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Synthesis, physicochemical and in vitro biological evaluation of 99mTc-cefepime radioconjugates, and development of DTPA-cefepime single vial kit formulation for labelling with technetium-99m

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Abstract

In the present work the synthesis, physicochemical properties and biological evaluation of cefepime (CFM) labelled with technetium-99m were studied. Two different synthesis routes of DTPA-CFM as well as the radiolabelling conditions were described. Radiochemical purity of the radioconjugates determined using radio-TLC and HPLC methods with radiochemical detection was higher than 95%. The obtained [99mTc]Tc-DTPA-CFM radioconjugate is highly hydrophilic (logD = − 4.00 \(\pm\) 0.14) and positively charged. It is completely stable in the presence of an excess of cysteine or histidine, acceptably stable in human serum and shows satisfactorily binding to the Staphylococcus aureus cell wall. Based on our results the [99mTc]Tc-DTPA-CFM radioconjugate may be considered to be a diagnostic radiopharmaceutical for detection of staphylococcal infections.

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Acknowledgements

This research was funded by National Science Centre (Poland), grant number 2017/01/X/ST4/00925. The contribution of PhD student Paweł Halik has been done in the frame of the National Centre for Research and Development Project No POWR.03.02.00-00-I009/17 (Radiopharmaceuticals for molecularly targeted diagnosis and therapy, RadFarm, Operational Project Knowledge Education Development 2014-2020 co-financed by European Social Fund). The authors thank Małgorzata Murawska for technical assistance.

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  1. Centre of Radiochemistry and Nuclear Chemistry, Institute of Nuclear Chemistry and Technology, Dorodna16, 03-195, Warsaw, Poland

    Przemysław Koźmiński, Agata Piądłowska, Paweł Halik & Ewa Gniazdowska

  2. Department of Preclinical Sciences, Division of Microbiology, Warsaw, Institute of Veterinary Medicine, University of Life Sciences - SGGW, Ciszewskiego 8, 02-786, Warsaw, Poland

    Magdalena Rzewuska

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  1. Przemysław Koźmiński
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Correspondence to Przemysław Koźmiński.

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Koźmiński, P., Rzewuska, M., Piądłowska, A. et al. Synthesis, physicochemical and in vitro biological evaluation of 99mTc-cefepime radioconjugates, and development of DTPA-cefepime single vial kit formulation for labelling with technetium-99m. J Radioanal Nucl Chem 331, 2883–2894 (2022). https://doi.org/10.1007/s10967-022-08363-5

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  • DOI: https://doi.org/10.1007/s10967-022-08363-5

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