毛蕊花苷固体脂质纳米粒的制备及对小鼠急性肝损伤的保护作用  

Preparation of verbascoside solid lipid nanoparticles and its protective effects on acute liver injury in mice

作　　者：杨珊珊[1] 慎爱民[1] 丁立新[1] 孙亦宁 吴磊[1] 

机构地区：[1]佳木斯大学药学院,黑龙江省生物药制剂重点实验室,黑龙江佳木斯154007

出　　处：《中国医院药学杂志》2014年第1期4-8,共5页Chinese Journal of Hospital Pharmacy

基　　金：黑龙江省教育厅科学技术研究项目(编号:12521559);佳木斯大学大学生科技创新项目(编号:xs2013-127)

摘　　要：目的:制备毛蕊花苷固体脂质纳米粒(VER-SLN),并研究VER对四氯化碳(CCl4)诱导的小鼠急性肝损伤的保护作用。方法:采用乳化超声-分散法制备VER-SLN,以包封率为评价指标,进行正交试验筛选最优处方,并考察其形态、粒径和Zeta电位;采用0.1%CCl4造成小鼠急性肝损伤,以测定小鼠血清丙氨酸转氨酶(ALT)和天冬氨酸转氨酶(AST)活性,肝组织中超氧化物歧化酶(SOD)活性和丙二醛(MDA)含量及对肝组织进行病理学检查等指标观察VER-SLN对肝损伤的保护作用。结果:通过正交试验筛选,得到的最优处方外观形态圆整,粒度分布均匀,平均粒径为(109±17)nm,Zeta电位为(-23±0.91)mV,包封率为96.66%;小鼠肝损伤实验表明,VER能明显降低CCl4致小鼠肝损伤血清ALT,AST值,肝组织中MDA的含量,增加肝组织中SOD活性,减轻CCl4对肝脏细胞的病理损伤。结论:该制剂处方设计和工艺方法可行,制剂质量符合要求,对四氯化碳致小鼠急性肝损伤有一定保护作用。OBJECTIVE To prepare verbascoside solid lipid nanoparticles（VER-SLN）and to observe the protective effects of VER-SLN on liver-injury induced by carbon tetrachlotide（CCl4）in mice.METHODS VER-SLN was prepared by emulsion ultrasound dispersing method.The formulation of VER-SLN were optimized by the orthogonal design with the entrapment efficacy as evaluation index;animal model of liver injury was induced by0.1% CCl4in mice.The protective effects of VER-SLN on the model were evaluated by the determination of the activity of serum alanine and aspartate aminotransferase（AST and ALT） activity,the activity of SOD and the MDA content in liver,and the hepatic tissue pathology was observed.RESULTS Screening by orthogonal experiment,the obtained VER-SLN was round and smooth particles with average size of（109±17）nm,Zeta potential（-23±0.91）mV and entrapment efficiency 96.66%.The experimental liver injury in mice showed that following the treatment with VER-SLN,AST and ALT activities,and the content of MDA in liver were obviously reduced;the activity of SOD in liver was obviously increased.Furthermore,the pathological changes were also improved significantly.CONCLUSION The preparation technique and formulation are practicable.VER-SLN is up to the quality standard;it has protective effects on the experimental chronic hepatic injury induced by CCl4in mice.

关 键 词：毛蕊花苷 固体脂质纳米粒 四氯化碳 肝损伤 

分 类 号：R285.5[医药卫生—中药学]