelle＇s average particle diameter was under 200 nm.The micelle also presented a certain stability when diluted,standing and alkaline change to basic condition at room temperature.The optimum preparation procedure was as follows：after simultaneously dissolved in acetone,naproxen and PPLA were dropped into water,while volume ratio between acetone and water and the weight ratio between naproxen and PPLA were respectively 1∶10 and 0.8∶10,PPLA micelle concentration 1.0 g/L.In PBS duration release could be up to 5 days at 37 ℃.Thus,PPLA could be considered as a novel applied polymer carriers in the promising drug delivery system for hydrophobic drugs.

关 键 词：聚乙二醇接枝聚乳酸 胶束 自组装 萘普生 医药原料 

分 类 号：R944.1[医药卫生—药剂学]