载盐霉素的聚乙二醇-神经酰胺胶束的制备和表征  

Preparation and characterization of salinomycin-loaded polyethylene glycol-ceramide micelles

作　　者：王美平[1] 钟延强[1] 高洁[1] 孙治国[1] 鲁莹[1] 

机构地区：[1]第二军医大学药学院药剂学教研室,上海200433

出　　处：《中国新药杂志》2016年第6期716-720,共5页Chinese Journal of New Drugs

摘　　要：目的:构建载盐霉素的聚乙二醇-神经酰胺胶束,增强盐霉素杀伤肝癌细胞和肝癌干细胞的能力,靶向治疗肝癌。方法:采用薄膜分散法制备载盐霉素的聚乙二醇-神经酰胺胶束,并以粒径、载药量、包封率和累积释放量等为指标考察其相关性质,利用CCK-8法测定其细胞毒性。结果:盐霉素和聚乙二醇-神经酰胺摩尔比1∶2,制得的载盐霉素的聚乙二醇-神经酰胺胶束的粒径约为11 nm,Zeta电位为-5.34 m V,载药量为(12.97±0.99)%,包封率为(74.17±3.89)%,48 h的累积释放量为65%,对普通Hep G2肝癌细胞和肝癌干细胞的杀伤IC50值分别为7.51和0.41μmol·L^(-1)。结论:成功制备了粒径较小、分散均一、高包封率和载药量的具有治疗作用的盐霉素胶束,其具有一定的缓释作用和较好的体外杀伤效果,为进一步的体内研究奠定基础。Objective： To prepare salinomycin-loaded polyethylene glycol-ceramide micelles and investigate their characteristics. Methods： Salinomycin-loaded polyethylene glycol-ceramide micelles were prepared by a lipidfilm based method. The particle size,encapsulation efficiency,drug loading and in vitro release and cytotoxicity of the micelles were evaluated. Results： The particle size,Zeta potential,drug loading,and encapsulation efficiencies were 11 nm,- 5. 34 m V,（ 12. 97 ± 0. 99） %,and（ 74. 17 ± 3. 89） %,respectively. The accumulative release rate was up to 65% at 48 h. The IC50 values for cancer cells and cancer stem cells were 7. 51 and 0. 41 μmol·L-1in vitro,respectively. Conclusion： Salinomycin-loaded polyethylene glycol-ceramide micelles showed great potential in antitumor therapy.

关 键 词：聚乙二醇-神经酰胺胶束 盐霉素 薄膜分散法 肿瘤细胞 肿瘤干细胞 

分 类 号：R979.14[医药卫生—药品]