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Radioiodinated anastrozole and epirubicin as potential targeting radiopharmaceuticals for solid tumor imaging

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Abstract

This study describes the preparation of radioiodinated anastrozole and epirubicin and their biological evaluation as potential solid tumor imaging gents. Radioiodinated anastrozole and epirubicin were successfully prepared via direct electrophilic substitution reaction at ambient temperature. The radiochemical yields for radioiodinated anastrozole and epirubicin were maximized to 92.9 ± 0.1 and 98.8 ± 0.1 %, respectively by studying different reaction parameters such as substrate amount, chloramine-T, pH of the reaction mixture, reaction temperature and reaction time. They showed in vitro stability up to 4 and 24 h, respectively. The preclinical evaluation and biodistribution in mice bearing solid tumor showed high retention and biological accumulation in solid tumor cells (12.4 and 25.3 % injected activity/g tissue) and high T/NT ratio equal to 4.7 ± 0.1 and 5.2 ± 0.1 at 2 and 1 h post-injection, respectively. Data described before could recommend radioiodinated anastrozole and radioiodinated epirubicin as potential targeting radiopharmaceuticals for solid tumor imaging.

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Authors and Affiliations

  1. Radioactive Isotopes and Generator Department, Hot Labs Center, Atomic Energy Authority, 13759, Cairo, Egypt

    T. M. Sakr

  2. Labeled Compounds Department, Hot Labs Center, Atomic Energy Authority, 13759, Cairo, Egypt

    A. B. Ibrahim, M. A. Motaleb & M. T. El-Kolaly

  3. Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, 11562, Cairo, Egypt

    O. M. A. Khoweysa & A. Abd El-Bary

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  1. A. B. Ibrahim
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  2. T. M. Sakr
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  3. O. M. A. Khoweysa
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  4. M. A. Motaleb
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  5. A. Abd El-Bary
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  6. M. T. El-Kolaly
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Correspondence to A. B. Ibrahim.

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Ibrahim, A.B., Sakr, T.M., Khoweysa, O.M.A. et al. Radioiodinated anastrozole and epirubicin as potential targeting radiopharmaceuticals for solid tumor imaging. J Radioanal Nucl Chem 303, 967–975 (2015). https://doi.org/10.1007/s10967-014-3560-9

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  • DOI: https://doi.org/10.1007/s10967-014-3560-9

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