Radiosynthesis and Biodistribution of 99mTc-Metronidazole as an Escherichia coli Infection Imaging Radiopharmaceutical

Appl Biochem Biotechnol. 2018 May;185(1):127-139. doi: 10.1007/s12010-017-2641-y. Epub 2017 Nov 2.

Abstract

Bacterial infection poses life-threatening challenge to humanity and stimulates to the researchers for developing better diagnostic and therapeutic agents complying with existing theranostic techniques. Nuclear medicine technique helps to visualize hard-to-diagnose deep-seated bacterial infections using radionuclide-labeled tracer agents. Metronidazole is an antiprotozoal antibiotic that serves as a preeminent anaerobic chemotherapeutic agent. The aim of this study was to develop technetium-99m-labeled metronidazole radiotracer for the detection of deep-seated bacterial infections. Radiosynthesis of 99mTc-metronidazole was carried by reacting reduced technetium-99m and metronidazole at neutral pH for 30 min. The stannous chloride dihydrate was used as the reducing agent. At optimum radiolabeling conditions, ~ 94% radiochemical was obtained. Quality control analysis was carried out with a chromatographic paper and instant thin-layer chromatographic analysis. The biodistribution study of radiochemical was performed using Escherichia coli bacterial infection-induced rat model. The scintigraphic study was performed using E. coli bacterial infection-induced rabbit model. The results showed promising accumulation at the site of infection and its rapid clearance from the body. The tracer showed target-to-non-target ratio 5.57 ± 0.04 at 1 h post-injection. The results showed that 99mTc-MNZ has promising potential to accumulate at E. coli bacterial infection that can be used for E. coli infection imaging.

Keywords: E. coli infection; Metronidazole; Nuclear medicine technique; Radiolabeled compounds; Scintigraphy.

MeSH terms

  • Animals
  • Disease Models, Animal
  • Escherichia coli / metabolism*
  • Escherichia coli Infections* / diagnostic imaging
  • Escherichia coli Infections* / drug therapy
  • Escherichia coli Infections* / metabolism
  • Metronidazole / chemistry*
  • Rabbits
  • Radiopharmaceuticals* / chemical synthesis
  • Radiopharmaceuticals* / chemistry
  • Radiopharmaceuticals* / pharmacokinetics
  • Radiopharmaceuticals* / pharmacology
  • Rats
  • Rats, Sprague-Dawley
  • Technetium / chemistry*

Substances

  • Radiopharmaceuticals
  • Metronidazole
  • Technetium