Abstract
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Objectives: In this study, we present an unique direct targeting approach by bio-conjugation of [64Cu]CuS with bombesin (Bom) peptide for targeted imaging of orthotopic prostate cancer. Materials and
Methods: [64Cu]CuS NPs were synthesized by a reaction of CuCl2 (CuCl2 with trace amounts of 64CuCl2) and Na2S in the presence of sodium citrate in aqueous solution. Then, lipoamide-PEG-Bom conjugate was linked to the surface of NPs by sodium borohydride (NaBH4) catalyzation. The orthotopic prostate tumor model was established by ventral prostate injection of PC-3-KD1 cancer cells. 6 to 8 weeks post tumor implantation, PET-CT scanning and image analysis were performed using Inveon microPET-CT scanner. Results: Water-soluble Bom-PEG-[64Cu]CuS NPs were synthesized with core diameter of 5.1 ± 0.94 nm using dynamic laser scattering and transmission electron microscope measurement (Figure 1). The in vitro assay indicated that Bom-PEG-[64Cu]CuS NPs had specific cellular uptake in PC-3-KD1 prostate cancer cells (Figure 2) and the in vivo microPET-CT scanning of NPs provided clear insights of orthotopic tumors by hypogastrium at 6h post injection (Figure 3). Conclusion: The combination of small size, integration of positron emitter 64Cu into the core structural component and tumor-targeting capability makes Bom-PEG- [64Cu]CuS nanoparticles ideally suited for PET imaging of orthotopic prostate tumor.
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