PEGPLGA多孔载药微球制备因素的优化.doc

PEG-PLGA多孔载药微球制备因素的优化 袁晓明 (安徽省宿州市食品药品检验所安徽宿州234000) 】目的：研究乙交酯-丙交酯-聚乙二醇(PEG-PLGA)载药微球 制备因素对外观形态、载药量和毡封率的影响，制备符合要求的多孔载药微球。 方法：以乙交酯(GA)、L-丙交酷(LA)和聚乙二醇(PEG)为原料制备PEG-PLGA; 以二氯甲烷为有机相，用W/O/W复乳法制备包封伊文思蓝的PEG-PLGA多孔载 药微球。以微球外观形态、载药量和毡封率为参考指标，对制备因素温度、聚合 物浓度和聚合物各组分摩尔比进行优化。结果：优化条件后最佳组合：温度40 °C (二氯甲烷的沸点)，浓度为75mg/ml,聚合物各组分摩尔比为63/27/10。此时 微球为多孔结构，成球规整，孔隙均匀，载药量和包封率相对较高，分别为0.38% 和32.41%。结论：制备温度、聚合物浓度和聚合物各组分摩尔比对载药微球的 外观形态、载药量和伍封率有较大影响。 关键词】乙交酯-丙交酯-聚乙二醇；载药微球；制备因素；优化 】R97 】A 】2095-1752 (2015) 32-0382-03 Optimization of preparation factors for PEG-PLGA drug-loaded microsphere YUAN Xiao-ming(Suzhou Institute For Food and Drug Control, Suzhou, Anhui, 234000) Abstract】 Objective To study the effect of preparation factors of glycolide-lactide-polyethylene glycol (PEG-PLGA) carrier drug microsphere on the appearance form, drug loadings and entrapment efficiency, to meet the requirements of preparing porous carrier drug microsphere.Methods PEG-PLGA was prepared with the raw material of glycolide(GA),L-lactide(LA) and polyethylene glycol(PEG).With the organic phase of dichloromethane, W/O/W multiple emulsion was used to prepare Evans blue porous drug-loaded microsphere encapsulated by PEG-PLGA. Using appearance form, drug loadings and entrapment efficiency as reference parameters,the factors of preparation temperature, polymer concentration and component molar ratio were optimized.Results After optimization, best combination: temperature 40 °C （the boiling point of dichloromethane）,the concentration-75 mg/ml, polymer components molar ratio-63/27/10.At the moment, microspheres had porous structure,regular ball neat, uniform pore, higher drug loadings and drug-loading rate, which were 0.38% and 32.41% respectively.Conclusion Preparation temperature, polymer concentration and component molar ratio have a great influence on appearance form, drug loadings and entrapment efficiency of drug-loaded microsphere. Keywords】 Glycolide-lactide-polyethylene glycol; Drug-loaded microsphere; Prepara