中文摘要：

背景：目前研究的大部分高分子药物载体没有靶向性,在应用上有局限性,只有几个国外课题组报道生物素化聚乙二醇/聚乳酸（Biotin-PEO-PLA）纳米粒子的体外靶向行为,国内没有这方面的研究报道。目的：分析Biotin-PEO-PLA纳米粒子作为靶向药物载体的可行性。方法：透析法制备包埋紫杉醇的Biotin-PEO-PLA纳米粒子并表征;通过高效液相色谱研究包埋紫杉醇的Biotin-PEO-PLA纳米粒子的体外释放行为;利用细胞毒性法比较研究生物素-亲和素三步法实施的包埋紫杉醇的Biotin-PEO-PLA纳米粒子对OVCAR-3（表面表达CA-125抗体）和SKOV-3（表面不表达CA-125抗体）细胞的体外靶向行为。结果与结论：包埋在Biotin-PEO-PLA纳米粒子中的紫杉醇的释放呈现初期的快速释放以及随后的缓慢释放。利用三步法处理的OVCAR-3细胞存活率明显低于SKOV-3细胞,表明通过Biotin-PEO-PLA/avidin/biotinylated MABX306与OVCAR-3细胞表面CA-125抗原的特异性相互作用,包埋紫杉醇的Biotin-PEO-PLA纳米粒子被更为有效地传递进了OVCAR-3细胞。

英文摘要：

BACKGROUND：Recently,the majority of polymer drug carriers have no targeting,thus are limited in applications.A few foreign research groups reported in vitro targeting behaviors of biotinylated poly（ethylene oxide）-poly（lactic acid）（Biotin-PEO-PLA） nanoparticles,however,the domestic study is absent.OBJECTIVE：To verify the feasibility of Biotin-PEO-PLA nanoparticles as targeted drug carriers.METHODS：Paclitaxel-loaded Biotin-PEO-PLA nanoparticles were prepared by dialysis method and characterized.The in vitro release behaviors of paclitaxel-loaded Biotin-PEO-PLA nanoparticles were studied by high performance liquid chromatogram technique.The active targeting properties of paclitaxel-loaded Biotin-PEO-PLA nanoparticles in vitro over OVCAR-3（CA-125 antigen positive） and SKOV-3 cells（CA-125 antigen negative） were also investigated through a three-step biotin-avidin interaction by MTT tests.RESULTS AND CONCLUSION：Paclitaxel loaded in Biotin-PEO-PLA nanoparticles shows an initial rapid release followed by a slow release period.Compared with SKOV-3 cells（CA-125 antigen negative）,the survival rate of OVCAR-3 through a three-step treatment was remarkably decreased.The cytotoxicity results implied that paclitaxel-loaded Biotin-PEO-PLA nanoparticles were delivered more effectively to OVCAR-3 cells（CA-125 antigen positive） under the specific interaction between the biotin groups on the surface of Biotin-PEO-PLA nanoparticles and the avidin/biotinylated MAb X306/CA-125 antigen complexes on the surface of OVCAR-3 cells.