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

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Abstract

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.

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Acknowledgements

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.

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Authors and Affiliations

  1. Department of Chemistry, Government College University, Faisalabad, 38000, Pakistan

    Syed Ali Raza Naqvi, Rashid Rasheed, Muhammad Tauqeer Ahmed & Ameer Fawad Zahoor

  2. Pakistan Institute of Nuclear Sciences and Technology (PINSTECH), Nilore, Islamabad, Pakistan

    Muhammad Khalid & Sajid Mahmood

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  1. Syed Ali Raza Naqvi
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  2. Rashid Rasheed
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  3. Muhammad Tauqeer Ahmed
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  4. Ameer Fawad Zahoor
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Correspondence to Syed Ali Raza Naqvi.

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Naqvi, S.A.R., Rasheed, R., Ahmed, M.T. et al. Radiosynthesis and preclinical studies of 177Lu-labeled sulfadiazine: a possible theranostic agent for deep-seated bacterial infection. J Radioanal Nucl Chem 314, 1023–1029 (2017). https://doi.org/10.1007/s10967-017-5477-6

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  • DOI: https://doi.org/10.1007/s10967-017-5477-6

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