A kit-based aluminium-[18F]fluoride approach to radiolabelled microbubbles

Abstract

The production of ¹⁸F-labelled microbubbles (MBs) via the aluminium-[¹⁸F]fluoride ([¹⁸F]AlF) radiolabelling method and facile inverse-electron-demand Diels–Alder (IEDDA) ‘click’ chemistry is reported. An [¹⁸F]AlF-NODA-labelled tetrazine was synthesised in excellent radiochemical yield (>95% RCY) and efficiently conjugated to a trans-cyclooctene (TCO) functionalised phospholipid (40–50% RCY), which was incorporated into MBs (40–50% RCY). To demonstrate the potential of producing ¹⁸F-labelled MBs for clinical studies, we also describe a kit-based approach which is amenable for use in a hospital radiopharmacy setting.