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合成了叶酸-聚乙二醇-二硬脂酰磷脂酰乙醇胺(Folate-PEG-DSPE),并用其作为靶向肿瘤的功能性材料,以甲氧基聚乙二醇-二硬脂酰磷脂酰乙醇胺(MPEG-DSPE)作为骨架材料,采用成膜水化法制备载多柔比星(1)胶束。所得胶束呈球状结构,粒径为(20±5)nm,叶酸修饰和非叶酸修饰胶束的包封率和载药量分别为(78.8±1.52)%、(79.2±147)%和(1 3.6±1.26)%、(1 3.9±1.19)%。流式细胞结果显示,分别给予游离罗丹明B(Rh B)、叶酸修饰和非叶酸修饰的载RhB胶束,摄取荧光的巨噬细胞分别占细胞总数的36.6%、1.5%和4.4%,说明聚合物胶束可显著减弱巨噬细胞的吞噬作用。体外抗KB人口腔上皮癌细胞活性的试验结果显示,1、叶酸修饰和非叶酸修饰胶束的IC_(50)分别为29 7、0.61和4.12μmol/L,表明叶酸修饰的聚合物胶束能显著提高1的抗肿瘤活性。
Folate-PEG-DSPE was synthesized and used as a functional tumor-targeting material. Poly (ethylene glycol) -distearylphosphatidyl Ethanolamine (MPEG-DSPE) was used as the framework material to prepare doxorubicin (1) micelles by the film-forming hydration method. The resulting micelles were spherical in shape with a diameter of (20 ± 5) nm. The entrapment efficiency and drug loading of folate-modified and non-folate-modified micelles were (78.8 ± 1.52)%, (79.2 ± 147)% and 1 3.6 ± 1.26%, (1 3.9 ± 1.19)%. Flow cytometry results showed that RhB, folic acid-modified and non-folic acid-modified RhB-loaded micelles, respectively, and fluorescence macrophages uptake accounted for 36.6%, 1.5% and 4.4% of the total number of cells respectively Polymeric micelles can significantly reduce macrophage phagocytosis. The results of in vitro anti-KB human oral cancer cell activity showed that IC50 of folic acid-modified and non-folic acid-modified micelles were 29.7, 0.61 and 4.12 μmol / L, respectively, indicating that folic acid-modified polymer micelles can Significantly increased anti-tumor activity of 1.