载表阿霉素聚乳酸微球的制备及性质研究
Preparation and Characterization of Polylactide Microspheres Containing Epirubicin
Abstract
表阿霉素是广谱的抗肿瘤药物,为了减少给药量,降低药物的毒副作用,并达到缓慢释放的目的,本研究以Span-80和Tween-80复合乳化剂为初乳乳化剂,以聚乙烯醇水溶液为复乳乳化剂,采用复乳-溶剂挥发法制备了聚乳酸载药微球,并分别用激光粒度分析仪,光学显微镜,透射电子显微镜,扫描电子显微镜以及激光共聚焦显微镜对微球微观形态进行了表征.通过优化实验,所得载表阿霉素聚乳酸微球粒径2-5μm,载药率最高可达到4.39%,包封率达37.2%,72h体外累积释放量为34.9%,具有明显的缓释效果.本研究制备了表阿霉素缓释新剂型,为进一步的动物实验、临床实验和临床应用提供了有价值的参考数据,有很好的应用前景.
【英文摘要】 Epirubicin is an anthracycline antibiotic and antitumor epimer of doxorubicin that has been used to treat a wide range of cancers.Polylactic acid(PLA) microspheres containing epirubicin hydrochloride were prepared with double emulsion-solvent evaporation technique in order to reduce the side effect and the dose of drug.The complex of sorbitan monooleate(Span-80) and sorbitan polyoxyethylene monooleate(Tween-80)(1∶5 by vol.) was used as emulsifier of the primary emulsion.The second emulsion was emulsified wi...