Tc-99m-Labeled RGD-Polyethylenimine Conjugates with Entrapped Gold Nanoparticles in the Cavities for Dual-Mode SPECT/CT Imaging of Hepatic Carcinoma

作者：Zhou Benqing; Wang Ruizhi; Chen Feng; Zhao Lingzhou; Wang Peng; Li Xin; Banyai Istvan^*; Ouyang Qiang^*; Shi Xiangyang; Shen Mingwu^*

来源：ACS APPLIED MATERIALS & INTERFACES, 2018, 10(7): 6146-6154.

DOI：10.1021/acsami.7b17107

• gold nanoparticles
• Tc-99m
• polyethylenimine
• SPECT/CT imaging hepatic carcinoma

We report the construction and characterization of Tc-99m-labeled arginine-glycine-aspartic acid (RGD)-polyethylenimine (PEI) conjugates with entrapped gold nanoparticles in the cavities (RGD-Tc-99m-Au PENPs) for dual mode single-photon emission computed tomography (SPECT)/computed tomography (CT) imaging of an orthotopic hepatic carcinoma model. In this study, PEI was successively decorated with diethylenetriaminepentaacetic acid, poly(ethylene glycol) (PEG), and PEGylated RGD segments, and was utilized as an effective nanoplatform to entrap Au NPs and to be labeled with Tc-99m. We showed that the designed RGD-Tc-99m-Au PENPs displayed desirable colloidal stability and radiostability, and cytocompatibility in the investigated concentration range, and could be specifically uptaken by alpha(v)beta(3) integrin-overexpressing liver cancer cells in vitro. In vivo CT and SPECT imaging results indicated that the particles were able to be accumulated within an orthotopic hepatic carcinoma and displayed both CT and SPECT contrast enhancement in the tumor tissue. With the proven biocompatibility in vivo via histological examinations, the designed RGD-Tc-99m-Au PENPs may be potentially employed as an effective nanoprobe for a highly efficient dual-mode SPECT/CT imaging of various alpha(v)beta(3) integrin-overexpressing tumors.

• 单位
  东华大学; 上海交通大学