Development of 68Ga-labelled ultrasound microbubbles for whole-body PET imaging

Javier Hernández-Gil, Marta Braga, Bethany I. Harriss, Laurence S. Carroll, Chee Hau Leow, Meng Xing Tang, Eric O. Aboagye, Nicholas J. Long

Research output: Contribution to journalArticlepeer-review

Abstract

Microbubble (MB) contrast agents have revolutionalised the way ultrasound (US) imaging can be used clinically and pre-clinically. Contrast-enhanced US offers improvements in soft-tissue contrast, as well as the ability to visualise disease processes at the molecular level. However, its inability to provide in vivo whole-body imaging can hamper the development of new MB formulations. Herein, we describe a fast and efficient method for achieving 68Ga-labelling of MBs after a direct comparison of two different strategies. The optimised approach produces 68Ga-labelled MBs in good yields through the bioorthogonal inverse-electron-demand Diel-Alder reaction between a trans-cyclooctene-modified phospholipid and a new tetrazine-bearing HBED-CC chelator. The ability to noninvasively study the whole-body distribution of 68Ga-labelled MBs was demonstrated in vivo using positron emission tomography (PET). This method could be broadly applicable to other phospholipid-based formulations, providing accessible solutions for in vivo tracking of MBs.

Original languageEnglish (US)
Pages (from-to)5603-5615
Number of pages13
JournalChemical Science
Volume10
Issue number21
DOIs
StatePublished - 2019
Externally publishedYes

ASJC Scopus subject areas

  • Chemistry(all)

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