Semiconductor quantum dots (QDs), after surface modification to provide water solubility and biocompatibility, have a promising future in biomedical applications. In this study, a dual receptor–targeting dual-modality PET/near-infrared fluorescence (NIRF) probe was developed for accurate assessment of the pharmacokinetics and tumor-targeting efficacy of QDs. Methods: QDs were modified by β-Glu-RGD-BBN (RGD is arginine-glycine-aspartate acid, and BBN is bombesin) peptides and then labeled with ¹⁸F via the 4-nitrophenyl-2-¹⁸F-fluoropropionate prosthetic group. Cytotoxicity and cell-binding assay of QD-RGD-BBN were performed with PC-3 cells. In vivo dual-modality PET/NIRF imaging of prostate tumor–bearing mice was investigated using QD-RGD-BBN and 2-¹⁸F-fluoropropionyl-QD-RGD-BBN (¹⁸F-FP-QD-RGD-BBN). An in vivo biodistribution study of ¹⁸F-FP-QD-RGD-BBN was performed on normal mice. Results: QD-RGD-BBN exhibited strong red luminescence (600–800 nm) with the same maximum fluorescence wavelength (705 nm) as QD705 and slightly lower toxicity than that of QD705 in PC-3 cells at concentrations of greater than 30 μg/mL. Uptake of QD-RGD-BBN in PC-3 cells showed no significant decrease in the presence of an excess amount of dimer arginine-glycine-aspartate acid (RGD₂) or bombesin(7–14) (BBN) peptide but was blocked significantly in the presence of an excess amount of NH₂-RGD-BBN. Dual-function PET/NIRF imaging is able to accurately assess the biodistribution and tumor-targeting efficacy of the ¹⁸F-labeled functionalized QDs. Conclusion: The functionalized QD probe has great potential as a universal dual-targeting probe for detecting tumors in living subjects, opening up a new strategy for the development of multitargeting multimodality ¹⁸F-labeled QD probes with improved tumor-targeting efficacy.

The potential value of multiplexed positron emission tomography (PET) tracers in mice with turpentine-induced inflammation was evaluated and compared with 2-[¹⁸F]fluoro-2-deoxy-D-glucose ([¹⁸F]FDG) for glucose metabolism imaging. These PET tracers included [¹⁸F]fluoromethylcholine ([¹⁸F]FCH) for choline metabolism imaging, (S-[¹¹C]methyl)-D-cysteine ([¹¹C]DMCYS) for amino acid metabolism imaging, [¹¹C]bis(zinc(II)-dipicolylamine) ([¹¹C]DPA-Zn²⁺) for apoptosis imaging, 2-(4-N-[¹¹C]-methylaminophenyl)-6-hydroxybenzothiazole ([¹¹C]PIB) for β amyloid binding imaging, and [¹⁸F]fluoride (¹⁸F⁻) for bone metabolism imaging. In mice with turpentine-induced inflammation mice, the biodistribution of all the tracers mentioned above at 5, 15, 30, 45, and 60 min postinjection was determined. Also, the time-course curves of the tracer uptake ratios for inflammatory thigh muscle (IM) to normal uninflammatory thigh muscle (NM), IM to blood (BL), IM to brain (BR), and IM to liver (LI) were acquired, respectively. Moreover, PET imaging with the tracers within 60 min postinjection on a clinical PET/CT scanner was also conducted. [¹⁸F]FDG and ¹⁸F⁻ showed relatively higher uptake ratios for IM to NM, IM to BL, IM to BR, and IM to LI than [¹⁸F]FCH, [¹¹C]DPA-Zn²⁺, [¹¹C]DMCYS and [¹¹C]PIB, which were highly consistent with the results delineated in PET images. The results demonstrate that ¹⁸F⁻ seems to be a potential PET tracer for inflammation imaging. [¹⁸F]FCH and [¹¹C]DMCYS, with lower accumulation in inflammatory tissue than [¹⁸F]FDG, are not good PET tracers for inflammation imaging. As a promising inflammatory tracer, the chemical structure of [¹¹C]DPA-Zn²⁺ needs to be further optimized.

Radiolabeled cyclic arginine-glycine-aspartic (RGD) peptides can be used for noninvasive determination of integrin α_vβ₃ expression in tumors. In this study, we performed radiosynthesis and biological evaluation of a new ¹⁸F-labeled RGD homodimeric peptide with one 8-amino-3,6-dioxaoctanoic acid (PEG₂) linker on the glutamate β-amino group (¹⁸F-FP-PEG₂-β-Glu-RGD₂) as a symmetric PET tracer for tumor imaging. Biodistribution studies showed that radioactivity of ¹⁸F-FP-PEG₂-β-Glu-RGD₂ was rapidly cleared from blood by predominately renal excretion. MicroPET-CT imaging with ¹⁸F-FP-PEG₂-β-Glu-RGD₂ revealed high tumor contrast and low background in A549 human lung adenocarcinoma-bearing mouse models, PC-3 prostate cancer-bearing mouse models, and orthotopic transplanted C6 brain glioma models. ¹⁸F-FP-PEG₂-β-Glu-RGD₂ exhibited good stability in vitro and in vivo. The results suggest that this tracer is a potential PET tracer for tumor imaging.

In this study, radiosynthesis and biological evaluation of a new [18F]labeled glutamine analogue, N-(2-[18F]fluoropropionyl)-L-glutamine ([18F]FPGLN) for tumor PET imaging are performed. [18F]FPGLN was synthesized via a two-step reaction sequence from 4-nitrophenyl-2-[18F]fluoropropionate ([18F]NFP) with a decay-corrected yield of 30 ± 5% (n=10) and a specific activity of 48 ± 10 GBq/μmol after 125 ± 5 min of radiosynthesis. The biodistribution of [18F]FPGLN was determined in normal Kunming mice and high uptake of [18F]FPGLN was observed within the kidneys and quickly excreted through the urinary bladder. In vitro cell experiments showed that [18F]FPGLN was primarily transported by Na+-dependent system XAG - and was not incorporated into proteins. [18F]FPGLN displayed better stability in vitro than that in vivo. PET/CT studies revealed that intense accumulation of [18F]FPGLN were shown in human SPC-A-1 lung adenocarcinoma and PC-3 prostate cancer xenografts. The results support that [18F]FPGLN seems to be a possible PET tracer for tumor imaging.