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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 construct salinomycin-resistant polyethylene glycol-ceramide micelles to enhance the ability of salinomycin to kill hepatoma cells and hepatoma stem cells and to target hepatocellular carcinoma. Methods: The preparation of polyethylene glycol - ceramide micelles of salinomycin was carried out by thin film dispersion method. The relevant properties were investigated by the particle size, drug loading, entrapment efficiency and cumulative release. The CCK - 8 Method to determine its cytotoxicity. Results: Salinomycin and polyethylene glycol - ceramide molar ratio of 1: 2, the prepared salinomycin polyethylene glycol - ceramide micelles particle size of about 11 nm, Zeta potential of -5.34 m V, the drug loading was (12.97 ± 0.99)%, the entrapment efficiency was (74.17 ± 3.89)% and the cumulative release amount was 48% after 48 h. The IC50 values of killing Hep G2 and HCC stem cells were 7.51 And 0.41μmol·L -1. CONCLUSIONS: Salinomycin-treated micelles with smaller particle size, uniform dispersion, high entrapment efficiency and drug loading have been successfully prepared, which have some sustained-release effects and good killing effect in vitro. As a result, In vivo research to lay the foundation.