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  

Targeted Study of Bufalin-mPEG-PLGA-PLL-cRGD on Colorectal Cancer in Nude Mice

作　　者：胡送娇[1,2] 王炎[1,2] 邱艳艳[1,2] 梁波[1,2] 刘培峰[3] 段友容[3] 彭文[1,2] 殷佩浩[1,2] 仇明[4] 李琦[1,2] 

机构地区：[1]上海中医药大学附属普陀医院 [2]上海中医药大学中西医结合肿瘤介入研究所,200062 [3]上海市肿瘤研究所,200032 [4]第二军医大学附属长征医院腹腔镜外科,上海200003

出　　处：《医学研究杂志》2013年第7期54-57,共4页Journal of Medical Research

基　　金：国家自然科学基金青年科学基金资助项目(81001594);上海市自然科学基金资助项目(11ZR1433200);上海市科委纳米专项基金资助项目(11nm0504500);上海市卫生局中医处基金资助项目(2010QL050B);上海市科委引导基金资助项目(114119B3100);上海市普陀区科委创新重大项目(2011PTKW001)

摘　　要：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。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 bufa- lin 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 in- jection 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.

关 键 词：蟾毒灵 纳米 cRGD 大肠肿瘤 肿瘤靶向 

分 类 号：R977.1[医药卫生—药品]