透明质酸靶向修饰苦参碱脂质体对肝癌H22小鼠的抑制作用  

Inhibition Effect of Hyaluronic Acid Targeting Modified Matrine Liposome on Murine H22 Hepatocarcinoma

作　　者：赵玉玺 张世鹏 张帆[1] 刘倪 刘福 Zhao Yuxi,Zhang Shipeng,Zhang Fan,Liu Ni,Liu Fu(North Sichuan Medical University,Shchuan,China63700)

机构地区：[1]川北医学院,四川南充637000

出　　处：《中国药业》2018年第16期5-7,共3页China Pharmaceuticals

基　　金：国家自然科学基金[81460637]

摘　　要：目的考察透明质酸靶向修饰苦参碱脂质体(HA-MA脂质体)对肝癌H22小鼠的抑制作用,并进行处方筛选。方法筛选HA-MA脂质体的最佳制备方法;并以磷脂比、药脂比、磷酸盐缓冲液的pH为单因素考察指标,通过正交试验法筛选最佳处方工艺;使用透析袋法检测HA-MA脂质体的体外释放度;裸鼠右腋皮下接种H22肝癌瘤株,尾静脉注射给药14 d后,称取瘤体质量并计算抑瘤率。结果采用薄膜分散法制备脂质体效果最好;最佳处方工艺的磷脂比为3:1,药脂比为1:25,磷酸盐缓冲液的pH=7.4;HA-MA脂质体与苦参碱脂质体释放曲线基本一致,且均有一定缓释效果;HA-MA脂质体对H22肝癌小鼠的抑瘤率与环磷酰胺相近,高于苦参碱和苦参碱脂质体。结论由于透明质酸的修饰,HA-MA脂质体抑制H22肝癌裸鼠的效果明显优于苦参碱和苦参碱脂质体。Objective To investigate the inhibition effect of hyaluronic acid targeting modified matrine liposome（ HA-MA liposome） on murine H22 hepatocarcinoma and optimize the formulation.Methods The method of preparing HA-MA liposome was screened.The formulation was screened by orthogonal design with ratio of phospholipids to cholesterol,ratio of drug to lipid,pH of phosphate buffer solution（ PBS） as the single indexes.The in vitro release of HA-MA liposome was measured by dialysis bag method.The H22 liver tumor was inoculated subcutaneously under the right axilla of nude mice.After 14 d of tail intravenous injection of drugs,the tumor weight was weighed and the tumor inhibition rate was calculated.Results The effect of HA-MA liposome prepared by thin film hydration method was the best,the optimal parameters were as follows：the ratio of phospholipids to cholesterol was 3：1,ratio of drug to lipid was 1：25,pH of PBS buffer was 7.4.The release curve of HA-MA liposome and MA liposome were basically the same,both of them had a sustained-release efficacy.The inhibition rate of HA-MA liposome on H22 hepatocarcinoma was similar to that of cyclophosphamide,but it was higher than that of MA and MA liposome.Conclusion The inhibition effect of HA-MA liposome on H22 hepatocarcinoma nude mice were significantly better than that of MA and MA liposomes owe to the modification of hyaluronic acid.

关 键 词：透明质酸 苦参碱 脂质体 肝癌 肿瘤细胞 抑制作用 靶向修饰 小鼠 

分 类 号：R285.5[医药卫生—中药学] R273[医药卫生—中医学]