半乳糖介导姜黄素牛血清白蛋白纳米粒的制备及质量评价

Preparation and Characterization of Galactose-mediated Curcumin Bovine Berum Albumin Nanoparticles

目的建立去溶剂法制备半乳糖介导的姜黄素白蛋白纳米粒,并考察其理化性质及体外释药特性。方法以半乳糖修饰的牛血清白蛋白作为载体材料,姜黄素作为模型药物,采用去溶剂法制备姜黄素半乳糖化白蛋白纳米粒,单因素考察优化处方工艺,采用激光纳米粒度仪对其粒径和Zeta电位进行测定;超速离心法测定包封率及载药量;透析法考察其体外释药特性。结果根据优化处方工艺制备的白蛋白纳米粒外观呈圆形或类圆形,粒径分布为(267.1±78.3) nm,Zeta电位为-40～-50 mV;包封率为79.4%,载药量为3.7%;姜黄素纳米粒在8 h释药量为20%,48 h释药量>80%。结论去溶剂法制备的姜黄素纳米粒具有良好的理化性质和释药性能,提高药物的稳定性,可显著提高药物释放速率,提高生物利用度。

Objective To prepare galactosylated bovine serum albumin nanoparticles (Gal-BSA NPs) of curcumin by desolvation method, and to investigate its physicochemical properties and in vitro release characteristics. Methods Gal-BSA NPs were prepared by emulsion solvent evaporation method, and the preparation processes was optimized. Its size and Zeta potential were measured by Laser size and Zeta potential instrument. Entrapment efficiency and drug loading were measured by ultracentrifugation. The in vitro release characteristics were investigated by dialysis method. Results According to the preparation of the formulation and process optimization, the appearance of Gal-BSA NPs prove to be round or oval, particle size distribution was (267.1±78.3) nm, Zeta potential was -40 to -50 mV. Entrapment efficiency was 79.4%, and drug loading was3.7%. Gal-BSA NPs release20% at 8 h and >80% at48 h. Conclusion Solvent evaporation method can successfully prepare Gal-BSA NPs, and shows good physical and chemical properties and release properties, improve the stability of the drug, and can prolong the drug release rate and improve the bioavailability.