Macromolecular prodrugs: XI. Synthesis and characterization of polymer–estradiol conjugate

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Estradiol-3-benzoate (EB), an ester derivative of the main oestrogen hormone estradiol, was chemically modified and bound to poly(α,β-(N-2-hydroxyethyl-dl-aspartamide))–poly(α,β-(N-2-aminoethyl-dl-aspartamide)) copolymer (PAHA). EB was first converted to estradiol-3-benzoate-17-(benzotriazole-1-carboxylate), which readily reacted with amino groups in PAHA affording the polymer–drug conjugate PAHA–EB. In PAHA–EB estradiol moiety was covalently bound to the polymeric carrier by carbamate linkage, through non-toxic ethylenediamine spacer. The synthesized compound is a potential hydrosoluble estradiol prodrug.

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