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Preparation and preclinical evaluation of 99mTc-diclofenac as a model for inflammation imaging

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Abstract

Experiments on labeling of diclofenac, an anti-inflammatory drug, with 99mTc were performed. High (about 96%) yield of 99mTc-diclofenac is reached under the following conditions: 50 μg of Sn(II), 100 μg of the substrate, 30 min, pH 7. 99mTc-diclofenac was stable for 4 h. Biological distribution of 99mTc-diclofenac was investigated in mice bearing inflammations experimentally induced in the left thigh by Escherichia coli (bacterial infection model) and turpentine oil (sterile inflammation model). The uptake ratio in the inflamed and contralateral thighs (target-to-nontarget, T/NT) was evaluated. In the case of bacterial infection, the T/NT ratio only slightly exceeds unity, whereas in the case of sterile inflammation it reaches 4.46 ± 0.07 in 2 h. Thus, 99mTc-diclofenac allows differentiation between septic and aseptic inflammation and can be recommended for further clinical trials.

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Authors and Affiliations

  1. Hot Laboratories Center, Atomic Energy Authority, P.O. Box 13759, Cairo, Egypt

    M. El-Tawoosy, A. F. Mahmoud & S. E. Soliman

Authors
  1. M. El-Tawoosy
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  2. A. F. Mahmoud
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  3. S. E. Soliman
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Correspondence to M. El-Tawoosy.

Additional information

Published in Russian in Radiokhimiya, 2014, Vol. 56, No. 6, pp. 531–535.

The text was submitted by the authors in English.

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El-Tawoosy, M., Mahmoud, A.F. & Soliman, S.E. Preparation and preclinical evaluation of 99mTc-diclofenac as a model for inflammation imaging. Radiochemistry 56, 622–627 (2014). https://doi.org/10.1134/S1066362214060071

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  • DOI: https://doi.org/10.1134/S1066362214060071

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