紫杉醇载药胶束的制备及体外评价  

The preparation and in vitro evaluation of paclitaxelloaded polymeric micelles

作　　者：曾剑夫 乔明曦[1] 宏伟[1] 胡海洋[1] 赵秀丽[1] 陈大为[1] 

机构地区：[1]沈阳药科大学药学院,辽宁沈阳110016

出　　处：《沈阳药科大学学报》2015年第1期1-6,共6页Journal of Shenyang Pharmaceutical University

摘　　要：目的以胆酸修饰的聚乙二醇单甲醚-聚丙交酯-胆酸(m PEG-PDLLA-CA)聚合物为载体材料,制备紫杉醇载药胶束,并对载药胶束的处方和工艺进行优化。方法采用芘荧光法测定m PEGPDLLA-CA聚合物的临界胶束质量浓度,薄膜分散法制备紫杉醇载药胶束,以包封率和载药量为指标,应用Box-Behnken设计效应面法优化胶束的制备工艺。结果在优化条件下制备的载药胶束平均粒径为(54.35±1.80)nm,包封率为(92.74±0.64)%,载药量为(24.05±0.16)%,载药胶束在室温条件放置48 h,载药量无显著变化,制剂稳定性良好。结论用Box-Behnken设计效应面法优化紫杉醇载药聚合物胶束的制备工艺,该载药胶束物理稳定性良好,具有广阔的应用前景。Objective To optimize the preparation process of paclitaxel-loaded poly （ ethylene glycol） me- thoxy-poly （ D, L-lactide） -cholic acid （mPEG-PDLLA-CA） micelles. Methods The CMC value of the copol- ymer micelles was determined by fluorescent method. The polymer micelles containing paclitaxel were pre- pared by the thin-film dispersion method. The preparation process for incorporating paclitaxel into mPEG- PDLLA-CA micelles was optimized by the Box-Behnken design-response surface method with entrapment efficiency and drug loading content as indexes. The mean diameter and particle size distribution（PDI） of the drug loaded micelles were determined by dynamic light scattering method. Results The paclitaxel-loaded mi- celles prepared according to the optimized results showed average particle size of（54.35 ± 1.8 ） nm, entrap- ment efficiency of（ 92. 74 ±0. 64 ） % and drug loading of（ 24. 05 ± 0. 16 ） %, respectively. The paclitaxel- loaded polymeric micelles revealed better stability at room temperature and slower drug release than the mPEG-PDLLA micelles. Conclusions The preparation process of paclitaxe-loaded mPEG-PDLLA-CA mi- celles has been optimized by Box-Behnken design-response surface method. The drug-loaded micelles have been demonstrated has good stability which is promising in the paclitaxel delivery for clinical therapy in the future.

关 键 词：BOX-BEHNKEN效应面法 聚乙二醇单甲醚-聚丙交酯-胆酸 聚合物胶束 物理稳定性 

分 类 号：R94[医药卫生—药剂学]