食品科学 ›› 2017, Vol. 38 ›› Issue (6): 242-247.doi: 10.7506/spkx1002-6630-201706038

• 工艺技术 • 上一篇    下一篇

响应面试验优化猴头菌素-PLGA微球制备工艺及其体外释药性能

何晋浙,姚丽娜,孙培龙   

  1. 浙江工业大学海洋学院,浙江 杭州 310014
  • 出版日期:2017-03-25 发布日期:2017-03-28
  • 基金资助:
    国家高技术研究发展计划(863计划)项目(2014AA022205)

Optimized Preparation and in Vitro Release Properties of Erinacines-PLGA Microspheres by Response Surface Methodology

HE Jinzhe, YAO Lina, SUN Peilong   

  1. Ocean College, Zhejiang University of Technology, Hangzhou 310014, China
  • Online:2017-03-25 Published:2017-03-28

摘要: 目的:以聚乳酸-羟基乙酸共聚物(poly (lactic-co-glycolic acid),PLGA)为载体,采用乳化溶剂挥发法制备猴头菌素缓释微球,并对其体外药物释放行为进行考察。方法:通过单因素试验,以包封率为评价指标,考察影响微球质量的因素,采用响应面试验法进行优化,筛选出最佳工艺条件。结果:最佳工艺为芯壁比(猴头菌素与PLGA质量比)1∶1.64、PLGA质量分数15%、搅拌速率1 200 r/min。最佳条件制备的猴头菌素微球表面光滑圆整,包封率为99.66%,微球体外384 h累计释放率达84.30%。结论:以PLGA为载体材料,采用乳化-溶剂挥发法可以制备包封率较高的猴头菌素微球,体外释药实验也表明该微球具有明显的缓释作用。

关键词: 猴头菌素, 聚乳酸-羟基乙酸共聚物(PLGA), 微球, 体外释药

Abstract: Purpose: To prepare slow-release erinacines microspheres with poly (lactic-co-glycolic acid) (PLGA) as carry using the emulsification solvent evaporation method and to investigate their release characteristics in vitro. Methods: The one-factor-at-a-time method was adopted to examine the factors affecting encapsulation efficiency, and their levels were optimized using response surface methodology. Results: The optimum preparation conditions were obtained as follows: erinacines to PLGA ratio, 1:1.64 (g/g); concentration of PLGA in dichloromethane, 15%; and stirring speed, 1 200 r/min. The obtained microspheres were complete and smooth with an encapsulation efficiency of 99.66% and a cumulative release rate in vitro of 84.30% in 384 h. Conclusion: The emulsification solvent evaporation method has been successfully applied to prepare erinacines microspheres with high entrapment efficiency and good sustained release performance.

Key words: erinacines, poly (lactic-co-glycolic acid) (PLGA), microspheres, drug release in vitro

中图分类号: