Technetium-99m-Labeled Sulfadiazine: a Targeting Radiopharmaceutical for Scintigraphic Imaging of Infectious Foci Due To Escherichia coli in Mouse and Rabbit Models

Appl Biochem Biotechnol. 2017 Sep;183(1):374-384. doi: 10.1007/s12010-017-2451-2. Epub 2017 Mar 11.

Abstract

Bacterial infection is one of the vital reasons of morbidity and mortality, especially in developing countries. It appears silently without bothering the geological borders and imposes a grave threat to humanity. Nuclear medicine technique has an important role in helping early diagnosis of deep-seated infections. The aim of this study was to develop a new radiopharmaceutical 99mTc-labeling sulfadiazine as an infection imaging agent. Radiolabeling of sulfadiazine with technetium-99m (99mTc) was carried out using stannous tartrate as a reducing agent in the presence of gentistic acid at pH = 5. The quality control tests revealed ~98% labeling efficiency. Paper chromatographic (PC) and instant thin-layer chromatographic (ITLC) techniques were used to analyze radiochemical yield. Biodistribution and infection specificity of the radiotracer were performed with Escherichia coli (E. coli) infection-induced rats. Scintigraphy and glomerular filtration rate (GFR) study was performed in E. coli-infected rabbits. Scintigraphy indicated E. coli infection targeting potential of 99mTc-SDZ, while biodistribution study showed minimal uptake of 99mTc-SDZ in non-targeted tissues. The uptake in the kidneys was found 2.56 ± 0.06, 2.09 ± 0.10, and 1.68 ± 0.09% at 30 min, 1 h, and 4 h, respectively. The infected muscle (target) to non-infected muscle (non-target) ratio (T/NT) was found 4.49 ± 0.04, 6.78 ± 0.07, and 5.59 ± 0.08 at 30 min, 1 h, and 4 h, respectively.

Keywords: E. coli infection; Infection imaging; Radiolabeled compounds; Scintigraphy; Sulfadiazine; Technetium-99m.

MeSH terms

  • Animals
  • Escherichia coli Infections / diagnostic imaging*
  • Escherichia coli Infections / drug therapy
  • Escherichia coli*
  • Isotope Labeling / methods*
  • Mice
  • Rabbits
  • Radionuclide Imaging
  • Rats
  • Rats, Sprague-Dawley
  • Sulfadiazine* / chemistry
  • Sulfadiazine* / pharmacokinetics
  • Sulfadiazine* / pharmacology
  • Technetium* / chemistry
  • Technetium* / pharmacokinetics
  • Technetium* / pharmacology

Substances

  • Sulfadiazine
  • Technetium