Preparation and biodistribution of [I-131]linezolid in animal model infection and inflammation


Lambrecht F. , Yilmaz O., DURKAN K. , ÜNAK P. , BAYRAK E.

JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY, vol.281, no.3, pp.415-419, 2009 (Journal Indexed in SCI) identifier identifier

  • Publication Type: Article / Article
  • Volume: 281 Issue: 3
  • Publication Date: 2009
  • Doi Number: 10.1007/s10967-009-0006-x
  • Title of Journal : JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY
  • Page Numbers: pp.415-419
  • Keywords: Linezolid, Infection detection, Bacterial inflamed, S. aureus, I-131, RESISTANT STAPHYLOCOCCUS-AUREUS, ANTIMICROBIAL PEPTIDES, BACTERIAL-INFECTIONS, QUALITY-CONTROL, BIOLOGICAL CHARACTERISTICS, TC-99M-CEFUROXIME AXETIL, DETECTING SITES, EFFICACY, AGENT, TC-99M-CIPROFLOXACIN

Abstract

Linezolid is the first of new class of antibiotics, the oxazolidinones, and exhibits activity against many gram-positive organisms, including vancomycin-resistant Enterococcus faecium, methicillin-resistant Staphylococcus aureus, and penicillin-resistant Streptococcus pneumoniae. Aim of the study: Linezolid was to label with I-131 and potential of the radiolabeled antibiotic was to investigate in inflamed rats with S. aureus ( S. aureus) and sterile inflamed rats with turpentine oil. Linezolid was labeled with I-131 by iodogen method. Biodistribution of [I-131] linezolid was carried out in bacterial inflamed and sterile inflamed rats. Radiolabeling yield of [I-131] linezolid was determined as 85 +/- 1% at pH 2. After injecting of [I-131] linezolid into bacterial inflamed and sterile inflamed rats, radiolabeled linezolid was rapidly removed from the circulation via the kidneys. Binding of [I-131] linezolid to bacterial inflamed muscle (T/NT = 77.48 at 30 min) was five times higher than binding to sterile inflamed muscle (T/NT = 14.87 at 30 min) of rats. [I-131] linezolid showed good localization in bacterial inflamed tissue. It was demonstrated that [I-131] linezolid can be used to detect S. aureus inflammation in rats.