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Synthesis of 99mTcV ≡ N-Pazufloxacin dithiocarbamate complex and biological evaluation in Wister rats artificially infected with Escherichia coli

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Abstract

99mTc ≡ N-Pazufloxacin dithiocarbamate (99mTc ≡ N-PZN) complex was synthesized through the [99mTc ≡ N]2+ core and its aptness was radiochemically and biologically evaluated in terms of radiochemical purity (RCP) in saline, in vitro stability in serum, in vitro bacterial uptake and percent in vivo uptake in male Wister rats (MWR) artificially infected with alive and heat killed Escherichia coli (E. coli). The 99mTc ≡ N-PZN complex showed more than 90% RCP up to 4 h after reconstitution in normal saline at room temperature with a maximum RCP value of 98.40 ± 0.28% (at 30 min). At 37 °C in serum the complex showed stable behaviour up to 4 h with the appearance of 15.95% undesirable by products within 16 h of the incubation. The complex showed saturated in vitro binding with E. coli with a maximum uptake of 74.25 ± 0.50% (at 90 min). Normal biodistribution behaviour was noted with a sixfold higher accumulation in the muscle of the MWR, artificially infected with live E. coli as compared to the MWR infected with heat killed E. coli, inflamed and normal muscle. The high RCP in saline, elevated in vitro stability in serum, saturated in vitro binding with E. coli and the sixfold higher accumulation in the infected (live) muscle of the MWR as compared to the inflamed and normal muscle, recognized the aptness of the 99mTc ≡ N-PZND complex as a prospective E. coli in vivo infection radiotracer.

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Authors and Affiliations

  1. Nuclear Medicine Research Laboratory (NMRL), University of Peshawar, Peshawar, KPK, Pakistan

    Syed Qaiser Shah

  2. Phytopharmaceutical & Neutraceuticals Research Laboratory (PNRL), University of Peshawar, Peshawar, KPK, Pakistan

    Muhammad Rafiullah Khan

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  1. Syed Qaiser Shah
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  2. Muhammad Rafiullah Khan
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Correspondence to Syed Qaiser Shah.

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Shah, S.Q., Khan, M.R. Synthesis of 99mTcV ≡ N-Pazufloxacin dithiocarbamate complex and biological evaluation in Wister rats artificially infected with Escherichia coli . J Radioanal Nucl Chem 288, 511–516 (2011). https://doi.org/10.1007/s10967-010-0954-1

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  • DOI: https://doi.org/10.1007/s10967-010-0954-1

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