透明质酸修饰的绿原酸脂质体对U14宫颈癌荷瘤小鼠的抑制作用  

The Anti Tumor Effect of Hyaluronic Acid Decoreted Chlorogenic Acid Liposomes on Mice Bearing Uterine Cervical Carcinoma(U14)

作　　者：赵玉玺[1] 魏莹[1] 陈珍[1] 张世鹏[1] 张帆[1] 

机构地区：[1]川北医学院药学院药物研究所,四川南充637000

出　　处：《现代生物医学进展》2017年第26期5029-5033,共5页Progress in Modern Biomedicine

基　　金：国家自然科学基金项目(81460637)

摘　　要：目的:对透明质酸(HA)靶向绿原酸(CA)脂质体(HA-CA脂质体)进行处方筛选,以及对U14宫颈癌小鼠的抑制作用实验。方法:筛选制备HA-CA脂质体的方法,并以磷脂比、药脂比、PBS的p H为单因素考察指标通过正交实验筛选最优处方;采用透析袋法考察HA-CA的体外释放;Bal b/c小鼠右腋皮下接种U14宫颈癌瘤株,连续尾静脉注射给药14 d后,摘取瘤体称重,并计算肿瘤生长抑制。结果:采用薄膜分散法制备脂质体,最优处方为磷脂比为4:1,药脂比为1:30,PBS的p H为7.4。HA-CA脂质体与CA脂质体释放曲线基本一致,都具有一定的缓释效果。48 h时,HA-CA脂质体和CA脂质体的累计释放度分别为78.39%、83.01%。HA-CA脂质体对U14宫颈癌小鼠的抑瘤率为60.39%,与阳性对照组环磷酰胺相当,高于CA和CA脂质体。结论:HA-CA脂质体由于其具有主动靶向配体HA的修饰,使其抑制U14宫颈癌裸鼠的效果明显高于CA和CA脂质体。Objective： To optimize the formulation of HA-CA liposomes and to study the anti-tumor effect of HA-CA liposomes on uterine cervical carcinoma mice. Methods： The methods of preparing HA-CA liposomes were screened, and the optimal fomulation was selected by the orthogonal design experiment with the the phospholipids/cholesterol ratio, the drug/lipids ratio and the pH value of PBS buffer was 7.4 as entrapment enfficiency was the index. The release of HA-CA liposomes was studyed by dialysis bag method. Uterine cervical carcinoma cells were inoculated subcutaneously into fight axillary ofBal b/c mice, after continuous treatment of 14 d,we weighed the tumor and calculated the rate of tumor growth inhibition. Results： HA-CA liposomes were prepared by thin film hydration methods. The optimal parameters were as follows： the phospholipids/cholesterol ratio was 4：1, the drug/lipids ratio was 1： 30, the pH value of PBS buffer was 7.4. The release curve of HA-CA liposome and CA liposome was basically the same, both of which a sustained-release efficacy. The cumulative release of HA-CA liposomes and CA liposomes were 78.39% and 83.01% at 48h. The inhibition rate of HA-CA liposomes on U14 cervical cancer mice was 60.39% and significantly higher than that of positive control group, which was higher than that of CA and CA liposomes. Conclusions： HA-CA liposomes can significantly inhibit the effect of U14 cervical cancer nude mice higher than that of CA and CA liposomes owe to the modification of the active target ligand HA.

关 键 词：透明质酸 绿原酸 靶向 脂质体 肿瘤 

分 类 号：R-33[医药卫生] R737.33