SOP/GL-CMCNP的制备工艺及肝靶向性评价研究

Preparation and liver targeting evaluation of SOP/GL-CMCNP

纳米粒表面修饰对药物递送与靶向性有显著的影响.旨在探究通过修饰甘草酸提高壳聚糖纳米粒肝靶向性的可行性.以甘草酸为靶分子,壳聚糖为载体制备了负载槐定碱磷脂复合物的纳米粒(SRI/GA-CMCNP),并对其体内外性能进行评价.以载药量和粒径作为评价指标,采用单因素法和正交实验对处方进行优化,并对最优处方制备的纳米粒的形态、体外释放和肝靶向性进行评价.结果表明纳米粒载药量为(5. 84±0. 20)%,平均粒径为(211. 5±4. 47) nm.将所制备的纳米粒经尾静脉注射给予健康小鼠后,具有明显的肝靶向性.制备的纳米粒可有效增加槐定碱的肝靶向性,提高药物在肝脏中的保留时间,为肝靶向性药物的研究提供了实验依据.

Nanoparticle surface modification has a significant impact on drug delivery and targeting.The aim of this paper was to investigate the feasibility of improving the liver targeting of chitosan nanoparticles by modifying glycyrrhizic acid.In this paper,glycyrrhizic acid was used as a target molecule,and chitosan was used as a carrier to prepare nanoparticles(SRI/GA-CMCNP)loaded with saponin complex phospholipid complex,and its in vitro and in vivo properties were evaluated.The drug loading and particle size were used as evaluation indexes.The prescriptions were optimized by single factor method and orthogonal experiment,and the morphology,in vitro release and liver targeting of nanoparticles prepared by optimal formulation were evaluated.The results showed that the most nanoparticle loading was(5.84±0.20)%,and the average particle size was(211.5±4.47)nm.After the prepared nanoparticles were administered to healthy mice via tail vein injection,they have obvious liver targeting properties.The nanoparticles prepared in this paper can effectively increase the liver targeting of sophoridine and improve the retention time of the drug in the liver,and provide an experimental basis for the research of liver-targeted drugs.