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99mTc-labeled teicoplanin and its biological evaluation in experimental animals for detection of bacterial infection

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Abstract

Labeling of teicoplanin with 99mTc using SnCl2·2H2O as reducing agent was performed. The dependence of the 99mTc-teicoplanin yield on the concentrations of teicoplanin and reducing agent, pH of the reaction mixture, reaction time, and reaction temperature was studied. Under optimum conditions (2 mg of teicoplanin, 5 μg of SnCl2·2H2O, pH 9, 30 min, 25°C), the labeling yield of 99mTc-teicoplanin of 87.7 ± 1.3% was achieved. 99mTc-teicoplanin is stable for 4 h after labeling; then its relative content decreased gradually to reach 81.7 ± 1.1% in 8 h. Biodistribution studies in mice with infection induced in the left thigh by Staphylococcus aureus were carried out. The bacterial infected thigh/contralateral thigh uptake ratio (T/NT) was evaluated. The time for the maximum accumulation of 99mTc-teicoplanin in the infection site was 2 h after administration of the labeled compound. The abscess-to-muscle ratio for 99mTc-teicoplanin was 4.33 ± 0.3, while that for commercially available 99mTc-ciprofloxacin was 3.8 ± 0.5 under similar conditions. Thus, 99mTc-teicoplanin can be used for infection imaging.

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Correspondence to M. El-Tawoosy.

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Published in Russian in Radiokhimiya, 2014, Vol. 56, No. 5, pp. 462–466.

The text was submitted by the authors in English.

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Motaleb, M.A., El-Tawoosy, M., Mohamed, S.B. et al. 99mTc-labeled teicoplanin and its biological evaluation in experimental animals for detection of bacterial infection. Radiochemistry 56, 544–549 (2014). https://doi.org/10.1134/S1066362214050154

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  • DOI: https://doi.org/10.1134/S1066362214050154

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