不同混合溶剂对丹参酮Ⅱ_A-PLGA微球的影响

Effects of different solvent mixtures on tanshinone Ⅱ_A-loaded PLGA microspheres

目的考察不同混合溶剂(二氯甲烷-二氧六环、二氯甲烷-乙酸乙酯、二氯甲烷-丙酮、二氯甲烷-乙腈)对丹参酮Ⅱ_A-PLGA微球的影响。方法乳化-溶剂挥发法制备微球后,测定其载药量、包封率、粒径、体外释放度、药物分布参数,分析微球性能与溶剂性质的相关性。结果所得微球平均载药量约10%,包封率约90%,粒径约40μm。不同混合溶剂中微球体外释放行为、药物分布存在明显差异,相关性显著。结论混合溶剂对丹参酮Ⅱ_A-PLGA微球性能和药物分布有较大影响。

AIM To investigate the effects of different solvent mixtures( dichloromethane-dioxane,dichloromethane-ethyl acetate,dichloromethane-acetone,dichloromethane-acetonitrile) on tanshinone Ⅱ_A-loaded PLGA microspheres. METHODS Emulsion-solvent evaporation method was applied to preparing microspheres,after which their drug loading,encapsulation efficiency,particle size,in vitro release and drug distribution parameters were determined, along with the correlation analysis of microsphere performance and solvent properties.RESULTS The obtained microspheres demonstrated the average drug loading of about 10%,encapsulation efficiency of about 90%,and particle size of about 40 μm. Obvious differences existed in the microspheres’ in vitro release behaviors and drug distributions in different solvent mixtures, together with significant correlations.CONCLUSION Solvent mixtures have great effects on the performance and drug distributions of tanshinoneⅡ_Aloaded PLGA microspheres.