乳化–溶剂挥发法制备5-氟尿嘧啶聚乳酸微球及其缓释过程的研究

Preparation of 5-Fluorouracil Polylactic Acid Microspheres by Emulsification-Solvent Volatilization Method and Its Sustained Release Process

摘要: 目的：制备尺寸均一的聚乳酸载药微球，考察其对5-氟尿嘧啶的体外缓释效果。方法：通过乳化–溶剂挥发法制备微球，考察因素包括表面活性剂种类、浓度及聚乳酸浓度；采用电子显微镜技术对微球的形态进行表征；利用粒径分析仪对微球粒径完成分析；使用定量分析法，测量药物在体外环境下的缓释曲线。结果：所获得的聚乳酸微球粒径约为(65 ± 12.5) µm；包封率和载药量分别达到85.35%和22.57%，体外模拟缓释曲线证明药物的缓释时间可长达240小时。结论：可为医用药物及缓释控制型聚乳酸载药复合微球的生产提供关键技术和参数支撑。

Abstract: Objective: Preparation of polylactic acid drug-loaded microspheres with uniform size and inves-tigation of its sustained release effect on 5-fluorouracil in vitro. Methods: Microspheres were prepared by emulsification-solvent volatilization method, and the factors to be investigated included surfactant type, concentration and polylactic acid concentration; the morphology of microspheres was characterized by electron microscopy; the microspheres were analyzed by particle size analyzer. The particle size analysis is completed; using quantitative analysis, the sustained release curve of the drug in the in vitro environment is measured. Results: The particle size of the obtained polylactic acid microspheres was about (65 ± 12.5) µm; and the encapsulation efficiency and drug loading reached 85.35% and 22.57%, respectively. The simulated sustained release curve in vitro proved that the sustained release time of the drug could be as long as 240 hours. Conclusion: It can provide key technology and parameter support for the production of medical drugs and sustained release controlled polylactic acid drug-loaded composite microspheres.