Renal-Clearable Peptide-Functionalized Ba2GdF7 Nanoparticles for Positive Tumor-Targeting Dual-Mode Bioimaging.

Abstract

Considering the dilemma between the effective tumor targeting and the avoidance of potential toxicity, it is desired to design nanoprobes with positive tumor-targeting and good renal clearance ability. In the present work, we developed epidermal growth factor receptor (EGFR)-targeted peptide-functionalized Ba2GdF7 nanoparticles (termed as pEGFR-targeted Ba2GdF7 NPs) for positive tumor-targeting magnetic resonance imaging and X-ray computed tomography (MRI/CT) dual-mode bioimaging. The positive tumor-targeting ability of pEGFR-targeted Ba2GdF7 NPs is achieved by conjugation of EGFR-targeted peptides on the 6.5 nm Ba2GdF7 NP surface through the formation of Gd-phosphonate coordinate bonds. The pEGFR-targeted Ba2GdF7 NPs display desirable cytocompatibility in the test concentration range and high binding affinity with lung cancer cells. In vivo MR and CT imaging results demonstrate that the pEGFR-targeted Ba2GdF7 NPs are able to be accumulated and detained within an engrafted A549 lung carcinoma, which enhances both MR and CT contrast in the tumor tissue. Systematic in vivo experimental results further demonstrate that the pEGFR-targeted Ba2GdF7 NPs have favorable in vivo renal clearance kinetics as well as reasonable in vivo biocompatibility.