Tumor Targeting and Imaging Using Cyclic RGD-PEGylated Gold Nanoparticle Probes with Directly Conjugated Iodine-125

作者：Kim Young Hwa; Jeon Jongho; Hong Su Hyun; Rhim Won Kyu; Lee Yun Sang; Youn Hyewon; Chung June Key; Lee Myung Chul; Lee Dong Soo; Kang Keon Wook^*; Nam Jwa Min

来源：Small, 2011, 7(14): 2052-2060.

DOI：10.1002/smll.201100927

Radioactive iodine-labeled, cyclic RGD-PEGylated gold nanoparticle (AuNP) probes are designed and synthesized for targeting cancer cells and imaging tumor sites. These iodine-125-labeled cRGD-PEG-AuNP probes are stable in various conditions including a range of pHs and high salt and temperature conditions. These probes can target selectively and be taken up by tumor cells via integrin alpha(v)beta(3)-receptor-mediated endocytosis with no cytotoxicity. The probes show a significant increase in the avidity of alpha(v)beta(3) integrin compared to the corresponding free cRGD peptides. In-vivo SPECT/CT imaging results show that the iodine-125-labeled cRGD-PEG-AuNP probes can target the tumor site as soon as 10 min after injection, and also that cyclic RGD peptides are needed for efficient and long-term in-vivo monitoring. The results suggest that the probes circulate through the whole body, including renal filtration, and are excretable. These promising results show that radioactive-iodine-labeled gold nanoprobes have potential for highly specific and sensitive tumor imaging or for use as angiogenesis-targeted SPECT/CT imaging probes.

• 出版日期2011-7-18