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Radiolabelling of lipid-based nanocarriers with fluorine-18 for in vivo tracking by PET

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Surasa Nagachinta, Guillaume Becker, Sylvestre Dammicco, Maria Elisa Serrano, Natacha Leroi, Mohamed Ali Bahri, Alain Plenevaux, Christian Lemaire, Rafael Lopez, André Luxen, Maria De La Fuente

Original languageEnglish
Article number110793
Pages (from-to)110793
JournalColloids And Surfaces B-Biointerfaces
Volume188
DOIs
Published1 Apr 2020

King's Authors

Abstract

Organic nanoparticles made out of biodegradable and biocompatible materials have attracted increased attention in the therapeutic and diagnostic fields. In this study, we attempted to explore a new radiolabelling chelating free strategy for biodegradable sphingomyelin nanometric emulsions with fluorine-18 ( 18F), a radioisotope regularly used in clinic. [ 18F]fluoride was produced by the cyclotron and was incorporated into 4-[ 18F]fluorobenzamido-N-ethylmaleimide ([ 18F]FBEM), which was coupled next to the emulsions previously functionalized with a thiol group, via inclusion of either a thiol-PEG-lipid (SH-PEG 12-C 18), or a peptide-PEG-lipid (Cys-Pro-Ile-Glu-Asp-Arg-Pro-Met-Cys-PEG 8-C 18) derivative. Radiolabelled emulsions were obtained in a rapid and efficient fashion through facile-conjugated chemistry without the use of organic solvents, and characterized in terms of size, polydispersity, surface charge, pH, and osmolarity. PET imaging and biodistribution studies in BALB/c mice allowed obtaining the pharmacokinetics of the radiolabelled emulsions and determining the clearance pathways. Altogether, we confirmed the potential of this new technique for the radiolabelling of lipid-based drug nanosystems for application in PET imaging diagnosis.

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