Synthesis and experimental study of norfloxacin labeled with technecium-99m as a potential agent for infection imaging

Svetlana Ivanovna Sazonova, Yuriy Borisovich Lishmanov, Natalia Valerievna Varlamova, Viktor Sergeevich Skuridin, Yulia Nikolayevna Ilushenkova, Maria Rostislavovna Karpova, Evgeny Alexandrovich Nesterov

Research output: Contribution to journalArticle

3 Citations (Scopus)

Abstract

Introduction: Differentiation between infection and sterile inflammation is one of the most difficult medical problems and is relevant in many clinical situations. Scintigraphy with radiolabeled antibiotics, especially labeled fluoroquinolones, is a promising tool for diagnosing bacterial inflammation. We have attempted to synthesize <sup>99m</sup>Tc-norfloxacin and studied its properties in experiment. Methods: In present study we labeled norfloxacin with 99mTc, determined its radiochemical purity by thin-layer chromatography procedure, compared the bactericidal activity of <sup>99m</sup>Tc-norfloxacin and unlabelled norfloxacin by disk diffusion, performed in vitro binding assays and evaluated the feasibility of <sup>99m</sup>Tc-norfloxacin to image soft-tissue infections in rat modal of thigh muscle infection. Scintigraphy was performed at 30 min, 90 min and 18 h post injection. Abscess -to-normal-site ratios were calculated. Results: In this study <sup>99m</sup>Tc-norfloxacin with high radiochemical purity and low colloid content was synthesized. Disk diffusion method showed that <sup>99m</sup>Tc-norfloxacin retains bactericidal properties of unlabelled norfloxacin. In vitro binding studies demonstrated small degree of the tracer binding with S. aureus and ability of <sup>99m</sup>Tc-norfloxacin to bind with killed as well as alive bacteria. Uptake of the tracer was clearly visible in infected muscles and not visible in sterile inflammed muscles. Conclusion: The <sup>99m</sup>Tc-norfloxacin retains bactericidal properties of unlabelled norfloxacin. The tracer demonstrated small degree of S. aureus binding both with killed as well as alive bacteria. Studies which were performed in vivo in rats with a model of thigh muscle infection showed good ability of the radiopharmaceutical to image the infection.

Original languageEnglish
Pages (from-to)73-81
Number of pages9
JournalIranian Journal of Nuclear Medicine
Volume23
Issue number2
Publication statusPublished - 1 Jun 2015

Fingerprint

Norfloxacin
Infection
Muscles
Thigh
Radionuclide Imaging
Inflammation
Bacteria
Soft Tissue Infections
Radiopharmaceuticals
Fluoroquinolones
Colloids
Thin Layer Chromatography
Abscess

Keywords

  • Infection
  • Inflammation
  • Norfloxacin
  • Scintigraphy
  • Technecium-99m

ASJC Scopus subject areas

  • Radiology Nuclear Medicine and imaging

Cite this

Synthesis and experimental study of norfloxacin labeled with technecium-99m as a potential agent for infection imaging. / Sazonova, Svetlana Ivanovna; Lishmanov, Yuriy Borisovich; Varlamova, Natalia Valerievna; Skuridin, Viktor Sergeevich; Ilushenkova, Yulia Nikolayevna; Karpova, Maria Rostislavovna; Nesterov, Evgeny Alexandrovich.

In: Iranian Journal of Nuclear Medicine, Vol. 23, No. 2, 01.06.2015, p. 73-81.

Research output: Contribution to journalArticle

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abstract = "Introduction: Differentiation between infection and sterile inflammation is one of the most difficult medical problems and is relevant in many clinical situations. Scintigraphy with radiolabeled antibiotics, especially labeled fluoroquinolones, is a promising tool for diagnosing bacterial inflammation. We have attempted to synthesize 99mTc-norfloxacin and studied its properties in experiment. Methods: In present study we labeled norfloxacin with 99mTc, determined its radiochemical purity by thin-layer chromatography procedure, compared the bactericidal activity of 99mTc-norfloxacin and unlabelled norfloxacin by disk diffusion, performed in vitro binding assays and evaluated the feasibility of 99mTc-norfloxacin to image soft-tissue infections in rat modal of thigh muscle infection. Scintigraphy was performed at 30 min, 90 min and 18 h post injection. Abscess -to-normal-site ratios were calculated. Results: In this study 99mTc-norfloxacin with high radiochemical purity and low colloid content was synthesized. Disk diffusion method showed that 99mTc-norfloxacin retains bactericidal properties of unlabelled norfloxacin. In vitro binding studies demonstrated small degree of the tracer binding with S. aureus and ability of 99mTc-norfloxacin to bind with killed as well as alive bacteria. Uptake of the tracer was clearly visible in infected muscles and not visible in sterile inflammed muscles. Conclusion: The 99mTc-norfloxacin retains bactericidal properties of unlabelled norfloxacin. The tracer demonstrated small degree of S. aureus binding both with killed as well as alive bacteria. Studies which were performed in vivo in rats with a model of thigh muscle infection showed good ability of the radiopharmaceutical to image the infection.",
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AU - Sazonova, Svetlana Ivanovna

AU - Lishmanov, Yuriy Borisovich

AU - Varlamova, Natalia Valerievna

AU - Skuridin, Viktor Sergeevich

AU - Ilushenkova, Yulia Nikolayevna

AU - Karpova, Maria Rostislavovna

AU - Nesterov, Evgeny Alexandrovich

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