Radiolabeling and quantitative in vivo SPECT/CT imaging study of liposomes using the novel iminothiolane-99mTc-Tricarbonyl complex

Z. Varga, Imola Cs Szigyártó, István Gyurkó, Rita Dóczi, I. Horváth, Domokos Máthé, Krisztián Szigeti

Research output: Contribution to journalArticle

3 Citations (Scopus)

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 50MBq 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 blood vessels and high uptake in the liver and spleen were observed.

Original languageEnglish
Article number4693417
JournalContrast Media and Molecular Imaging
Volume2017
DOIs
Publication statusPublished - Jan 1 2017

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Liposomes
Single Photon Emission Computed Tomography Computed Tomography
Sulfhydryl Compounds
Radioisotopes
Pharmaceutical Preparations
Gel Chromatography
Blood Vessels
Spleen
Pharmacokinetics
Lipids
Liver
Serum

ASJC Scopus subject areas

  • Radiology Nuclear Medicine and imaging

Cite this

Radiolabeling and quantitative in vivo SPECT/CT imaging study of liposomes using the novel iminothiolane-99mTc-Tricarbonyl complex. / Varga, Z.; Szigyártó, Imola Cs; Gyurkó, István; Dóczi, Rita; Horváth, I.; Máthé, Domokos; Szigeti, Krisztián.

In: Contrast Media and Molecular Imaging, Vol. 2017, 4693417, 01.01.2017.

Research output: Contribution to journalArticle

Varga, Z. ; Szigyártó, Imola Cs ; Gyurkó, István ; Dóczi, Rita ; Horváth, I. ; Máthé, Domokos ; Szigeti, Krisztián. / Radiolabeling and quantitative in vivo SPECT/CT imaging study of liposomes using the novel iminothiolane-99mTc-Tricarbonyl complex. In: Contrast Media and Molecular Imaging. 2017 ; Vol. 2017.
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