吉西他滨白蛋白纳米粒的制备及其对胰腺癌细胞的毒性研究  

Preparation of bovine serum albumin nanoparticles loaded with gemcitabine and the cytotoxic effect on pancreatic cancer cells in vitro

作　　者：李金明[1] 陈卫[3] 龙江[1] 金忱[1] 陆伟跃[2] 倪泉兴[1] 傅德良[1] 侯惠民[3] 

机构地区：[1]复旦大学华山医院胰腺病研究所 [2]复旦大学药学院药剂学教研室 [3]药物制剂国家工程研究中心

出　　处：《中华胰腺病杂志》2008年第5期295-297,共3页Chinese Journal of Pancreatology

基　　金：上海市科委重大科技攻关项目（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：目的制备具有药物缓释作用的吉西他滨白蛋白纳米粒，探讨其体外对胰腺癌细胞的毒性作用，为提高胰腺癌介入化疗的疗效提供新型制剂药物。方法以吉西他滨和白蛋白为原料，通过去溶剂-交联方法制备吉西他滨白蛋白纳米粒，采用高效液相色谱技术测定吉西他滨药物浓度，MTT法检测吉西他滨纳米粒对胰腺癌细胞株PANC1的细胞毒性。结果吉西他滨纳米粒的粒径为（156．2±2．2）nm，Zeta电位为（-20．4±1．41）mV，载药量为10．8％，药物释药时间为3h；0．01—50μg/ml的吉西他滨白蛋白纳米粒对PANC1细胞抑制率为31％-44％，与同浓度吉西他滨对PANC1细胞抑制率26％～47％几乎等同。结论吉西他滨白蛋白纳米粒制剂具有明显的药物缓释作用，将有助于胰腺癌介入化疗疗效的改进。Objectives To investigate preparation of gemcitabine albumin nanoparticles, and its property of slow-release, the cytotoxic effect on pancreatic cancer cells（ PANC1 ） in vitro, for improving the effect of regional intra-arterial infusion chemotherapy in pancreatic cancer with new medicament in the future. Methods The gemcitabine albumin nanoparticles were prepared with bovine serum albumin and gemcitabine with the desolvation-crosslink method, the concentration of gemcitabine was detected by high performance liquid chromatography （HPLC）. The cytotoxic effect on pancreatic cancer cells in vitro were detected with MTT colorimetric assay. Results The mean diameter of gemcitabine albumin nanoparticles was （ 156.2±2.2） nm, and Zeta potential was （ -20.4±1.41 ）mV, drug loading was 10.8% , drug release time in virto was 3 hours respectively. Gemeitabine albumin nanoparticles （0. 01 - 50 μg/ml） had a 31% - 44% inhibitory rate on PANC1 cell, which was similar to the inhibitory rate of same concentration of gemcitabine （26% - 47% ）. Conclusions The new preparation of gemcitabine albumin nanoparticles had obvious drug slow-release effect, which may help improve the effect of regional intra-arterial infusion chemotherapy for pancreatic cancer.

关 键 词：胰腺肿瘤 纳米技术 白蛋白 吉西他滨 细胞毒作用 

分 类 号：R735.9[医药卫生—肿瘤]