替莫唑胺白蛋白纳米粒的制备及其脑内递药特性研究  

Preparation and Brain Delivery Evaluation of Temozolomide-loaded Albumin Nanoparticles

作　　者：金滔[1] 彭花楠[1] 姚金娜[1] 戴东波[1] 李范珠[1] 

机构地区：[1]浙江中医药大学药学院,浙江杭州310053

出　　处：《中国医药工业杂志》2013年第1期41-45,共5页Chinese Journal of Pharmaceuticals

基　　金：浙江省新世纪151人才工程;浙江省卫生高层次创新人才培养工程

摘　　要：以牛血清白蛋白为载体,采用高压均质法制备替莫唑胺白蛋白纳米粒,并运用脑微透析技术,考察该纳米粒经大鼠尾静脉注射给药后的脑内递药特性。结果表明,白蛋白纳米粒形态圆整,平均粒径为(117.60±3.40)nm,电位为(-14.70±3.51)mV,包封率与载药量分别为(52.16±2.23)%和(5.33±0.10)%。替莫唑胺白蛋白纳米粒组的tmax和AUC0→t比其溶液剂组显著提高,但cmax无显著差异。结果提示本品可延长药物在脑内的持续时间,促进药物的脑内吸收,有望成为替莫唑胺脑部递药的有效载体。Temozolomide-loaded albumin nanoparticles were prepared by high pressure homogenization method with bovine serum albumin as carrier material. The brain delivery behaviors of the prepared nanoparticles iv administrated to rats were investigated by brain microdialysis technique. The results showed that the products were spherical with the average diameter of （117.60±3.40） nm,ξ poteneial of （-14.70±3.51） mV, encapsulation efficiency of （52.16±2.23） % and drug loading of （5.33±0.10） %. The tmax and AUC0→t of ternozolomide-loaded albumin nanoparticles were significantly improved compared with the temozolomide solution, while Cmax had no significant difference. The results suggested that the nanoparticles could extend the retention time in brain and increased the drug absorption in cerebral fluids. Albumin nanoparticles could be a potentially effective carrier for brain delivery of temozolomide.

关 键 词：替莫唑胺 白蛋白纳米粒 高压均质法 脑内递药 脑微透析技术 

分 类 号：R944.9[医药卫生—药剂学]