Urokinase Plasminogen Activator Receptor-Mediated Targeting of a Stable Nanocomplex Coupled with Specific Peptides for Imaging of Cancer

Targeting peptides are a promising tool for early diagnosis and therapy of cancer. Overexpression of urokinase plasminogen activator receptor (uPAR) leads to the progression of tumors including prostate, colorectal, ovarian, and breast cancers. To improve the diagnosis and imaging efficiency, herein we report a stable nanocomplex comprising methoxy-PEG-hydrazide (mPEG-H-M)-modified gold nanoparticles (AuNPs) conjugated to uPAR (urokinase plasminogen activator receptor)-targeting peptides GFD (growth factor domain-G) and SMB (somatomedian B-S) for efficient imaging of uPAR-overexpressing cancer cells. Fluorescently labeled targeting peptides were covalently linked to mPEG-H coated AuNPs, characterized, and analyzed by UV–vis spectroscopy, diffraction light scattering (DLS), transmission electron microscopy (TEM), energy-dispersive X-ray spectroscopy (EDX), and fluorescence spectroscopy. In vitro evaluation was assessed with a fluorescence-activated cell sorter (FACS), cell adhesion, and fluorescence microscopy. The peptide-functionalized nanocomplex showed a higher uptake of AuNPs@MGS in comparison with AuNPs@G or AuNPs@S alone in uPAR-overexpressing cells and exhibits no toxicity when analyzed with MTT assay. Our results demonstrated that the developed nanocomplex can be used as a platform for imaging and diagnosis of metastatic tumors.