Journal of Radioanalytical and Nuclear Chemistry

, Volume 314, Issue 2, pp 1023–1029 | Cite as

Radiosynthesis and preclinical studies of 177Lu-labeled sulfadiazine: a possible theranostic agent for deep-seated bacterial infection

  • Syed Ali Raza Naqvi
  • Rashid Rasheed
  • Muhammad Tauqeer Ahmed
  • Ameer Fawad Zahoor
  • Muhammad Khalid
  • Sajid Mahmood


Sulfadiazine acts through inhibition of bacterial dihydropteroate synthetase. The radio-labeling of sulfadiazine with lutetium-177 (177Lu) is expected to serve as a theranostic agent for deep-seated bacterial infections. The radiosynthesis of 177Lu-sulfadiazine indicated a > 95% yield under optimized reaction conditions, and promising stability was found in blood serum. Biodistribution data in the absence of infection revealed minimal accumulation in key body organs. Kidneys were the main excretory organs, showed an uptake of 1.76 ± 0.09% ID/g organ at 6-h post-injection. Biodistribution, scintigraphic data, glomerular filtration rate, and cytotoxicity results encourage clinical investigation of 177Lu-sulfadiazine as a novel theranostic agent for deep-seated bacterial infection.


Sulfadiazine Lutetium-177 177Lu-sulfadiazine Nuclear medicine Deep-seated infections 



The study is a part of HEC funded project No.5612/Punjab/NRPU/R&D/HEC/2016, thanks to HEC, GCU Faisalabad, PINSTECH Islamabad and INOR Abbottabad for providing resources, platform, and technical assistance to conduct this research. We are also thankful to Mr. Javid Gil (PINSTECH) for providing technical assistance in handling 177LuCl3. The authors are also grateful to Prof. Drlica Karl (USA) for editing and proof reading of the manuscript.

Compliance with ethical standards

Conflict of interest

There is no conflict of interest exist among all the authors.

Supplementary material

10967_2017_5477_MOESM1_ESM.tif (468 kb)
Supplementary material 1 (TIFF 467 kb)


  1. 1.
    Vranakis I, Goniotakis I, Psaroulaki A, Sandalakis V, Tselentis Y, Gevaert K, Tsiotis G (2014) J Proteom 97:88–99CrossRefGoogle Scholar
  2. 2.
    Kircher M, Lapa C (2017) Curr Cardiovasc Imaging Rep 10:6. doi: 10.1007/s12410-017-9400-x CrossRefGoogle Scholar
  3. 3.
    Gandomkar M, Najafi R, Babaei MH, Shafiei M, Sadat Ebrahimi SE (2006) DARU J Pharm Sci 14:183–187Google Scholar
  4. 4.
    Vinjamuri S, Solanki KK, Bomanji J, Siraj Q, Britton KE, Hall AV, O’Shaughnessy E, Das SS (1996) Lancet 347:233–235CrossRefGoogle Scholar
  5. 5.
    Wareham D, Michael J, Das S (2005) Braz Arch Biol Technol 48:145–152CrossRefGoogle Scholar
  6. 6.
    Liu S, Edwards DS, Barrett JA (1997) Bioconjugate Chem 8:621–636CrossRefGoogle Scholar
  7. 7.
    Akhtar MS, Iqbal J, Khan MA, Irfanullah J, Jehangir M, Khan B, ul-Haq I, Muhammad G, Nadeem MA, Afzal MS, Imran MB (2004) J Nucl Med 45:849–856Google Scholar
  8. 8.
    Bolzati C, Refosco F, Marchiani A, Ruzza P (2010) Curr Med Chem 17:2656–2683CrossRefGoogle Scholar
  9. 9.
    Ramogida CF, Orvig C (2013) Chem Commun 49:4720–4739CrossRefGoogle Scholar
  10. 10.
    Pillai MRA, Chakraborty S, Das T, Venkatesh M, Ramamoorthy N (2003) Appl Radiat Isot 59:109–118CrossRefGoogle Scholar
  11. 11.
    Cutler CS, Hennkens HM, Sisay N, Huclier-Markai S, Jurisson SS (2013) Chem Rev 113:858–883CrossRefGoogle Scholar
  12. 12.
    Hakimi A, Jalilian AR, Shirvani-Arani S, Abbasian P, Khoshmaram V, Ghannadi-Maragheh M (2015) J Radioanal Nucl Chem 303:1–10CrossRefGoogle Scholar
  13. 13.
    Naseri Z, Hakimi A, Jalilian AR, Nemati Kharat A, Shirvani-Arani S, Bahrami-Samani A, Ghannadi-Maragheh M (2012) Radiochim Acta 100:267–272CrossRefGoogle Scholar
  14. 14.
    Vaidyanathan G, Zalutsky MR (1996) Phys Med Biol 41:1915–1931CrossRefGoogle Scholar
  15. 15.
    Kaltsas GA, Papadogias D, Makras P, Grossman AB (2005) Endocr Relat Cancer 12:683–699CrossRefGoogle Scholar
  16. 16.
    Bergsma H, Konijnenberg MW, van der Zwan WA, Kam BLR, Teunissen JJM, Kooij PP, Mauff KAL, Krenning EP, Kwekkeboom DJ (2016) Eur J Nucl Med Mol Imaging 43:1802–1811CrossRefGoogle Scholar
  17. 17.
    Chakraborty S, Das T, Sarma HD, Venkatesh M, Banerjee S (2008) Nucl Med Biol 35:589–597CrossRefGoogle Scholar
  18. 18.
    Ahmed MT, Naqvi SAR, Rasheed R, Zahoor AF, Usman M, Hussain Z (2017) Appl Biochem Biotechnol. doi: 10.1007/s12010-017-2451-2 Google Scholar
  19. 19.
    Levey AS, Greene T, Schluchter MD, Cleary PA, Teschan PE, Lorenz RA, Molitch ME, Mitch WE, Siebert C, Hall PM, Steffes MW (1993) J Am Soc Nephrol 4:1159–1171Google Scholar
  20. 20.
    Rasheed R, Tariq S, Naqvi SAR, Gillani SJ, Rizvi FA, Sajid M, Rasheed S (2016) J Label Compd Radiopharm 59:398–403CrossRefGoogle Scholar
  21. 21.
    Erion JL, Bugaj JE, Schmidt MA et al (1999) J Nucl Med 40:223Google Scholar
  22. 22.
    Hens M, Vaidyanathan G, Zhao X-G, Bigner DD, Zalutsky MR (2010) Nucl Med Biol 37:741–750CrossRefGoogle Scholar
  23. 23.
    Motaleb MA, El-Kolaly MT, Ibrahim AB, El-Bary A (2011) J Radioanal Nucl Chem 289:57–65CrossRefGoogle Scholar
  24. 24.
    Vallabhajosula S, Killeen RP, Osborne JR (2010) Semin Nucl Med 40:220–241CrossRefGoogle Scholar
  25. 25.
    Werner J, Dragotakes SC, Fernandez-del Castillo C, Rivera JA, Ou J, Rattner DW, Fischman AJ, Warshaw AL (1998) Ann Surg 227:86–94CrossRefGoogle Scholar
  26. 26.
    Ilem-Ozdemir D, Caglayan-Orumlu O, Asikoglu M, Ozkilic H, Yilmaz F, Hosgor-Limoncu M (2016) J Radioanal Nucl Chem 308:995–1004CrossRefGoogle Scholar

Copyright information

© Akadémiai Kiadó, Budapest, Hungary 2017

Authors and Affiliations

  1. 1.Department of ChemistryGovernment College UniversityFaisalabadPakistan
  2. 2.Pakistan Institute of Nuclear Sciences and Technology (PINSTECH)IslamabadPakistan

Personalised recommendations