5-FU-PLGA复乳微球的制备及体外释放

摘要

采用乳化溶剂挥发法制备W/O/W型5-FU-PLGA复乳微球,采用单因素设计考察了第一相体积比(内水相与油相)、第二相体积比(初乳与外水相)对复乳稳定性的影响,采用正交设计考察了搅拌温度、搅拌时间、辅料浓度和有机相中载体材料浓度对微球质量的影响,并对制备条件进行优化。最适宜制备条件为:第一相体积比为1:2,第二相体积比为1:1,搅拌温度为10 ℃、搅拌时间为6 h、辅料浓度为0.5%、有机相中载体材料浓度为15%。依据最适宜条件制备的微球圆整度良好、粒径范围窄,平均粒径5.20 μm,载药量为5.34%,包封率为77.22%。体外释放试验表明微球具有明显的缓释效果,释放行为符合Higuchi模型。

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	黄慧玲
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	魏振平

关键词： 5-氟尿嘧啶；乳化溶剂挥发法；复乳微球

Abstract：

5-FU-PLGA double emulsion microspheres were prepared by double emulsion solvent evaporation method. Single factor design was used to study the influence of the first phase volume ratio (inner water phase and oil phase) and the second phase volume ratio (the first phase and outer water phase) on the double emulsion. Orthogonal design was used to study the influence of stirring temperature, stirring time, the concentration of excipient and the concentration of carrier in oil phase on the prepared microspheres. And the preparation conditions were optimized. The optimal preparation method was as follows: the first phase volume ratio was 1:2, the second phase volume ratio was 1:1, the stirring temperature was 10 ℃, the stirring time was 6 h, the concentration of excipient and the concentration of carrier in oil phase were 0.5% and 15%, respectively. The prepared microspheres showed perfect sphericity and narrow particle size distribution. The average particle size was 5.20 μm. The drug loading was 5.34%. The encapsulation efficiency was 77.22%. The in vitro release study showed that the 5-FU-PLGA microspheres showed obvious sustained-release effect and the release behavior accorded with Higuchi model.

Keywords： 5-fluorouracil； emulsion solvent evaporation method； double emulsion microsphere

Received 2013-11-04;

Corresponding Authors: 魏振平, E-mail: zpwei2000@sina.com。 Email: zpwei2000@sina.com

About author: 黄慧玲(1987-),女,硕士研究生,从事药物新剂型方向的研究。

引用本文:

黄慧玲, 李益, 王玥, 魏振平.5-FU-PLGA复乳微球的制备及体外释放[J]. 化学工业与工程, 2016,33(1): 76-81

Huang Huiling, Li Yi, Wang Yue, Wei Zhenping.Preparation and in Vitro Release of 5-FU-PLGA Double Emulsion Microsphere[J]. Chemcial Industry and Engineering, 2016,33(1): 76-81

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