去甲斑蝥素壳聚糖微球的制备及其体外释放特性  

Study on preparation and in vitro release of norcantharidin-loaded chitosan microspheres

作　　者：王钦[1] 成艳[1] 张玮[1] 张学农[1] 

机构地区：[1]苏州大学药学院药剂学教研室,苏州215123

出　　处：《中国新药杂志》2008年第11期947-951,共5页Chinese Journal of New Drugs

基　　金：江苏省科技厅社会发展项目(BS200522);江苏省高新技术产业发展项目(JHB05-46);苏州大学医学发展基金(EEl32503);江苏省卫生厅基金(H200630)

摘　　要：目的:制备去甲斑蝥素壳聚糖微球,并考察其体外释放特性。方法:以液体石蜡为油相,Span- 80为乳化剂,甲醛作为交联剂,采用乳化-交联法制备去甲斑蝥素壳聚糖微球。均匀设计优化制备工艺,扫描电镜观察微球表面形态,动态透析法检测微球的体外释放特性。结果:制备的微球形态圆整,粒径分布较为均匀,平均粒径(25±10)μm,载药量(15.08±2.85)%,包封率(57.80±1.35)%。微球在0.1 mol·L^(-1) HCl、磷酸盐缓冲液(pH值5.3)和生理氯化钠溶液中的释放均遵循Higuchi方程。结论:所优化的制备工艺简单易行,载药量高,缓释作用显著。Objective：To study the preparation technique and in vitro release characteristics of norcanthari- din-loaded chitosan microspheres. Methods：Norcantharidin-loaded chitosan microspheres were achieved by emulsification cross-linking process with liquid paraffin as oil phase, Span-80 as emulsifier, and formaldehyde as cross linking agent. The uniform experimental design was applied to optimize the formulation and preparation procedure. The surface morphology of the microspheres was observed by scanning electron microscope （SEM）. Dynamic dialysis method was used to determine the release characteristic of norcantharidin from microspheres in vitro. Results： Novel microspheres with a global shape and narrow distribution were prepared. The average diameter was （25 ± 10）μm. The drug-loading rate was （15.08 ± 2.85）%. The entrapment rate of microspheres was （57. 80 ± 1.35 ） % . The drug release behavior in 0.1 mol. L-1 hydrochloride, phosphate buffered saline （ pH 5.3 ） and physiological saline was discribed by Higuchi model. Conclusion：The optimized preparation technique was feasible, and microspheres with high drug-loading rate and evident effect of sustained drug release were prepared.

关 键 词：去甲斑蝥素 壳聚糖 微球 制备 体外释放 

分 类 号：R943.41[医药卫生—药剂学] R979.1[医药卫生—药学]