With his high natural abundance, characteristic resonance properties, and its negligible presence in the human body, fluorine is a perfect candidate for in vivo MRI. [1] In the past ten years plenty of studies have been published on the use of 19F-MRI in the diagnosis and treatment of various diseases. [2] Several fluorous reporter agents have been used, mostly consisting of liquid perfluorocarbons (PFC) or perfluoropolyethers (PFPE) administered as nano formulations. In this communication we wish to report the synthesis and full characterization of a novel 19F-MRI reporter consisting of a single highly fluorinated symmetrical molecule and its facile and scalable formulation in water, which yields a stable and monodisperse nanoemulsion of a mean particle size of 150-210 nm, allowing for the dispersion in water of up to 100 mg/ml of the reporter. The unique structure of this molecule results in a single, very intense 19F-NMR peak, which ensures facile identification of the reporter and avoids artefacts formation, particularly in MRI experiments. Biocompatibility was evaluated in vitro on two different cell cultures showing no cytotoxicity and excellent survival rate. Finally both in vitro and in vivo 19F-MRI experiments showed very low detection limits, short acquisition time, and good detectability in vivo, even for small number of cells. These promising results may pave the way to different modifications of the nanoemulsion, allowing several in vivo applications of the reporter, which are under current investigation in our laboratory.
[1] Ruiz-Cabello, J.; Barnett, B.P., Bottomley, P.A.; Bulte, J.W.M. NMR Biomed.
[2] Du, W.; Xu, Z.; Nyström, A.M.; Zhang, K.; Leonard, J.R.; Wooley, K.L. Bioconj Chem 2008, 19, 12, 2492.
claudia.pigliacelli@polimi.it
