聚乳酸-羟基乙酸纳米粒的制备

Preparation of poly lactic acid-glycolic acid nanoparticles

背景：聚乳酸-羟基乙酸是一种生物相容性良好的可降解材料,确定其最佳制备工艺条件,有利于聚乳酸-羟基乙酸后续药物载体研究与工业化生产条件的确立。目的：以聚乳酸-羟基乙酸为包裹材料,探索纳米粒的制备条件对粒径、表面形态等的影响,确定最佳制备工艺条件。方法：采用乳化-溶剂挥发法制备聚乳酸-羟基乙酸纳米粒,以粒径为观察指标,探讨乳化剂种类、乳化剂含量、油相种类、超声时间、挥发时间、油相与水相体积比（W∶O）以及聚合物质量浓度等制备条件对纳米粒粒径的影响,确定制备聚乳酸-羟基乙酸纳米粒的最佳工艺条件。结果与结论：优化后的制备工艺条件是在室温下,以一定的搅拌速度和滴加速度,选择常用无毒的乳化剂,浓度在0.3%~1.0%,丙酮为有机相,超声时间8~15min、挥发时间6~10h、水油相比（W∶O）〉25∶1,聚合物质量浓度〈60g/L。提示该制备工艺简单、稳定,优化制备条件,可制备出表面形态规整、粒径适宜的聚乳酸-羟基乙酸纳米粒。

BACKGROUND： Poly lactic acid-glycolic acid （PLGA） is a type of biodegradable material with good biocompatibility. Optimum preparation conditions of PLGA are conductive to the follow-up studies of drug delivery and their establishment of industrial production conditions. OBJECTIVE： To explore the effects of preparation conditions of nanoparticles based on the wrapping material of PLGA on their particle size and surface morphology, and determine the optimum preparation and process. METHODS： PLGA nanoparticles were prepared using emulsion-solvent evaporation technique. The particle size of nanoparticles was measured. The effects of emulsifier type, emulsifier concentration, oil phase type, sonic time, volatile time, the volume ratio of water to oil, and polymer concentration on the particle size were analyzed to establish the optimum preparation conditions of PLGA. RESULTS AND CONCLUSION： The optimization parameters at the room temperature, with a certain stirring speed and drop acceleration, selection of the commonly used nontoxic emulsifier, the concentration was from 0.3% to 1%, acetone as organic phase, extraction time was from 8 to 15 minutes, volatile time was from 6 to 10 hours, ratio of water and oil 25：1, and the polymer concentration 60 g/L. The preparation process is simple, stable and optimized. The PLGA nanoparticles can be prepared with structured morphology surface and proper particle size.