cells. Finally, Man-DG-DOX exhibits the best in vitro antitumor effect against HepG2 cells among the five Man-DOX conjugates with different linkers. Although the in vitro antitumor activity of Man-DG-DOX is still lower than free DOX, Man-DG-DOX shows significant selectivity toward HepG2 cells. Man-DG-DOX might achieve selective DOX delivery for mannose receptor overexpressed tumors.
在这项工作中,开发了五种具有不同接头的 Man-DOX 偶联物,用于靶向 DOX 递送。具有不同接头的五种 Man-DOX 缀合物的特征在于1H NMR、HRMS、HPLC、UV-vis 和荧光光谱。Man-Suc-DOX、Man-TDG-DOX 和 Man-DG-DOX 可以在去离子
水中自组装成流体动力学直径为 150-200 nm 和负 zeta 电位的近球形纳米颗粒,而 Man-SS-DOX 和Man-SeSe-DOX 几乎不分散在去离子
水中。通过耗散粒子动力学模拟研究了Man-Suc-DOX、Man-TDG-DOX和Man-DG-DOX的自组装行为,结果表明Man-Suc-DOX、Man-TDG-DOX和Man -DG-DOX 全部自组装成球形颗粒,表面有 Man 和接头,内部有 DOX。体外药物释放研究表明,Man-Suc-DOX、Man-TDG-DOX 和 Man-DG-DOX