紫杉醇两亲性嵌段键合物胶束的研究Study on the micell of mPEG-PLA-paclitaxel block copolymer conjugates
杜坡,崔福德,李汉蕴,景遐斌
DU Po1,CUI Fu-de1,LI Han-yun2,JING Xia-bin3(1.School of Pharmacy
摘要(Abstract)：
目的对聚乙二醇单甲醚-聚乳酸-紫杉醇(mPEG-PLA-PTX)两亲性嵌段键合物进行研究。方法采用溶剂蒸发法制备键合物胶束,动态光散射法(DLS)测定粒径,扫描电子显微镜(SEM)表征形态,考察键合物中mPEG、PLA的相对分子质量分别对胶束粒径、临界胶束浓度(CMC)和体外释放的影响。结果胶束呈壳-核结构,粒径为纳米级,键合物疏水段PLA相对分子质量增加,胶束粒径增大,CMC下降,体外释放速度减慢;键合物亲水段mPEG相对分子质量增加,胶束粒径变化不大,CMC上升,体外释放速度加快。键合物胶束体外释药遵从一级动力学,不存在突释现象。结论mPEG-PLA-PTX可以形成胶束,体外释药遵从一级动力学,为进一步研究两亲性嵌段键合物提供了依据。
Objective To investigate the micell of mPEG-PLA-paclitaxel(mPEG-PLA-PTX) block copolymer conjugates.Methods The micell of mPEG-PLA-PTX was prepared by solvent evaporation method;the average size and size distribution were determined by dynamic light scattering(DLS).The morphology was characterized by scanning electron microscopy(SEM).The influence of mPEG and PLA on size distribution,critical micell concentration(CMC) and drug release profile were investigated.Results The micell was sized in nano-levels and shaped spherically with core and shell.The size of the micell was increased,CMC was reduced and the drug release was decreased with the increase of the molecular weight of the hydrophobic segment(PLA);reversely,the size of the micell was almost constant,CMC was increased and the drug release was risen with the increase of the molecular weight of the hydrophilic segment(mPEG).The micell of block copolymer conjugates releases drugs followed the rule of first order equation and had no burst effect.Conclusions mPEG-PLA-PTX micell is produced successfully and the drug release is revealed under the rule of first order equation.It provides an experiment basis for the development of mPEG-PLA-PTX block copolymer conjugates.
关键词(KeyWords)：
紫杉醇;胶束;嵌段键合物;体外释放
paclitaxel;micell;block copolymer conjugate;in vitro release
基金项目(Foundation):
作者(Author):
杜坡,崔福德,李汉蕴,景遐斌
DU Po1,CUI Fu-de1,LI Han-yun2,JING Xia-bin3(1.School of Pharmacy
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