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

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

doi:10.1016/j.colsurfb.2020.110793

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

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

Neuroimaging

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20 Citations (Scopus)

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.

Original language	English
Article number	110793
Pages (from-to)	110793
Journal	Colloids And Surfaces B-Biointerfaces
Volume	188
DOIs	https://doi.org/10.1016/j.colsurfb.2020.110793
Publication status	Published - 1 Apr 2020

Keywords

Biodistribution
Emulsions
Nanocarriers
Positron Emission Tomography (PET)
Radiolabeling
[ F]FBEM

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10.1016/j.colsurfb.2020.110793

https://linkinghub.elsevier.com/retrieve/pii/S0927776520300230

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title = "Radiolabelling of lipid-based nanocarriers with fluorine-18 for in vivo tracking by PET",

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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AU - Nagachinta, Surasa

AU - Becker, Guillaume

AU - Dammicco, Sylvestre

AU - Serrano, Maria Elisa

AU - Leroi, Natacha

AU - Bahri, Mohamed Ali

AU - Plenevaux, Alain

AU - Lemaire, Christian

AU - Lopez, Rafael

AU - Luxen, André

AU - De La Fuente, Maria

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

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Keywords

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