Radiolabeling of Ceftriaxone with 99mTc as a Targeting Radiopharmaceutical for Staphylococcus Aureus Detection in Mouse Model

Document Type : Original Paper

Authors

1 Department of Microbiology, Faculty of Sciences, Zanjan Branch, Islamic Azad University, Zanjan, Iran

2 Biology Research Center, Zanjan Branch, Islamic Azad University, Zanjan, Iran

3 Department of Nuclear Medicine, Faculty of Medicine, Zanjan University of Medical Sciences, Zanjan, Iran

4 Department of Radioisotope, Nuclear Researches Center, Atomic Energy Organization of Iran, Tehran, Iran

5 Faculty of Veterinary Sciences, Sciences and Researches Branch, Islamic Azad University, Tehran, Iran

Abstract

Introduction
Bacterial infection is one of the major causes of morbidity and mortality especially in developing countries. Nuclear medicine has an important role in helping the diagnosis of deep-seated infections by developing more specific radiopharmaceuticals. The aim of this study was to evaluate 99mTc-labeling ceftriaxone as a new radiopharmaceutical for Staphylococcus aureus infection imaging in nuclear medicine.
Materials and Methods
Radiolabeling of ceftriaxone was carried out by adding 370 MBq of 99mTc to 10 mg of ceftriaxone in the presence of 50 µg of SnCl2.2H2O at pH=5. The radiochemical purity and stability tests at room temperature and human blood serum were evaluated with ITLC. Intramuscular infection was induced by injection of Staphylococcus aureus into the left thigh muscle of the mice. The biodistribution of 99mTc-ceftriaxone was studied in normal and infected mice at various times post-injection.
Results
Radiochemical purity of the product was 94.5±5.4% with a good stability at room temperature and human serum, 80.6% and 71.2% after 24 h, respectively. The biodistribution studies showed the localization of 99mTc-ceftriaxone at the site of infection with high sensitivity without any significant accumulation in vital organs.
Conclusion
Due to the ease of 99mTc-ceftriaxone conjugation method, high labeling efficiency, and high uptake in the infected muscle, it may provide a promising candidate as a targeting radiopharmaceutical for imaging infectious foci due to Staphylococcus aureus in nuclear medicine.

Keywords

Main Subjects

References

  1. Love C, Palestro CJ. Radionuclide imaging of infection. J Nucl Med Technol. 2004;32(2):47-57.
  2. Yurt Lambresht F, Yilmaz O, Unak P, Seyitoglo B, Durkan K, Baskan H. Evaloation of 99mTc- cefuroxime axetil for imaging of inflammation. J radioanalytical Nucl Chem. 2008;277(2):491-4.
  3. El-Ghany EA, El-Kolaly T, Amine AM, El-Sayed AS, Abdel-Gelil F. Synthesis of 99mTc–pefloxacin: a new targeting agent for infectious foci. J radioanalytical Nucl Chemistry. 2005;266(1):131-9.
  4. Gemmel F, Dumarey N, Welling M. Future diagnostic agents. Semin Nucl Med. 2009;39(1):11-26.
  5. Agency IAE. Development of Kits for 99mtc Radiopharmaceuticals for Infection Imaging: International Atomic Energy Agency; 2004.
  6. Oyen WJ, Corstens FH, Boerman OC. Discriminating infection from steril inflammation. Can radiolabelled antibiotics solve the problem? Eur J Nucl Med Mol Imaging. 2005;32(2):151-2.
  7. Singh B, Mittal BR, Bhattagharya A, Aggarwal A, Nagi ON, Singh AK. Technetium-99m ciprofloxacin imaging in the diagnosis of postsurgical bony infection and evaluation of the response to antibiotic theraoy: A case report. J Orthop Surg (Hong Kong). 2005;13(2):190-4.
  8. Benitez A, Roca M, Martin-comin J. Labeling of antibiotics for infection diagnosis. Q J Nucl Med Mol Imaging. 2006;50(2):147-52.
  9. Vinjamuri S, Hall AV, Solanki KK,  Bomanji J, Siraj Q, O'Shaughnessy E, Das SS, Britton KE. Comparison of 99mTc Infecton imaging with radiolabelled white-cell imaging in the evaluation of bacterial infection. Lancet;1996;347(8996):233-5.
  10. Hall AV, Solanki KK, Vinjamuri S, Britton KE, Das SS. Evaluation of the efficacy of 99mTc-Infecton, a novel agent for detecting sites of infection. J Clin Pathol. 1998;51(3):215-9.
  11. Britton KE, Vinjamuri S, Hall AV, Solanki K, Siraj QH, Bomanji J, Das SS. Clinical evaluation of technetium-99m infecton for the localization of bacterial infection. Eur J Nucl Med. 1997;24(5):553-6.
  12. Lambrecht FY. Evaloation of 99mTc-labeled antibiotics for infection detection. Ann Nucl Med. 2011;25(1):1-6.
  13. Mirshojaei SF, Erfani M, Sadat Ebrahimi SE, Talebi MH. Freeze- Dried cold kit for preparation of 99mTc- ciprofloxacin as an infection imaging agent. Iran J Nucl Med. 2010;18(2):46-51.
  14. Brunton L, Blumenthal D, Buxton I, Parker K. Goodman and Gilman's Manual of Pharmacology and Therapeutics: McGraw-Hill; 2007.
  15. Scheld WM. The potential uses of ceftriaxone. Eur J Clin Microbiol. 1983;2(5):485-8.
  16. Mostafa M, Motaleb MA, Sakr TM. Labelling of ceftriaxone for infective inflammation imaging using 99mTc eluted from 99Mo/99mTc generator based on zirconium molybdate. Appl Radiat Isot. 2010;68(10):1959-63.
  17. Bartlett AH, Hulten KG. Staphylococcus aureus pathogenesis: secretion systems, adhesins, and invasins. Pediatr Infect Dis J. 2010;29(9):860-1.
  18. Chattopadhyay S, Saha Das S, Chandra S, De K, Mishra M, Ranjan Sarkar B, et al. Synthesis and evaluation of 99mTc-moxifloxacin, a potential specific imaging agent. Appl Radiat Isot. 2010;68(2):314-6.
  19. Siaens RH, Rennen HJ, Boerman OC, Dierckx R, Slegers G. Synthesis and comparison of 99mTc-enrofloxacin and 99mTc-ciprofloxacin. J Nucl Med. 2004;45(12):2088-94.

 

Iranian Journal of Medical Physics
Volume 9, Issue 2 - Serial Number 2
May and June 2012
Pages 103-110

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History

  • Receive Date: 05 February 2012
  • Revise Date: 03 March 2013
  • Accept Date: 16 April 2012

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