野菊花总黄酮-PLGA缓释微球的制备及其工艺优化

doi:10.13481/j.1671-587x.20160339

摘要/Abstract

摘要：

目的: 制备野菊花总黄酮(TFC)-聚乳酸-羟基乙酸共聚物(PLGA)缓释微球,并对制备工艺进行优化。方法: 采用复乳溶剂挥发法制备TFC-PLGA微球,观察初乳搅拌速度、聚乙烯醇(PVA)浓度和TFC与PLGA的投药比等不同因素对微球包封率(EE)的影响。显微镜观察微球大体形态;扫描电镜(SEM)观察微球表面形态和粒径大小;紫外分光光度法测量微球EE及其体外释放结果。结果: 在搅拌速度为3000r·min^-1、PVA浓度为3.0%、TFC与PLGA投药比为1:15的优化条件下,TFC-PLGA微球平均EE为(45.03±1.25)%,平均粒径大小为(102.20±1.97)μm。体外释放实验,24h时微球累积释放率为22.07%,20d时累积释放率达92.32%,TFC-PLGA微球具有明显的缓释效果。结论: 采用优化的制备工艺可以制备出粒径适宜、分散较均匀、EE较高的TFC-PLGA缓释微球。

关键词: 野菊花总黄酮, 聚乳酸-羟基乙酸共聚物, 微球, 缓释

Abstract:

Objective: To prepare the sustained release microspheres of total flavonoids of chrysanthemum indicum(TFC)-polyactic-co-glycolic acid(PLGA) and to optimize the conditions. Methods: The TFC-PLGA microspheres were prepared by using the double emulsion solvent evaporation method.The effects of different conditions,such as the stirring rate,the polyvinyl alcohol(PVA) concentration and the ratio of TFC to PLGA on the entrapment efficiency(EE) of microspheres were observed.The general morphology of the microspheres was observed by microscope;the surface morphology and particle size of the microspheres were observed by SEM;the EE and in vitro release results of the microspheres were measured by UV spectrophotometry. Results: When the stirring rate was 3 000 r·min^-1,the PVA concentration was 3.0%,and the ratio of of TFC to PLGA was 1:15 as the optimal conditions,the acquired TFC-PLGA microspheres showed well-defined properties,with uniform sphere in appearance,general particles without adhesion,and the average EE was (45.03±1.25)% and the mean diameter was (102.20±1.97)μm.The results of release experiment in vitro showed that the percentage of accumulative release were 22.07% in 24 h and 92.32% on 20 d and the micropheres had significant sustained release effect. Conclusion: The TFC-PLGA microspheres with suitable size, uniform dispersion and high EE can be acquired under the optimized conditions.

Key words: total flavonoids of chrysanthemum indicum, polyactic-co-glycolic acid, microspheres, sustained release

中图分类号:

R285

卢晴, 车鸿泽, 陈楠楠, 陈飞, 焦鹏, 马宁. 野菊花总黄酮-PLGA缓释微球的制备及其工艺优化[J]. 吉林大学学报(医学版), 2016, 42(03): 617-621.

LU Qing, CHE Hongze, CHEN Nannan, CHEN Fei, JIAO Peng, MA Ning. Preparation of total flavonoids of chrysanthemum indicum(TFC)-PLGA sustained release microspheres and its optimization of technology[J]. Journal of Jilin University Medicine Edition, 2016, 42(03): 617-621.

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