毛菊苣总倍半萜磁性脂质体纳米粒的制备及肝靶向性研究

Cichorium glandulosum is widely distributed in xinjiang, and is used a characteristic medicinal plant for a long history. Sesquiterpene-Rich Fraction (SRF)from Cichorium glandulosum is proved to be effective for hepatoprotective. In this study, SRF was used as a model medicine to prepare the compound targeting preparation with magnetic liposome nanoparticle (MLN) as the carrier. The purpose of which is to enhance the selectivity and targeting of liver lesion sites and improve the bioavailability. The content of lactucin and lactucopicrin and pharmaceutical features as evaluation indexes are to optimize the preparation technology of SRF-MLN by using orthogonal design of L9(34). The drug loading, the entrapment efficiency, the physicochemical property of particle, and in vitro drug release characteristics, in vivo drug distribution were studied. The liver-injury model in mice was made. The content of ALT, AST, TBA, and DBIL in the serum and liver were measured. At the same time, MDA, GSH-Px, SOD activities of the different groups in liver homogenate were compared. pathological change in liver were observed and the liver-protecting mechanism of SRF-MLN was explored. This research will provide a new reference for the preparation and evaluation of liver-targeted drug delivery system of Uigur effective part.

毛菊苣总倍半萜有效部位(SRF)是从新疆特色资源毛菊苣中提取得到的一类天然倍半萜类活性成分，已证明具有确切的肝损伤保护作用。本课题以SRF为模型药物，采用磁性脂质体纳米粒(MLN)为载体制备SRF复合靶向制剂，以增强对肝病变部位的选择性和靶向性，提高生物利用度。以活性成分山莴苣素和山莴苣苦素的含量及药剂学特性为评价指标，采用正交试验设计优化毛菊苣总倍半萜有效部位磁性脂质体纳米粒(SRF-MLN)的制备工艺；通过对制剂载药量、包封率、给药载体的理化性质与体外释药行为、动物体内分布靶向性进行研究，探讨SRF-MLN作为治疗肝损伤药物靶向给药系统的可行性；建立小鼠肝损伤模型，比较各组小鼠血清ALT、AST、TBA、DBIL含量，肝组织匀浆中MDA、GSH、SOD等指标的变化，观察肝脏病理改变，探讨SRF-MLN保护肝脏机制。课题研究结果将为维药有效部位新型肝靶向给药系统的制备与评价提供参考。