1 Technical Efficacy: Stage 2 J. Magn. Reson. Imaging 2018;48:1617-1625.

Fluorine-19 (19 F) magnetic resonance (MR) molecular imaging is a promising noninvasive and quantitative molecular imaging approach with intensive research due to the high sensitivity and low endogenous background signal of the 19 F atom in vivo. Perfluorocarbons (PFCs) have been used as blood substitutes since 1970s. More recently, a variety of PFC nanoparticles have been designed for the detection and imaging of physiological and pathological changes. These molecular imaging probes have been developed to label cells, target specific epitopes in tumors, monitor the prognosis and therapy efficacy and quantitate characterization of tumors and changes in tumor microenvironment noninvasively, therefore, significantly improving the prognosis and therapy efficacy. Herein, we discuss the recent development and applications of 19 F MR techniques with PFC nanoparticles in biomedicine, with particular emphasis on ligand-targeted and quantitative 19 F MR imaging approaches for tumor detection, oxygenation measurement, smart stimulus response and therapy efficacy monitoring, et al.

Objectivesc-Met is a receptor tyrosine kinase shown inappropriate expression and actively involved in progression and metastasis in most types of human cancer. Development of c-Met-targeted imaging and therapeutic agents would be extremely useful. Previous studies reported that c-Met-binding peptide (Met-pep1, ) specifically targets c-Met receptor. Here, we evaluated 18F-labeled Met-pep1 for PET imaging of c-Met positive tumor in human head and neck squamous cell carcinoma (HNSCC) xenografted mice.Methodsc-Met-binding peptide, Met-pep1, was synthesized and labeled with 4-nitrophenyl [18F]-2-fluoropropionate ([18F]-NPFP) ([18F]FP-Met-pep1). The cell uptake, internalization and efflux of [18F]FP-Met-pep1 were assessed in UM-SCC-22B cells. In vivo pharmacokinetics, blocking and biodistribution of the radiotracers were investigated in tumor-bearing nude mice by microPET imaging.ResultsThe radiolabeling yield for [18F]FP-Met-pep1 was over 55% with 97% purity. [18F]FP-Met-pep1 showed high tumor uptake in UM-SCC-22B tumor-bearing mice with clear visualization. The specificity of the imaging tracer was confirmed by significantly decreased tumor uptake after co-administration of unlabeled Met-pep1 peptides. Prominent uptake and rapid excretion of [18F]FP-Met-pep1 was also observed in the kidney, suggesting this tracer is mainly excreted through the renal-urinary routes. Ex vivo biodistribution showed similar results that were consistent with microPET imaging data.ConclusionsThese results suggest that 18F-labeled c-Met peptide may potentially be used for imaging c-Met positive HNSCC cancer in vivo and for c-Met-targeted cancer therapy.

Aim: To demonstrate the feasibility of intratracheal administration in orthotopic lung cancer model with 19F MRI. Materials & methods: αvβ3-integrin targeting ability of the perfluorocarbon (PFC) nanoparticles was tested. Orthotopic lung cancer model was established in rabbits under computed tomography guidance. αvβ3-targeted PFC nanoparticles were administrated intratracheally or intravenously, and 19F MRI was performed before and up to 24 h after administration. Results: The targeted PFC nanoparticles could bind with αvβ3-integrin. PFC concentrations in the tumors of intratracheal group after administration were significantly higher than intravenous group. Conclusion: Intratracheal administration of PFC nanoparticles was shown to be feasible and efficacious. 19F MRI with αvβ3-targeted PFC nanoparticles provided quantitative assessment of nanoparticles distribution and tumor angiogenesis.