叶酸修饰的白蛋白纳米粒的制备及理化性质的研究

Study on Preparation and Physicochemical Properties of Bovine Serum Albumin Nanoparticles Modified by Folate

将叶酸与牛血清白蛋白通过酰胺键合成叶酸修饰的白蛋白,在此基础上选择反溶剂法自组装形成纳米粒;并对其粒径、Zeta电位、微观形态、包封率和体外释药特性进行考察。结果表明,白蛋白和叶酸最适宜的投料比为1∶50,白蛋白取代度是(32.7±1.8)%;叶酸修饰的白蛋白纳米粒粒径为(255.8±2.3)nm,Zeta电位为(-29.8±2.1)m V,紫杉醇包封率为(83.2±1.4)%,体外释放呈现明显的缓释特征。采用本实验方法制备的包裹紫杉醇的叶酸白蛋白纳米粒具有良好的理化性质和缓释特性,有望成为紫杉醇的新型靶向输送制剂。

Albumin modified by folate（FA-BSA） was synthesized by the amide bond with folate and bovine serum albumin. On this basis,the anti-solvent method was chosen to form nanoparticles by self-assembling. The particle size,Zeta potential,microscopic morphology,encapsulation efficiency and the in vitro release characteristics were investigated. Results showed that the optimum input ratio of bovine serum albumin to folate was 1∶50 and the substitution degree of FA-BSA was（32. 7 ± 1. 8） %. The particle size of FA-BSA nanoparticles was（255. 8 ± 2. 3） nm,Zeta potential was（-29. 8 ± 2. 1） mV,and the encapsulation efficiency of PTX was（83. 2 ± 1. 4） %. The in vitro release of FA-BSA nanoparticles exhibited distinctly sustained release characteristics. The FA-BSA nanoparticles encapsulating PTX,which was prepared by the present method, had good physicochemical properties and sustained release characteristics,and were expected to become a novel target delivery system for PTX.