The development of efficient magnetic resonance imaging (MRI) contrast agents (CAs) for early detection, disease monitoring, and evaluation of treatment is an important component of biomedical imaging research. 1H MRI is the most frequently used technique, but suffers from strong background signal. CAs based on fluorinated molecules using 19F MRI techniques, have the potential to generate images with high CNR due to the lack of endogenous 19F in soft tissue. However, developing 19F MRI CAs with sufficient fluorine content remains challenging. Most of the current 19F MRI CAs under study are based on hydrophobic perfluorocarbons (PFCs) and perfluoropolyethers (PFPEs), which limits formulation options and in vivo applications. We report herein, the synthesis and preliminary evaluation of a highly water soluble fluorinated molecule bearing 24 magnetically equivalent 19F atoms. It was characterized by 1H, 13C, 19F NMRs, and Mass Spectrometry. The aqueous solubility allowed formulation of liposomal nanoparticle-based CAs with a 19F content of 17.2 mg/mL and mean particle diameter range of 145-200 nm. 19F MRI phantom studies using a spin echo sequence on a novel 1 Tesla instrument resulted in images with CNR &gt;40 at 0.25 M concentration of the molecule. A preliminary toxicity study on RAW264.7 macrophages showed that greater than 85% of the cells were metabolically active following treatment with the compound and at concentrations ≤ 30 mM, for up to 24 hours. Details of the chemical synthesis, liposomal nanoparticle formulation, 19F MRI and toxicity data, as well as ongoing in vivo studies will be presented.

Synthesis and evaluation of novel hydrophilic molecule for 19F MRI application

255th National Meeting (2018)

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.