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Labeling of Aspirin with 99mTc to Obtain a Possible Tumor Imaging Agent

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Radiochemistry Aims and scope

Abstract

About 35% reduction in cancer deaths among patients having solid tumors is related to using aspirin, which encouraged us to develop a new specific tumor diagnostic radiopharmaceutical agent. This can be done by direct labeling of aspirin with technetium-99m using stannous chloride as a reductant at pH 9. At this pH, aspirin is saponificated to salicylate ions. Salicylate binds to pertechenetate to form 99mTc salicylate complex. The radiochemical yield (RCY, %) of 99mTc-salicylate complex obtained from aspirin was determined using paper chromatography, electrophoresis, and HPLC and was found to reach 90.2%. The 99mTc salicylate complex obtained from aspirin was stable for up to 5 h. The tumor uptake of the 99mTc salicylate complex obtained from aspirin was determined by ex-vivo study in tumor-bearing mice. This study showed that 99mTc salicylate complex was concentrated in tumor sites (ascites or solid), allowing tumor radioimaging. High target/non-target (tumor muscles/normal muscles) uptake ratio shows that 99mTc salicylate complex can be utilized for early detection of solid tumors. Molecular modeling and docking study conofirm the possibility of using the radiolabeled 99mTc salicylate complex for specific cancer imaging in binding with epidermal growth factor receptors (EGFR).

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Funding

The study was financially supported by the Deanship of Scientific Research at Umm Al-Qura University, Makkah, Saudi Arabia (grant code: 19-MED-1-01-0038).

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Authors and Affiliations

  1. Department of Pharmaceutics, College of Pharmacy, Umm Al-Qura University, 21955, Makkah, Saudi Arabia

    M. Dawoud & K. M. Attallah

  2. Department of Pharmaceutics, College of Pharmacy, Helwan University, 11795, Cairo, Egypt

    M. Dawoud

  3. Labeled Compounds Department, Hot Laboratories Center, Atomic Energy Authority, 13759, Cairo, Egypt

    K. M. Attallah, S. M. Abdelhalim, F. A. Marzook, A. F. Mahmoud & I. T. Ibrahim

  4. Biological Applications Department, Nuclear Research Center, Atomic Energy Authority, 13759, Cairo, Egypt

    M. R. Abdelgawad

  5. College of Pharmacy, Al-Bayan University, 2268, Baghdad, Iraq

    I. T. Ibrahim

Authors
  1. M. Dawoud
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  2. K. M. Attallah
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  3. S. M. Abdelhalim
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  4. F. A. Marzook
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  5. M. R. Abdelgawad
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  6. A. F. Mahmoud
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  7. I. T. Ibrahim
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Correspondence to K. M. Attallah or I. T. Ibrahim.

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Dawoud, M., Attallah, K.M., Abdelhalim, S.M. et al. Labeling of Aspirin with 99mTc to Obtain a Possible Tumor Imaging Agent. Radiochemistry 63, 820–827 (2021). https://doi.org/10.1134/S106636222106014X

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  • DOI: https://doi.org/10.1134/S106636222106014X

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