转铁蛋白修饰共载阿霉素和Rg3脂质体靶向抑制胃癌细胞增殖

TF modified doxorubicin and Rg3 loaded liposome for gastric cancer targeting and therapy

目的制备转铁蛋白修饰共载细胞毒药物阿霉素(doXorubicin,DOX)和抗新生血管药物人参皂甙Rg3脂质体(TF modified doxorubicin and Rg 3loaded liposome,TF—LP—DOX/Rg 3),研究与胃癌细胞的亲和力以及对胃癌细胞的增殖抑制作用。方法采用后插入法制备转铁蛋白修饰共载阿霉索和人参皂甙Rg3脂质体(TF—LP—DOX/Rg 3)。通过定量的细胞摄取实验和定性共聚焦实验研究胃癌细胞对普通脂质体(liiposome,LP)和转铁蛋白修饰脂质体(TF modified liposome,TFLP)的亲和力。MTT实验研究不同载药脂质体对胃癌细胞的增殖抑制能力。构建MKN—28胃癌细胞肿瘤球模型,研究不同脂质体对肿瘤球的穿透能力和肿瘤球生长抑制作用。结果细胞摄取实验结果显示,MKN—28细胞对TF—LP的摄取效率是LP的2.9倍(P<0.01),MTT实验表明,TF—LP—DOX/Rg3对MKN—28细胞的增殖抑制能力显著强于其他组(P<0.01);肿瘤球实验结果显示,TF—LP—DOX/Rg3具有良好的肿瘤球穿透作用和肿瘤球生长抑制作用。结论转铁蛋白修饰共载细胞毒药物阿霉素(D0X)和抗新生血管药物人参皂甙Rg3脂质体是一种潜在高效的胃癌靶向给药系统。

Objective To prepare TF conjugated doxorubicin and Rg 3 loaded liposome and evaluate their properties and effect on the treatment of gastric cancer. Method The liposomes were prepared by thin iflm hydration method. The efifciency of cellular uptake on MKN-28 cells in vitro was evaluated. The anti-proliferation efifciency of TF-LP-DOX/Rg 3 was evaluated by MTT assay. Tumor spheroids were used to evaluate anti-tumor ability of TF-LP-DOX/Rg 3. Results The result demonstrated that TF-LP uptaken by MKN-28 were 2.9 times higher than that of LP(P<0.01). The MTT assay and the inhibition of tumor spheroids in vitro conifrmed strong inhibitory effect of TF-LP-DOX/Rg 3. Conclusion TF-LP-DOX/Rg 3 easily prepared and it is a potential delivery system for the treatment of gastric cancer.