多西他赛Pluronic F68聚合物胶束的制备与体外评价

山东大学学报(医学版) ›› 2011, Vol. 49 ›› Issue (11): 156-160.

多西他赛Pluronic F68聚合物胶束的制备与体外评价

于克炜1, 2，刘志红1，张娜1

山东大学 1.药学院药剂学教研室，济南 250012； 2. 附属济南市中心医院药剂科，济南 250013

收稿日期:2011-06-27 出版日期:2011-11-10 发布日期:2011-11-10
通讯作者: 张娜（1969- ），女，博士，教授，主要从事基因药物及靶向纳米制剂研究。E-mail: zhangnancy9@sdu.edu.cn
作者简介:于克炜（1981- ），男，硕士研究生，主要从事药物新剂型研究

Docetaxel-loaded Pluronic F68 polymeric micelles:preparation and in vitro evaluation

YU Ke-wei1,2, LIU Zhi-hong1, ZHANG Na1

1. Institute of Pharmaceutics, School of Pharmacy, Shandong University, Jinan 250012, China;
2. Department of Pharmacy, Jinan Central Hospital Affiliated to Shandong University, Jinan 250013, China

Received:2011-06-27 Online:2011-11-10 Published:2011-11-10

摘要/Abstract

摘要：

目的制备多西他赛（DTX）的普朗尼克F68 (Pluronic F68) 聚合物胶束，并对其理化性质进行研究。方法采用纳米沉淀法制备DTX胶束，以L9(34)正交实验优化处方；高效液相色谱法测定药物的含量；通过透射电镜观察DTX胶束的形态，并进行粒度分布和zeta电位的测定；采用动态膜透析法考察DTX胶束的体外释药行为。结果 DTX胶束的包封率为 (89.10±1.50) %，载药量为 (0.060±0.003)%，外观形态呈现球形或类球形，粒径为 (135.1±3.42) nm，zeta电位为 (-10.56±3.52) mV。体外释放结果显示DTX胶束具有一定的缓释能力。结论利用纳米沉淀法成功制备了DTX胶束，成型好，粒径小，改善了DTX的溶解性。

关键词: 多西他赛；普朗尼克F68；聚合物胶束；纳米沉淀法

Abstract:

Objective To prepare docetaxel (DTX)-loaded Pluronic F68 polymeric micelles (DTX-micelles) and evaluate their physicochemical characterization. Methods The DTXmicelles were prepared by nano-precipitation methods. Based on the results of single factor experiments, the DTX-micelle formulation was optimized by orthogonal design. The encapsulation efficacy (EE%) and drug loading (DL%) were determined by the RP-HPLC method. The physicochemical characteristics were evaluated, including surface morphology, particle size and size distribution as well as zeta potential. The in vitro release behaviors of DTX-micelles were carried out by the dynamic membrane dialysis technique. Results The drug-loading rate and entrapment rate were (0.060±0.003)% and (89.10±1.50)%, respectively. The DTX-micelles were spherical with a mean particle size of (135.1±3.42) nm and a zeta potential of (-10.56±3.52)mV. The release of DTX from DTX-micelles followed the Weibull equation. Conclusions DTX-micelles were successfully prepared and improved the solubility of DTX.

Key words: Docetaxel; Pluronic F68; Polymeric micelles; Nanoprecipitation methods

中图分类号:

R944.9

于克炜1, 2，刘志红1，张娜1. 多西他赛Pluronic F68聚合物胶束的制备与体外评价[J]. 山东大学学报(医学版), 2011, 49(11): 156-160.

YU Ke-wei1,2, LIU Zhi-hong1, ZHANG Na1. Docetaxel-loaded Pluronic F68 polymeric micelles:preparation and in vitro evaluation[J]. JOURNAL OF SHANDONG UNIVERSITY (HEALTH SCIENCES), 2011, 49(11): 156-160.

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