Indomethacin macromolecular prodrugs: Synthesis, characterization and in vitro evaluation | Abstract

Der Pharma Chemica
Journal for Medicinal Chemistry, Pharmaceutical Chemistry, Pharmaceutical Sciences and Computational Chemistry

ISSN: 0975-413X
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Indomethacin macromolecular prodrugs: Synthesis, characterization and in vitro evaluation

Author(s): Samaneh Abyari Miyandoab and Mirzaagha Babazadeh

The present research work describes the synthesis and in vitro evaluation of novel acrylic-type polymeric systems having degradable ester bonds linked to indomethacin as materials for drug delivery systems. First, indomethacin was linked to 2-hydroxyethyl methacrylate by an activated ester methodology in a one-pot procedure with a high yield. The resulted polymerizable monomer was then copolymerized with 2-hydroxyethyl methacrylate or methyl methacrylate (in 1:3 mole ratios) by the free radical polymerization method, utilizing benzoyl peroxide at 70±2°C. The characterization of the obtained polymer-drug conjugates by FT-IR, 1H-NMR, elemental analysis, and gel permeation chromatography techniques confirmed their structure successfully. Indomethacin release from the obtained polymers was preliminarily evaluated at different buffered solutions (pH 1, 7.4, and 10) into dialysis bags to show the capacity of prodrugs to release the indomethacin under hydrolytic conditions. Detection of hydrolysis by UV spectroscopy at the wavelength of maximum absorption of the free indomethacin in selected intervals showed that the drug can be released by selective hydrolysis of the ester bond at the side of the drug moiety. The release profiles indicated that the degree of hydrolysis increase as the polymeric prodrug passes from acidic to alkali medium. In alkali pH, the polymeric prodrugs reach degree of swelling that makes the liable bonds accessible to hydrolysis.


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