N-三甲基壳聚糖包覆茵陈总黄酮脂质体的制备及对小鼠急性肝损伤的保护作用  

Preparation of N-Trimethyl Chitosan-coated Liposomes Loaded with Total Flavones of Artemisia capillaris Thunb. and Protective Effect on Acute Hepatic Injury in Mice

作　　者：倪斌 高畅 方春云 李燕[1] 郭春钰[1] NI Bin;GAO Chang;FANG Chunyun;LI Yan;GUO Chunyu(First Affiliated Hospital of Gannan Medical University,Ganzhou 341000)

机构地区：[1]赣南医学院第一附属医院,江西赣州341000

出　　处：《中国医药工业杂志》2022年第6期857-861,共5页Chinese Journal of Pharmaceuticals

基　　金：江西省教育厅青年基金项目(GJJ170884);赣州市科技局项目(GZ2019ZSF003)。

摘　　要：使用乙醇注入法制备茵陈总黄酮脂质体,再利用带正电荷的N-三甲基壳聚糖对脂质体进行包覆。为了增强脂质体的贮存稳定性,采用冷冻干燥工艺制备冻干品。单因素试验结果显示,采用6%海藻糖作冻干保护剂时冻干品表面光滑平整、再分散性能良好。冻干前后药物包封率为(91.8±0.5)%和(92.5±0.3)%,平均粒径为(164.0±4.2)和(165.5±5.9)nm,多分散性指数(PDI)为0.255±0.007和0.361±0.030,ζ电位为(23.8±0.2)和(21.6±0.4)mV。冻干脂质体复溶后在透射电镜下呈均匀类球形。进一步采用四氯化碳致小鼠急性肝损伤模型考察本品的肝保护作用。结果显示,与模型组相比,本品可明显降低小鼠血清谷丙转氨酶、谷草转氨酶及肝组织中丙二醛的水平,对急性肝损伤保护作用显著。本研究可为难溶性中药成分口服给药系统的设计提供新思路。The liposomes loaded with total flavones of Artemisia capillaris Thunb.were prepared by ethanol injection method,and N-trimethyl chitosan with positive charge was used to coat on the liposomes.Then,lyophilization was adopted to enhance the storage stability of the prepared liposomes.The results of single factor tests showed that lyophilized liposomes with good appearance and reconstitution profiles were obtained by using 6% of trehalose as a lyoprotectant.The encapsulation efficiency,particle size,polydispersity index(PDI) and ζ potential of the liposomes before and after lyophilization were (91.8±0.5)% and (92.5±0.3)%,(164.0±4.2) and (165.5±5.9)nm,0.255±0.007 and 0.361±0.030,(23.8±0.2) and (21.6±0.4)mV,respectively.Under the transmission electron microscope,the reconstituted liposomes were spherical in shape.Furthermore,the liver protection effect of the liposomes was investigated with carbon tetrachloride-induced acute liver injury in murine models.Compared with model group,the levels of alanine aminotransferase(ALT),glutamic-oxaloacetic transaminase(AST) in serum and malonaldehyde in liver tissue of the liposomes treated group were significantly reduced,which demonstrated the title liposomes had a remarkable protective effect on acute hepatic injury in mice.This study can provide a new idea for the oral delivery of traditional Chinese medicine components with low solubility.

关 键 词：茵陈 总黄酮 三甲基壳聚糖 脂质体 冻干 稳定性 急性肝损伤 

分 类 号：R944.9[医药卫生—药剂学]