载穿心莲内酯mPEG-PLA聚合物胶束制备工艺研究

The preparation of mPEG-PLA polymeric micelles loading Andrographolide

[目的]制备载穿心莲内酯mPEG-PLA聚合物胶束。[方法]以共聚物材料聚乙二醇-聚乳酸为载体,以穿心莲内酯为模型药物,用溶剂挥发法制备胶束。用星点设计效应面法优化处方;用高效液相色谱法测定穿心莲内酯含量并计算包封率和载药量;用激光粒度仪测定胶束的粒径;用透射电子显微镜对胶束进行形貌观察。[结果]最优处方为:聚乙二醇-聚乳酸40 mg,有机相甲醇2 mL,穿心莲内酯6.68 mg,水相44.14 mL,包封率为(85.19±3.28)%,载药量为(12.38±0.80)%。胶束平均粒径为(147.96±21.79)nm,呈棒状结构。[结论]穿心莲内酯聚合物胶束的处方制备工艺简单易行,胶束可以提高药物在水中的溶解度。

[Objective]To prepare mPEG-PLA polymeric micelles loading Andrographolide （mPEG-PLA-A）. [Methods]Using poly（ ethylene glycol）-poly（ lactic acid） （mPEG-PLA） material as the carrier and Andrographolide as the model drug , the micelles are prepared by solvent-evaporation method. Optimization preparation method was gained by central composite design. The drug entrapping efficiency and loading capacity were determined by High Performance Liquid Chromatography（ HPLC）. The main particle size was determined by zeta sizer H-3000 Laser Particle Size Analyzer. Using transmission electron microscope （TEM） to observe the morphology of the micelles. [Results]Optimization preparation method： the mass of mPEG2000-PLA1000 was 40rag, the volume of organic phase methyl alcohol was lml, the mass of A was 6.68mg, the volume of water was 44.14ml. The drug entrapping efficiency and loading capacity were （85.19±3.28） % and （12.38±0.8） 0%. This micelle has a rob structure with the size of （147.96±21.79） nm. [Conclusion]The process is practical and simple for the preparation of A loaded mPEG-PLA micelle and the micelles can increase drug solubility.