局部应用环孢素A聚乳酸微球的性状及释药研究  

A study on the properties and release of cyclosporin A polylactic acid microspheres for topical application

作　　者：梁志波[1] 李小飞[1] 刘锟[1] 吴红[2] 赵晋波[1] 

机构地区：[1]第四军医大学唐都医院胸外科,西安710038 [2]第四军医大学药学系化学教研室

出　　处：《中国药物与临床》2007年第1期9-12,共4页Chinese Remedies & Clinics

基　　金：国家自然科学基金资助项目(39970707);陕西省自然科学基金资助项目(99SM37)

摘　　要：目的对局部应用环孢素A聚乳酸微球的性状及其在体外、体内释放进行研究。方法通过采用O/W型乳化-溶剂挥发法制备环孢素A聚乳酸微球。观察微球分散度、粒径及外观形态及体外释药特性,对比全身与局部给药后全血中及气管组织中的环孢素A药物浓度。结果环孢素A聚乳酸微球的形态圆整,平均粒径18.234μm,跨距:1.131,粒径在9.525～32.400μm者占总数的80%以上。包封率为(86.1±0.8)%,载药量为(34.5±0.6)%。环孢素A聚乳酸微球的体外释药情况:30d的累积释药量为40.8%,采用局部埋植微球后前2周可以维持较高的血药浓度,2周后也可以维持在200ng/ml的药物浓度。结论环孢素A聚乳酸微球具有较好的缓释性能。局部应用可获得有效的血药浓度,在局部气管组织中的药物浓度高于全身用药组。Objective To characterize the properties of Cyclosporin A polylactic acid microspheres （CyA-PLA- MS） and profdes of drug release in vitro and in vivo. Methods CyA-PLA-MS was prepared using solvent evaporation method from an oil-in-water system. The microspheres were characterized for dispersity, mean particle size, morphology, as well as in-vitro drug release profiles compared with CyA levels in the whole blood and tracheal tissue after systematic and topical uses. Results CyA-PLA-MS was shown to be spherical particles with smooth surfaces. The mean particle size was 18.234 μm, with more than 80% of the microspheres falling in the range of 9.525-32.400 μm. The drug loadings ranged （34.5±0.6）% with a high encapsulation efficiency （86.1±0.8%） determined by HPLC. In vitro release study revealed a profile of sustained release of cyclosperin A from CyA-PLA- MS. The accumulated release percentage of cyclosporin A microspheres were 40.8% in 30 d. In rat whole blood, the level of topically administered CyA was persistently high during the first two weeks and remained at about 200 ng/ml during weeks 3 and 4. Conclusion CyA-PLA-MS showed good release profiles. Topical use of CyA achieved in therapeutic blood level, as well as a higher level in the tracheal tissue compared with as reached by systematic use. 　

关 键 词：亲环素类 微球体 血药浓度 聚乳酸 

分 类 号：R944[医药卫生—药剂学]