甘草酸表面修饰N-己酰化壳聚糖纳米粒的制备及其稳定性研究

Preparation of N-caproyl Chitosan Nanoparticles Surface-modified with Glycyrrhizin and Its Stability in Vitro

目的:制备N-己酰化壳聚糖纳米粒(CCS-NPs)和甘草酸表面修饰N-己酰化壳聚糖纳米粒(CCS-NPs-GL),并考察其稳定性。方法:应用离子凝胶法制备CCS-NPs,高碘酸盐氧化法制备CCS-NPs-GL;考察各纳米粒在冷冻干燥前、后和不同pH缓冲盐中粒径、电位的变化以及不同温度对CCS-NPs-GL的粒径、药物包封率和甘草酸结合率的影响。结果:CCS-NPs和CCS-NPs-GL在冷冻干燥后粒径稍有增大,缓冲盐溶液中迅速分散,电位下降不明显;在生理pH条件下,两者易于分散且粒径无明显变化;不同温度下,CCS-NPs-GL的粒径、药物包封率和甘草酸结合率无明显变化。结论:CCS-NPs-GL作为潜在的肝靶向主动传输载体,其粒子的稳定性可满足后续静脉给药的体内靶向研究和药效学评价。

OBJECTIVE： To prepare N- caproyl chitosan nanoparticles（CCS- NPs） and N- caproyl chitosan nanoparticles surface- modified with glycyrrhizin（CCS- NPs GL） and study its stability. METHODS： CCS NPs were prepared hy ionic gelation method and CCS - NPs - GL was obtained though periodate oxidation method. The particle size, zeta potential before and after freeze- drying at different pH value were investigated. The particle size, drug encapsulation efficiency and glycyrrhizin binding ratio of CCS- NPs- GL was investigated at different temperatures.RESULTS： The particle size increased, well - dispersed in salt solution, zeta potential drop was not obvious after freeze - drying. In physiological pH medium, both CCS- NPs and CCS NPs - GL were easy to disperse and had no significant change in particle size. No significant change was noted for CCS - NPs - GL of the particle size, drug encapsulation efficiency and glycyrrhizin binding ratio indifferent temperatures.CONCLUSION： CCS- NPs- GL, as a potential initiative drug carrier, its particle stability can satisfy the research on its intravenously hepatoeyte- targeted delivery and pharmacodynamic evaluation.