64Cu-Labeled multifunctional dendrimers for targeted tumor PET imaging

Wenhui Ma; Fanfan Fu; Jingyi Zhu; Rui Huang; Yizhou Zhu; Zhenwei Liu; Jing Wang; Peter S. Conti; Xiangyang Shi; Kai Chen

doi:10.1039/C7NR09269E

⁶⁴Cu-Labeled multifunctional dendrimers for targeted tumor PET imaging†

Wenhui Ma,‡^ab Fanfan Fu,‡^c Jingyi Zhu,^d Rui Huang,^a Yizhou Zhu,^a Zhenwei Liu,^a Jing Wang,^b Peter S. Conti,^a Xiangyang Shi

*^cd and Kai Chen

*^a

Author affiliations

* Corresponding authors

^a Molecular Imaging Center, Department of Radiology, Keck School of Medicine, University of Southern California, Los Angeles, CA 90033, USA
E-mail: chenkai@med.usc.edu

^b Department of Nuclear Medicine, Xijing Hospital, The Fourth Military Medical University, Xi'an, Shaanxi 710032, China

^c College of Chemistry, Chemical Engineering and Biotechnology, Donghua University, Shanghai 201620, China
E-mail: xshi@dhu.edu.cn

^d State Key Laboratory for Modification of Chemical Fibers and Polymer Materials, College of Materials Science and Engineering, Donghua University, Shanghai 201620, China

Abstract

We report the use of multifunctional folic acid (FA)-modified dendrimers as a platform to radiolabel with ⁶⁴Cu for PET imaging of folate receptor (FR)-expressing tumors. In this study, amine-terminated generation 5 (G5) poly(amidoamine) dendrimers were sequentially modified with fluorescein isothiocyanate (FI), FA, and 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA), followed by acetylation of the remaining dendrimer terminal amines. The as-formed multifunctional DOTA-FA-FI-G5·NHAc dendrimers were then radiolabeled with ⁶⁴Cu via the DOTA chelation. We show that the FA modification renders the dendrimers with targeting specificity to cancer cells overexpressing FR in vitro. Importantly, the radiolabeled ⁶⁴Cu-DOTA-FA-FI-G5·NHAc dendrimers can be used as a nanoprobe for specific targeting of FR-overexpressing cancer cells in vitro and targeted microPET imaging of the FR-expressing xenografted tumor model in vivo. The developed ⁶⁴Cu-labeled multifunctional dendrimeric nanoprobe may hold great promise to be used for targeted PET imaging of different types of FR-expressing cancer.

Nanoscale

⁶⁴Cu-Labeled multifunctional dendrimers for targeted tumor PET imaging†

Abstract

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⁶⁴Cu-Labeled multifunctional dendrimers for targeted tumor PET imaging

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