依托泊苷胶束的制备与表征.PDFVIP

依托泊苷胶束的制备与表征  1 2 劳新南 ，曹高忠 (1.桐乡市康复医院，浙江 桐乡 314500 ；2.温州医科大学附属第一医院，浙江 温州 325000) 摘要：目的 制备并表征装载依托泊苷(VP-16)的D--生育酚-聚乙二醇琥珀酸酯(TPGS)胶束(VP-16/TPGS)。方法 采用 薄膜水化法制备VP-16/TPGS ，测定其粒径、Zeta 电位，研究其体外药物释放行为，考察其细胞摄取和细胞毒性，评价其 血液相容性。结果 所制得的 VP-16/TPGS 胶束具有较小的粒径；具有较高的载药量和包封率；体外呈现良好的缓控释 效果；可增强H446 细胞对其的摄取，进而提高抗肿瘤活性；具有较高的血液相容性。结论 VP-16/TPGS 胶束是一种安 全、有效的VP-16 递送系统。 关键词：依托泊苷；D--生育酚-聚乙二醇琥珀酸酯；胶束 中图分类号：R943 文献标志码：B 文章编号：1007-7693(2017)07-0992-05 DOI: 10.13748/ki.issn1007-7693.2017.07.013 引用本文：劳新南, 曹高忠. 依托泊苷胶束的制备与表征[J]. 中国现代应用药学, 2017, 34(7): 992-996. Preparation and Characterization of Etoposide Micelles 1 2 LAO Xinnan , CAO Gaozhong (1.The Rehabilitation Hospital of Tongxiang, Tongxiang 314500, China; 2.The First Affiliated Hosptial of Wenzhou Medical University, Wenzhou 325000, China) ABSTRACT: OBJECTIVE To prepare and characterize the eptoposide(VP-16)-loaded D-α tocopheryl polyethylene glycol succinate(TPGS) micelles. METHODS The VP-16/TPGS was prepared using thin-film hydration method. The particle size and Zeta potential were measured. The drug release behavior, cellular uptake and cytotoxicity were also studied. At last, the hemocompatibility was also evaluated. RESULTS The prepared VP-16/TPGS micelles had small sizes, high drug loading capacity and encapsulated efficiency. The VP-16/TPGS micelles also exhibited a sustained and controllable in vitro release behavior. The enhanced cellular uptake of the VP-16/TPGS micelles by H446 celles improved the cytotoxicity. Besides, the VP-16/TPGS micelles showed a good hemocompatibility. CONCLUSION VP-16/TPGS nanomicelle may be a s