99mTc‐tricabonyl labeling of ofloxacin and its biological evaluation in Staphylococcus aureus as an infection imaging agent. (19th July 2013)

• Record Type: Journal Article
• Authors: Erfani, Mostafa; Doroudi, Alireza; Hadisi, Leila; Andishmand, Ali; Mirshojaei, Seyedeh Fatemeh; Shafiei, Mohammad
• Is Part Of: Journal of labelled compounds & radiopharmaceuticals. Volume 56:Number 12(2013)
• Page Start: 627
• Page End: 631
• Publication Date: 2013-07-19
• Subjects: Tracers (Chemistry) -- Periodicals; Radiopharmaceuticals -- Periodicals; 615.8424
• DOI: 10.1002/jlcr.3093
• Languages: English
• ISSNs: 0362-4803

Abstract

<abstract abstract-type="main"> <title> <x xml:space="preserve">Abstract</x> </title> <p>Even in recent decades, one of the major causes of death and unhealthiness in the whole world is infection and inflammation. The use of radiopharmaceuticals is a powerful tool in managing the patients with infectious diseases. In this study, ofloxacin as a second‐generation fluoroquinolone has been labeled with [<sup>99m</sup>Tc(CO)<sub>3</sub>(H<sub>2</sub>O)<sub>3</sub>]<sup>+</sup> core to formulate a suitable infection imaging agent. Ofloxacin was radiolabeled with <sup>99m</sup>Tc using carbonyl core. Radioligand chemical analysis involved HPLC methods. Radioconjugate stability and lipophilicity were determined. Binding with <italic>Staphylococcus aureus</italic> and biodistribution in infected mice for labeled compound were studied. The radioligand was characterized by HPLC, and its radiochemical purity was more than 90%. <italic>In vitro</italic> stability studies have shown the complex was stable at least 6 h after labeling at room temperature. The <italic>n</italic>‐octanol/water partition coefficient experiment exhibited logP = 1.52 ± 0.21 for <sup>99m</sup>Tc(CO)<sub>3</sub>‐ofloxacin. The complex showed specific binding to <italic>S</italic>. <italic>aureus</italic>. Biodistribution results showed that radioligand had high accumulation in the infected muscle in a mice (T/NT = 2.02 ± 0.12 at 4 h postinjection). On the basis of stability and infection site uptake ratio, suitability of this complex as a radiotracer for imaging of infections is recognized.</p> </abstract>