超临界CO2抗溶剂法制备紫杉醇缓释微球

采用超临界流体强制分散溶液技术,以D,L-聚乳酸和D,L-聚乳酸-聚乙二醇共聚物为载体材料,分别制备了紫杉醇缓释微球.通过扫描电镜、激光粒度仪检测微球外形及粒径分布;紫外吸光度法测量其载药量和包封率,恒温振荡透析法检测药物的体外释放性能;MTT法检测载药微球对Hela细胞的抑制作用.实验表明,两种载体的缓释微球球形度均较好,表面光滑,平均粒径较小,且粒径分布较窄.以聚乳酸和共聚物为载体的缓释微球载药量分别为5.4%±0.3%和5.3%±0.4%,包封率分别为51%±3%和45%±3%;药物释放呈缓释模式,共聚物载药微球药物释放速率较快.MTT法检测结果表明,载药微球对Hela细胞的增殖有明显抑制,共聚物载药微球对细胞增殖抑制更为明显.

Preparation of paclitaxel loaded microparticles by supercritical CO2 anti-solvent precipitation

Paclitaxel loaded microparticles were prepared via solution-enhanced dispersion by supercritical CO2 (SEDS) technique, using poly(D, L-lactide) and poly(D, L-lactide)-polyethylene glycol-poly(D, L-lactide) as matrix. SEM showed that P(D, L)LA and P(D, L)LA-PEG-P(D, L)LA microparticles loaded or without PTX all exhibited rather spheri-cal shape and small particles size with narrow particle size distribution. The drug loading and encapsulation efficiency of PTX/P(D, L) LA mieroparticles were 5.4 % ± 0.3 % and 51% ± 3% ; while PTX/P(D, L) LA-PEG-P( D, L) LA microparti-cles were 5. 3 % ± 0. 4% and 45 % ± 3 %, respectively. In vitro release of paclitaxel from these drug loaded microparticles exhibited sustained release model, encapsulated drug in the P(D, L)LA-PEG-P(D, L)LA copolymer microparticles release faster than PTX loaded P(D, L)LA microparticles. In vitro cytotoxicity evaluation of drug loaded microparticles against cervix cancer Hela cell line indicated that the drug loaded microparticles, especially drug loaded P(D, L)LA-PEG-P(D, L) LA copolymer microparticles, had superior anti-proliferation activity against the Hela cell line compared with free PTX for-mulation.