依托泊苷胶束的制备与表征

劳新南; 曹高忠

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.
	LAO Xinnan,CAO Gaozhong.Preparation and Characterization of Etoposide Micelles[J].Chin J Mod Appl Pharm(中国现代应用药学),2017,34(7):992-996.

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依托泊苷胶束的制备与表征
劳新南¹, 曹高忠²
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-α-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-α-生育酚-聚乙二醇琥珀酸酯胶束

DOI：10.13748/j.cnki.issn1007-7693.2017.07.013

分类号:R284.1；R917.101

基金项目:

Preparation and Characterization of Etoposide Micelles

LAO Xinnan¹, CAO Gaozhong²

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 safe and efficient drug delivery system for VP-16.

Key words: etoposide D-α tocopheryl polyethylene glycol succinate (TPGS) micelles