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

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Date

2015

Journal Title

Journal ISSN

Volume Title

Type

Article

Publisher

SPRINGER

Series Info

Journal of Radioanalytical and Nuclear Chemistry;VOL : 303 Issue : 1

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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Keywords

Anastrozole, Epirubicin, Radioiodination, Solid tumor, Targeting

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