Radiolabeling and Quantitative In Vivo SPECT/CT Imaging Study of Liposomes Using the Novel Iminothiolane-99m Tc-Tricarbonyl Complex

Contrast Media & Molecular Imaging
Zoltán VargaKrisztián Szigeti

Abstract

The in vivo biodistribution of liposomal formulations greatly influences the pharmacokinetics of these novel drugs; therefore the radioisotope labeling of liposomes and the use of nuclear imaging methods for in vivo studies are of great interest. In the present work, a new procedure for the surface labeling of liposomes is presented using the novel 99mTc-tricarbonyl complex. Liposomes mimicking the composition of two FDA approved liposomal drugs were used. In the first step of the labeling, thiol-groups were formed on the surface of the liposomes using Traut's reagent, which were subsequently used to bind 99mTc-tricarbonyl complex to the liposomal surface. The labeling efficiency determined by size exclusion chromatography was 95%, and the stability of the labeled liposomes in bovine serum was found to be 94% over 2 hours. The obtained specific activity was 50 MBq per 1 μmol lipid which falls among the highest values reported for 99mTc labeling of liposomes. Quantitative in vivo SPECT/CT biodistribution studies revealed distinct differences between the labeled liposomes and the free 99mTc-tricarbonyl, which indicates the in vivo stability of the labeling. As the studied liposomes were non-PEGylated, fast clearance from the bloo...Continue Reading

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Citations

Feb 2, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Narottam LamichhaneJaved Mahmood
Jan 26, 2021·Chemical Society Reviews·Juan PellicoRafael T M de Rosales
Feb 23, 2021·Asian Journal of Pharmaceutical Sciences·Panoraia I SiafakaEvren Atlıhan Gündoğdu
Jun 21, 2020·Chemistry and Physics of Lipids·Liliana Aranda-LaraKeila Isaac-Olivé
Nov 25, 2021·Nanomedicine·Samuel BonnetSamuel Legeay

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Methods Mentioned

BETA
dynamic light scattering
transmission electron microscopy
size exclusion chromatography

Software Mentioned

VivoQuant
Chromnav
Fusion

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