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研究生物降解性阿霉素聚乳酸微球的体外释放及其对视网膜的毒性。方法 :采用溶媒挥发法制备生物降解性阿霉素聚乳酸微球。用扫描电镜观察其形态 ,荧光分光光度法观测其体外释放情况 ;2 8只兔用于间接检眼镜、ERG、光镜和透射电镜检查以评价药物的视网膜毒性。结果 :制得的微球平均粒径为 37.9μm,其中阿霉素载药量为 2 .85 % ;体外释放速率缓慢 ,第 42天时阿霉素的释放率仅达 6 6 .44% ;观察表明 ,游离阿霉素剂量超过 5 μg或阿霉素聚乳酸微球超过 1 5 μg时 ,视网膜出现毒性反应。结论 :阿霉素聚乳酸微球较游离阿霉素毒性小 ,具有缓释长效的特点 ,提示该制剂有可能成为一种有效的治疗增生性玻璃体视网膜病变的眼内释药系统。
To study the in vitro release of biodegradable doxorubicin polylactide microspheres and its toxicity to the retina. Methods: The biodegradable doxorubicin polylactic acid microspheres were prepared by solvent evaporation method. Scanning electron microscopy was used to observe the morphological changes of the cells. Fluorescence spectrophotometry was used to observe the release in vitro. Twenty-eight rabbits were used in indirect ophthalmoscope, ERG, light microscope and transmission electron microscopy to evaluate the retinal toxicity. Results: The average particle size of the prepared microspheres was 37.9 μm. The drug loading of adriamycin was 2.85%. The release rate in vitro was slow. The release rate of adriamycin was only 66.44% on the 42nd day. Show that the dose of free doxorubicin more than 5 μg or doxorubicin polylactic acid microspheres more than 15 μg, the retina toxic reaction occurs. CONCLUSION: Adriamycin-loaded polylactic acid microspheres are less toxic than doxorubicin and have the characteristics of prolonged release and long-term efficacy, suggesting that the preparation may be an effective intraocular drug delivery system for the treatment of proliferative vitreoretinopathy.