吉西他滨白蛋白纳米球在大鼠体内的分布和缓释  

Distribution and slow-release characters of gemcitabine-ioaded bovine serum albumin nanospheres in SD rats

作　　者：李金明[1] 龙江[1] 傅德良[1] 罗国培[1] 郭燕萍[1] 金忱[1] 虞先浚[1] 倪泉兴[1] 

机构地区：[1]复日大学胰腺病研究所复旦大学华山医院外科,上海200040

出　　处：《中华实验外科杂志》2009年第9期1133-1135,共3页Chinese Journal of Experimental Surgery

基　　金：上海市科委重大科技攻关资助项目（05DZ19346）;上海市经委重点产业技术产学研联合攻关项目（沪产学研06-23）

摘　　要：目的通过110、406nm两种粒径的吉西他滨（GEM）白蛋白纳米球在大鼠体内的分布，比较两者的靶向性、缓释性和安全性。方法以SD大鼠为实验对象，设置110nmGEM纳米球组（n=10）、406nmGEM纳米球组（n=10）和GEM原料药组（n=10）。采用高效液相色谱技术（HPLC），动态检测GEM在大鼠血浆和不同脏器组织内药物浓度。结果大鼠血浆药物-时间曲线以原料药组为高（P〈0．05）；给药6h后，406nm组在胰腺（155．59ug／g）、肝脏（43．57ug／g）、脾脏（35．27ug／g）三个重要靶器官的GEM药物浓度明显高于110nm和原料药组（P〈0．05），而在心脏（116．26ug／g）、肺脏（8．32ug/g）、肌肉（81．58ug／g）、肾脏（92．10ug／g）组织中的浓度与另外两组差异无统计学意义（P〉0．05）。结论406nm吉西他滨白蛋白纳米球具有优良的靶向性、缓释性和安全性，可以应用于胰腺癌的区域性动脉介入治疗。Objective To detect safety, slow-release characters and targeting effects of two kinds of gemcitabine （GEM）-loaded bovine serum albumin nanospheres （mean particle diameters were 110 and 406 nm respectively） through tissue distribution in SD rats. Methods Thirty male SD rates were divided into3 groups：（1） GEM group （n=10）;（2） 110 nm GEM nanospheres group （n=10）;（3） 406 nm GEM nanospheres group （n = 10）. Pure GEM was used as the model drug, and SD rats as experimental model animal. The concentrations of GEM in blood plasma and various organs of SD rats were dynamically detected by high performance liquid chromatography （HPLC）. Results Blood plasma GEM-time curve in GEM group was higher than the other two groups （ P 〈 0.05）. The concentrations of GEM in targeting organs,including pancreas （ 155.59 ug/g）, liver （43.57ug/g） and spleen （ 35.27ug/g）, were significantly higher in 406 nm nanospheres group than the other two groups 6 h after administration, but those of GEM in heart （116.26ug/g）,lung （8.32 ug/g）,kidney （92. 10 ug/g）,and muscles （81.58 ug/g） were similar to the other 2 groups （ P 〉 0.05 ）. Conclusion 406 nm GEM-loaded serum albumin nanospheres had excellent targeting effect, slow-release character and safety,and could be applied to the treatment of pancreatic cancer by regional intra-arterial infusion chemotherapy.

关 键 词：吉西他滨 纳米粒 白蛋白 胰腺癌 

分 类 号：R96[医药卫生—药理学]