MR/SPECT Imaging Guided Photothermal Therapy of Tumor-Targeting Fe@Fe3O4 Nanoparticles in Vivo with Low Mononuclear Phagocyte Uptake.

The (125)I-c(RGDyK) peptide PEGylated Fe@Fe3O4 nanoparticles ((125)I-RGD-PEG-MNPs) with the average hydrodynamic diameter of ∼40 nm as a novel multifunctional platform were developed for tumor-targeting MR/SPECT imaging guided photothermal therapy in vivo. On the αvβ3-positive U87MG glioblastoma xenograft model, the signals of tumor from T2-weighted MR and SPECT imaging were much higher than those in the blocking group at 6 h post injection (p.i.) of RGD-PEG-MNPs and (125)I-RGD-PEG-MNPs intravenously, respectively. The pharmacokinetics and biodistribution were analyzed quantitatively by gamma counter ex vivo. The fact suggested that RGD-PEG-MNPs exhibited excellent targeting property and low mononuclear phagocyte uptake. At 6 h p.i. for (125)I-RGD-PEG-MNPs, the maximum uptake of 6.75 ± 1.24% of the percentage injected dose per gram (ID/g) was accumulated in the tumor. At 48 h p.i., only 1.11 ± 0.21% and 0.16 ± 0.09% ID/g were accumulated in the liver and spleen, respectively. With the guidance of MR/SPECT imaging, the multifunctional nanoparticles achieved a good photothermal therapeutic efficacy in vivo.