A dual-modal 19F MRI/18F PET approach using sultone-derived chemical tags

Abstract

Biocompatibility and hydrophilicity are key factors in the design of water-soluble imaging probes, particularly for ¹⁹F MRI, where perfluorocarbon contrast agents are typically highly hydrophobic. To address this limitation, two original sultones containing a polyfluorinated pentaerythritol scaffold were developed and evaluated as precursors of hydrophilic and sensitive ¹⁹F MRI tags. Their ring opening with ^19/18F-fluoride led quantitatively to the corresponding polyfluorinated sulfo compounds that demonstrated water-solubility properties suitable for formulation and in vivo injection. ¹⁹F MRI studies in mice, performed with unprecedented low doses (<100 μM) of the stable polyfluorinated sulfo compounds, provided high-contrast whole-body images consistent with PET imaging of their radiofluorinated analogues. These findings demonstrate that polyfluorinated sultones are promising chemical precursors for ¹⁹F MRI and dual ¹⁹F MRI/¹⁸F PET probes, enabling improved diagnostic performance.