Aim: In the present study, we aimed to characterize the tumor-targeting properties of ultra-small iron oxide nanoparticles (IONPs) as multimodality imaging contrast agent.
Methods: The dimeric cRGD peptides [cyclic(Cys-Arg-Gly-Asp-dSer-Cys)-Tyr-dSer-Lys-Tyr-cyclic(Cys-Arg-Gly-Asp-dSer-Cys)], which specifically targeted integrin-αvβ3 receptor highly overexpressed in tumor vasculature and tumor cells, were covalently conjugated onto the surface of ultra-small IONPs followed by the labeling of nuclide 125I- through the chloramine-T method to afford the desired 125I-(cRGD)2-IONPs nanoprobe.125I-(cRGD)2-IONPs were injected into tumor-bearing mice for magnetic resonance (MR) and single photon emission computed tomography (SPECT) multi-modality imaging of tumors.
Results: The prepared IONPs demonstrated were very useful for T1/T2 and SPECT imaging of tumors in vivo, exhibiting a high tumor uptake of a clinically useful target-to-background ratio in a short time.
Conclusion: We successfully developed a novel integrin-αvβ3 receptor-targeted ultra-small IONPs, which could be successfully used as T1-T2-MRI/SPECT contrast agents for high-resolution and high-sensitivity of tumor imaging in vivo.
Keywords: MRI; dimeric cRGD peptide; integrin αβ; iron oxide NPs; multimodal imaging; single photon emission computed tomography; tumor targeting.