多西他赛牛血清白蛋白纳米粒的制备及体外评价  

Preparation and in vitro Evaluation of Docetaxel-loaded Bovine Serum Albumin Nanoparticles

作　　者：吕鹏[1,2] 胡荣 卞玮[4] 杨亚妮[4] 何军[1,4] 

机构地区：[1]浙江工业大学长三角绿色制药协同创新中心,浙江杭州310014 [2]上海市浦东医院/复旦大学附属浦东医院临床药学室,上海201399 [3]重庆市药品技术审评认证中心,重庆400014 [4]中国医药工业研究总院药物制剂国家工程研究中心,上海201203

出　　处：《中国医药工业杂志》2017年第7期1030-1034,共5页Chinese Journal of Pharmaceuticals

基　　金：国家重点基础研究发展计划(973项目)(2013CB932504)

摘　　要：采用Nab^(TM)技术制备载多西他赛的牛血清白蛋白纳米粒,以粒径、包封率和载药量为指标,基于单因素试验和正交设计对处方进行优化。并采用动态透析法,考察其体外释放特性。结果表明,多西他赛白蛋白纳米粒优化处方为:牛血清白蛋白1%、氯仿/乙醇比11:1、油/水相比例1:49、药载比1:14.8、水相pH 6.6;制备时乳化均质压力为151.68 MPa,均质25次。照上述优化处方和工艺制备的3批样品平均粒径为(190.10-11.91)nn,包封率为(95.6±0.5)%,载药量(8.1±0.1)%,并具有缓释效果。Docetaxel （DCT） has been recognized as one of the most efficient anticancer drugs. However, its poor water solubility has limited the clinical applications. Albumin, a versatile protein carrier for drug delivery, has been shown to be nontoxic, non-immunogenic, biocompatible and biodegradable. Therefore, it is an ideal material to fabricate nanoparticles for drug delivery. Albumin nanoparticles have gained considerable attention owing to their high binding capacity of various drugs and being well tolerated without any serious side-effects. In this paper, the DCT-loaded bovine serum albumin nanoparticles （BSA-NPs） were prepared by NabTM-technology. Based on the results of a single factor test and an orthogonal design, the preparation and formulation of the title nanoparticles were optimized with particle size, encapsulation efficiency and drug loading as indexes. The property of drug release in vitro was investigated by the dynamic dialysis. Finally, the optimal formulation of the NPs was as follows： BSA 1%; chloroform∶ethanol in a 11∶1 ratio; oil-to-water phase ratio of 1∶49; drug to BSA ratio of 1∶14.8; pH 6.6 of water phase; and the process parameters were as follows： homogenization pressure of 151.68 MPa and for 25 cycle times. The optimized results showed that DCTBSA-NPs had small particle size of （190.10±11.91）nm, high encapsulation efficiency of （95.6±0.5）% and drug loading of （8.1±0.1）% as well as the characteristic of sustained-release in vitro.

关 键 词：多西他赛 牛血清白蛋白纳米粒 Nab^TM技术 处方优化 体外释放 

分 类 号：R944.9[医药卫生—药剂学]