活性氧响应的白及多糖载药胶束制备及其表征

Preparation and characterization of reactive oxygen species-responsive Bletilla striata polysaccharide micelle

目的制备活性氧响应的白及多糖载药胶束,进行处方、制备工艺优化,并进行体外评价。方法合成活性氧响应白及多糖载体材料,以姜黄素为模型药物,采用透析法制备载药胶束;通过单因素和正交设计法优化处方;用透射电镜和激光粒子测定仪对胶束的形态和粒径分布、Zeta电位进行表征;用过氧化氢模拟活性氧环境,观察胶束形态变化。结果在优化条件下制备的载药胶束外观呈圆球形,分布均匀,平均粒径为(225.33±2.97)nm,Zeta电位为(-16.80±0.37)m V,包封率为(85.75±0.87)%,载药量为(20.21±0.44)%;在氧化条件下胶束材料可发生降解。结论优化条件下制备的白及多糖载药胶束粒径分布均匀,包封率和载药量良好。

Objective To prepare reactive oxygen species(ROS)-responsive Bletilla striata polysaccharide(Oxi-BSP) micelles, optimize their preparation technnology, and evaluate its in vitro characterizations. Methods Oxi-BSP was synthesized, then curcumin(Cur)-loaded micelles were prepared by a dialysis method. The formulation and preparation technology was optimized using an orthogonal design method. The morphology was observed by transmission electron microscope, while the particle size, particle distribution, and zeta potential were determined by laser particle size analyzer. Hydrogen peroxide was used to simulate the ROS environment and then the change of micellar morphology was observed. Results The Cur-loaded micelles were spherical with homogeneous distribution, the mean size was(225.33 ± 2.97) nm, the zeta potential was(-16.80 ± 0.37) m V, the encapsulation efficiencies was(85.75 ± 0.87)%, and drug loading capacities was(20.21 ± 0.44)%. And the micelles were responsive to ROS stimuli. Conclusion The obtained micelles display an uniform particle size distribution with moderate drug encapsulation efficiencies and drug loading capacities.