阿昔洛韦-乙交酯-丙交酯共聚物毫微粒制备工艺的优化选择

Optimization of the technological process to prepare acyclovir poly (DL-lactic-co-glycolic acid) nanoparticles

目的 :筛选制备阿昔洛韦 乙交酯 丙交酯共聚物毫微粒 (ACV PLGA NP)的优化工艺。方法 :单因素试验初选制备ACV PLGA NP的 pH值范围、聚乙烯醇 (Polyvinylalcohol ,PVA)浓度范围、PLGA分子量、药物及丙酮浓度范围。按均匀设计表设计实验 ,进行结果预测及验证。结果 :优化工艺与PLGA分子量及丙酮浓度无关 ,pH值为 1 5 ,PVA浓度为 5 0mg/ml,ACV浓度为 0 8mg/ml。按优化条件制备的ACV PLGA NP平均包封率为 61 0 0 %,载药量为 6 79%。结论 :按照均匀设计法优选的条件制备ACV PLGA NP ,其目标量在预测值范围内。

Objective: To optimize the technological process for the preparation of acyclovir poly (DL lactic co glycolic acid) nanoparticles (ACV PLGA NP) Methods: The range of pH value, the concentration were preliminarily determined with single factor test ACV PLGA NP was prepared with spontaneous emulsification solvent diffusion and the 5 factors and 9 levels for the preparation of ACV PLGA NP were selected with uniform design U 9(9 6) test Results:The molecular weight of PLGA and the concentration of acetone were not related to the optimization of the technological process The pH value was 1 5, the concentration of PVA was 50 mg/ml and the concentration of ACV was 0 8 mg/ml Using these conditions, a white colloidal solution was obtained, in which the drug loading was 6 79%and drug embedding ratio was 61 00% Conclusion: The target variables of ACV PLGA NP prepared with the optimized technological process are within the predicted limits