Abstract

In the current study radio complexation of the moxifloxacin dithiocarbamate (MXND) with technetium-99m (99mTc) using the [99mTc–N]2+ core through legend exchange reaction was explored. The 99mTcN–MXND complex was biologically evaluated as a potential radiopharmaceutical for in vivo scintigraphy using artificially infected male sprague–dawley rats (MSDR) with Staphylococcus aureus (S. aureus). The radiochemistry of the complex was explored in terms of radiochemical purity (RCP), in vitro stability in serum at 37 °C for 16 h, in vitro binding with S. aureus and biodistribution in artificially infected with S. aureus MSDR. It was observed that the complex showed stability of more than 90% up to 4 h after reconstitution with a maximum RCP value of 97.55 ± 0.42% at 30 min. The complex showed significantly in vitro stability in serum at 37 °C with an insignificant free species up to 16.50% within 16 h. In vitro saturated binding with S. aureus was noted up to 120 min with maximum value of 73.25% at 90 min of incubation. Almost sixfold uptake was noted in the infected muscle of the MSDR as compared to inflamed and normal muscle. The 97.55 ± 0.42% RCP values, stability in serum with insignificant untagged 16.50% species, 73.25% in vitro binding with S. aureus and sixfold uptake in the target organ posed the 99mTcN–MXND complex as a promising radiopharmaceutical for S. aureus infectious foci.

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