硫酸长春新碱PLGA微球的制备及其性质  

Preparation and Characterization of Vincristine Sulfate-loaded PLGA Microspheres

作　　者：陈红丽[1] 陈汉[1] 李学敏[1] 袁平[1] 张其清[1] 

机构地区：[1]中国医学科学院北京协和医学院生物医学工程研究所天津市生物医学材料重点实验室,天津300192

出　　处：《中国医学科学院学报》2007年第3期342-346,共5页Acta Academiae Medicinae Sinicae

基　　金：国家高技术研究发展计划项目(863项目)(2002AA326040);国家杰出青年科学基金(59625306)~~

摘　　要：目的采用W/O/O溶剂挥发法制备硫酸长春新碱PLGA微球,评估添加剂碳酸锌对微球形态及药物释放速率的影响。方法测定硫酸长春新碱在4种不同pH条件下的降解规律,选定适合药物体外释放最适宜介质条件。在微球制备过程中添加2种不同量(w/w5%、10%)的碳酸锌,对其和不添加碳酸锌的硫酸长春新碱PLGA微球进行表征及体外释放测定。结果碳酸锌可明显增加微球中药物的稳定性,36d的体外释放测定结果显示,添加碳酸锌的微球累积释药量都达到70%以上,而未添加碳酸锌的微球释药量仅为(54.2±1.1)%。添加10%碳酸锌对提高微球药物稳定性的作用优于5%碳酸锌。结论添加碳酸锌对于制备硫酸长春新碱PLGA微球是必要的,能改善药物在PLGA微球内部酸性微环境中的稳定性,明显减少其药物降解量。Objective To prepare the vincristine sulfate （VCR） microspheres by W/O/O solvent evaparation method and evaluate the effect of zinc carbonate （ ZnCO3） on the morphology and release kinetics of the microspheres. Methods Degradation kinetic of VCR was tested in PBS of four different pH values at 37℃ to select the optimal incubation medium for in vitro release. Microspheres were made with or without ZnCO3 （ w/w 5% and 10% ） in the polymeric phase. The properties and in vitro release profiles of the micro- spheres were examed. Results ZnCO3 increased the stability of VCR in the PLGA microspheres. During the 36 days of in vitro release, the accumulative release of VCR from the microspheres reached 〉 70% when added with ZnCO3, and was （54. 2 ±1.1 ）% when no ZnCO3was added. 10% ZnCO3 showed superior effect than 5% ZnCO3in the stabilization of microspheres. Conclusions Adding ZnCO3 is essential during the preparation of PLGA microspheres. It can remarkably improve the stability of drugs in the acid microenvironment inside PLGA microspheres and decrease the VCR degradation during incubation.

关 键 词：硫酸长春新碱 微球 碳酸锌 稳定性 

分 类 号：R943[医药卫生—药剂学]