SPG膜乳化法制备丹参酮ⅡA聚乳酸-羟基乙酸微球的工艺优化

Preparation of Tanshinone ⅡA-loaded Polylactic Acid-Glycolic Acid Microspheres by SPG Membrane Emulsification Technique

摘要:

目的：优选SPG膜乳化法制备丹参酮Ⅱ_A-聚乳酸-羟基乙酸（PLGA）微球的工艺条件。方法：采用SPG膜乳化法制备丹参酮Ⅱ_A-PLGA微球。在单因素试验基础上，以载药量、包封率及多分散系数（PDI）的综合评分为因变量，通过响应面法考察PLGA质量浓度、流动相流速、聚乙烯醇（PVA）质量浓度及油水相体积比等自变量对处方工艺的影响。结果：最佳处方工艺为PLGA质量浓度44.29 g·L^-1，流动相流速825.68 r·min^-1，PVA质量浓度2.5 g·L^-1，油水相体积比1：7.86；制备的丹参酮Ⅱ_A-PLGA微球表面光滑圆整且粒径均一，平均粒径2.338 μm，PDI指数0.328，载药量1.20%，包封率89.57%，与预测值相对误差较小。结论：采用SPG膜乳化法制备微球的工艺简单、方便，可用于提高丹参酮Ⅱ_A的生物利用度。

Abstract:

Objective: To prepare tanshinone Ⅱ_A-loaded polylactic acid-glycolic acid(PLGA) microspheres by SPG membrane emulsification technique. Method: Based on single factor tests,with composite score of drug loading,encapsulation efficiency and polydispersity index(PDI) as dependent variable,response surface methodology was adopted to optimize prescription process by taking flow rate of mobile phase,volume ratio of oil-water phase,PLGA and PVA concentration as independent variables. Result: Optimum prescription process was as follows:PLGA concentration 44.29 g·L^-1,circulation speed 825.68 r·min^-1,PVA concentration 2.5 g·L^-1 and volume ratio of oil-water 1 ：7.86;These prepared tanshinone Ⅱ_A-loaded PLGA microspheres had smooth rounded surface and uniform size with average size of 2.338 μm,PDI index of 0.328,drug loading efficiency of 1.20% and encapsulation efficiency of 89.57%,relative errors of these parameters were small by comparing with the predictive values. Conclusion: SPG membrane emulsification technique was simple and effective,it could improve bioavailability of tanshinone Ⅱ_A.