RGD修饰的载蟾毒灵纳米粒在裸鼠人大肠癌模型中的靶向性研究

摘要

Objective To investigate the in vivo targeting efficacy of nanoparticles (NPs) made of methoxy polyethylene glycol (mPEG),polylactic-co-glycolic acid (PLGA),poly-1-lysine (PLL),and cyclic arginine-glycine-aspartic acid (cRGD) loaded with bufalin (bufalin-mPEG-PLGA-PLL-cRGD NPs),and to provide experimental evidence and method for the application of bufalin to treat colon cancer.Methods The mice were classified into 2 groups on the basis of the nanoparticles that they were administered:Dir-bufalin-mPEG-PLGA-PLL-cRGD NPs group and Dir-bufalin-of mPEG-of PLGA-PLL-cRGD NPs group,by injection through the vena caudalis one time in the experience.Fluorescence imaging of the tumor bearing mice was performed at 3 and 19h after injection by using a small animal in vivo fluorescence imaging system.Results Compared with the Dir-bufalin-mPEG-PLGA-PLL nanoparticles,the tumor fluorescence intensity of the mice treated with Dir-mPEG-PLGA-PLL-cRGD NPs was relatively stronger and lasted longer at 3h and 19h post-injection.Conclusion The Dir-bufalin-mPEG-PLGA-PLL-cRGD nanoparticles resulted in better tumor targeting and longer residue time in vivo.The experimental data show that the nanoparticles can help to improve the treatment effect of colorectal cancer.%目的 探讨bufalin-mPEG-PLGA-PLL-cRGD体内药物靶向分布规律,为大肠癌的临床治疗提供实验依据和方法.方法 建立荷C26结肠癌裸鼠模型,并随机分为两组:Dir-bufalin-mPEG-PLGA-PLL纳米组和Dir-bufalin-mPEG-PLGA-PLL-cRGD纳米组,经尾静脉给药.药物注射后3、19h后采用活体成像系统测定裸鼠活体的荧光强度.结果 注射纳米粒3、19h后,与Dir-bufalin-mPEG-PLGA-PLL纳米粒相比,注Dir-bufalin-mPEG-PLGA-PLL-cRGD纳米粒的荷瘤裸鼠肿瘤部位显示出较高的荧光强度.结论 Dir-bufalin-mPEG-PLGA-PLL-cRGD纳米粒能更有效地靶向大肠癌.本实验制备的载药纳米粒的体内荧光活体成像实验数据表明,该纳米粒有助于提高大肠癌的治疗效果.