iRGD修饰脂质体的制备及其结肠癌靶向性研究

摘要

目的：制备 iRGD修饰脂质体（iRGD-LP），研究其结肠癌靶向性。方法采用薄膜分散法制备 iRGD 修饰脂质体（iRGD-LP），研究脂质体的粒径和电位；通过定性和定量细胞摄取实验研究结肠癌RKO细胞对普通脂质体（LP）和iRGD修饰脂质体（iRGD-LP）的摄取效率。构建结肠癌RKO细胞肿瘤球模型，研究脂质体的肿瘤球穿透能力；构建结肠癌裸鼠异位模型，研究iRGD-LP的体内分布。结果 iRGD-LP的粒径为（109.4±12.9）nm，电位为（4.2±1.47）mV；结肠癌RKO细胞对iRGD-LP的摄取效率是LP的3.2倍，差异有统计学意义（P＜0.01）；细胞肿瘤球穿透实验和体内分布实验结果均显示iRGD-LP具有良好的肿瘤细胞靶向性。结论 iRGD修饰脂质体是一种潜在高效的结肠癌靶向给药系统。%Objective To prepare iRGD modified liposome(iRGD-LP)and evaluate their targeting efficiency in vitro and in vivo to colon cancer cell.Methods The iRGD-LP was prepared by film-ultrasonic method,its particle size and Zeta potential were evaluated.The cellular uptake efficiency of RKO cell to LP and iRGD-LP were evaluated in vitro and in vivo.Tumor spheroid model were constructed and the penetration efficiency of solid tumor were evaluated.Ectopic colon cancer nude mice model was constructed,and iRGD -LP distribution in the rat body were studied.Results The particle diameter of iRGD-LP was (109.4 ±12.9)nm with the Zeta potential of (4.2 ±1.47)mV.The cellular uptake efficiency of RKO cell to iRGD-LP were 3.2 times higher than that of LP(P<0.01).The tumor spheroid penetration test and iRGD-LP distribution in vivo imaging results showed iRGD-LP had the strongest fluorescence intensity.Conclusion The iRGD-LP might serve as a promising colon cancer delivery system of antitumor drugs.