5Fu-聚乳酸微球的体外释药及其抗癌效应研究

Release Characteristic and Antitumor Effect of 5-fluorouracil Loaded Polylactide Microspheres

目的 研究生物可降解抗癌药 5Fu PLA微球的释药特点 ,鉴定其体外杀伤肿瘤细胞的活性。方法 采用恒温振荡透析法和一阶导数紫外分光光度法测定了 5Fu PLA微球的药物释放特性 ;MTT法测定了不同时相 5Fu PLA微球对 5种肿瘤细胞株的杀伤活性。结果 5Fu PLA微球具有良好的缓释功能 ,半量释放期t1/2 为 10 .4天。 5Fu PLA微球对 5种肿瘤细胞株均有较强的杀伤活性 ,且杀伤活性与作用时间和释药量呈正相关关系。结论 5Fu PLA微球中药物分布均匀 ;微球制备和溶蚀过程对5Fu的药效无影响。 5Fu PLA微球具有良好的缓释功能 ,能在较长时间内维持有效的杀伤活性。

Objective In order to investigate the release characteristic and antitumor effects of bio soluble micorspheres of 5 fluorouracil loaded plylactide(5Fu PLA).Methods The constant temperature vibration dialysis assay and MTT colorimetric assay were used.Results The 5Fu PLA microspheres had a good function of extended release,t 1/2 =10.4 day,and five tumor cell lines were senstive to 5Fu PLA microspheres.The cytotoxities were positive interrelated with the drug reaction time and the released dose.Conclusion The therapeutic effect of 5 Fu will not be reduced by PLA microsphere preparation and release.