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.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
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)
