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


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.

SUBMITTER: Hernandez-Gil J 

PROVIDER: S-EPMC6552490 | biostudies-literature | 2019 Jun

REPOSITORIES: biostudies-literature

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Development of <sup>68</sup>Ga-labelled ultrasound microbubbles for whole-body PET imaging.

Hernández-Gil Javier J   Braga Marta M   Harriss Bethany I BI   Carroll Laurence S LS   Leow Chee Hau CH   Tang Meng-Xing MX   Aboagye Eric O EO   Long Nicholas J NJ  

Chemical science 20190501 21


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 <i>in vivo</i> whole-body imaging can hamper the development of new MB formulations. Herein, we describe a fast and efficient method for achieving <sup>68</sup>Ga-labelling of MBs after a dire  ...[more]

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