包埋紫杉醇的Pluronic P85/聚乳酸纳米粒子制备及体外释放行为考察  

Preparation and in vitro Release Behavior of Paclitaxel-Loaded Pluronic P85 /Polylactic Acid Nanoparticles

作　　者：李资玲[1] 熊向源[1] 龚妍春[1] 李玉萍[1] 

机构地区：[1]江西科技师范大学生命科学学院,南昌330013

出　　处：《中国实验方剂学杂志》2014年第1期1-4,共4页Chinese Journal of Experimental Traditional Medical Formulae

基　　金：国家自然科学基金项目(21264009;81060264);江西省教育厅科学技术研究项目(GJJ10594);人事部留学人员科技活动项目([2010]412)

摘　　要：目的:制备包埋紫杉醇的Pluronic P85/聚乳酸(PLA-P85-PLA)纳米粒子并考察其形态及体外释放行为。方法:采用本体聚合法合成PLA-P85-PLA嵌段共聚物,透析法制备PLA-P85-PLA纳米粒子,UV测定包封率及载药量,HPLC测定紫杉醇的体外释放行为,MTT测定纳米粒子的生物相容性。HPLC条件为流动相乙腈-PBS(50∶50),检测波长227 nm。结果:包埋紫杉醇的PLA-P85-PLA纳米粒子粒径140 nm,包封率56%,载药量9.4%,体外释放在前20 h呈快速释放形式,接着在长达近4 d的时间内呈现缓慢释放,且仅约12%被包埋的紫杉醇释放出来,包埋紫杉醇的PLA-P85-PLA纳米粒子处理的OVCAR-3细胞存活率(41%)明显低于空白紫杉醇(70%)。结论:PLA-P85-PLA嵌段共聚物是良好的药物载体,可用于包埋疏水性强的抗癌药物。Objective： To prepare paclitaxel-loaded Pluronic P85/polylactic acid （PLA-P85-PLA） nanoparcticles, then investigate its morphology and in vitro release behavior. Method： PLA-P85-PLA block copolymer was synthesized by bulk polymerization, PLA-P85-PLA nanoparcticles were prepared by dialysis method, encapsulation efficiency and drug loading capacity were determined by UV, in vitro release behavior of paclitaxel-loaded PLA-P85-PLA nanoparticles was determined by HPLC, biocompatibility of nanoparticles was measured by MTT. HPLC conditions were as follows： mobile phase of acetonitrile-PBS solution （50： 50）, detection wavelength at 227 rim. Result： Particles size of paclitaxel-loaded PLA-P85-PLA nonoparticles was 140 rim, encapsulation efficiency and drug loading capacity were 56% and 9.4%, respectively; In vitro release of these prepared nonoparticles in the first 20 h was a rapid release form, followed by a slow release form within nearly 4 d and only about 12% of entrapped paclitaxel released, cell survival rate of OVCAR-3 treated by paclitaxel-loaded PLA-P85-PLA nanoparcticles （41%） was lower than free paclitaxel （70%）. Conclusion： PLA-P85-PLA block copolymer was a good drug carrier for embedding drug with low solubility.

关 键 词：紫杉醇 PLURONIC P85 纳米粒子 体外释放行为 高效液相色谱 细胞存活率 细胞毒性试验 

分 类 号：R944.2[医药卫生—药剂学] R283.6[医药卫生—药学]