RGD修饰的载蟾毒灵多级靶向纳米粒在裸鼠人肝癌移植瘤中的靶向研究

Tumor-targeting Efficiency of Bufalin-loaded mPEG-PLGA-PLL-cRGD Nanoparticles in Hepatocellular Carcinoma-bearing Nude Mice

目的观察RGD修饰的载蟾毒灵多级靶向纳米粒对荷LM3肝癌裸鼠的靶向性,为蟾毒灵纳米粒的肝癌临床治疗提供依据和方法。方法两组荷LM3肝癌裸鼠分别注射Dir-bufalin-mPEG-PLGA-PLL和Dir-bufalin-mPEG-PLGA-PLL-cRGD纳米粒,于药物注射后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,注射Dir-bufalin-mPEG-PLGA-PLL-cRGD纳米粒的荷瘤裸鼠肝脏肿瘤部位显示出较高的荧光强度。结论 RGD修饰的载蟾毒灵多级靶向纳米粒具有更有效的瘤体靶向性,可能为临床抗肝癌治疗提供实验基础和理论依据。

Objective To observe the targeting efficacy of bufalin - loaded mPEG - PLGA - PLL - cRGD nanoparticles （ bufalin - mPEG - PLGA - PLL - cRGD NPs） in LM3 hepatocellular carcinoma - bearing nude mice and to provide the basis and method for the hepa- tocellular clinical treatment of the bufalin nanoparticles. Methods The mice were classified into 2 groups, At 3 and 19 hours after injec- tion, the tumor fluorescence intensity of the mice were observated via in vivo targeting fluorescence imaging. Results After 3 and 19 hours after injection, compared with the Dir - bufalin - mPEG - PLGA - PLL nanoparticles, the tumor fluorescence intensity of the LM3 hepatocel- lular carcinoma - bearing nude mice injected Dir - bufalin - mPEG - of PLGA - PLL - cRGD nanoparticles showed the higher. Conclusion The cRGD moiety resulted in better tumor targeting in vivo. This may provide theoretical basis for clinical treatment.