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Eur J Med Chem. 2011 Oct;46(10):4980-91. doi: 10.1016/j.ejmech.2011.08.004. Epub 2011 Aug 23.

Polymeric systems containing dual biologically active ions.

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  • 1Institute of Polymer Science and Technology, CSIC, C/Juan de la Cierva 3, 28006 Madrid, Spain.


This paper reports the synthesis and characterization of dual functional polymerizable salts containing quaternary ammonium cations ionically linked to non steroidal anti-inflammatory drugs (NSAIDs), and their polymers and copolymeric systems obtained with acrylic monomers of different hydrophilicity, e.g. methyl methacrylate and 2-hydroxyethyl methacrylate. NSAIDs used were meclofenamic acid, ketoprofen and ibuprofen. Sustained release of the NSAID from polymeric and copolymeric samples was observed over a period of 10 days and the hydrophobic/hydrophilic character of both the polymeric system and the drug played a role in the release behaviour. The antimicrobial activity of dual functional monomeric and polymeric derivatives was confirmed against Gram-positive and Gram-negative bacteria and polymeric compounds presented higher bactericidal action than the precursory monomers. The extracts of copolymeric samples had anti-inflammatory activity in a nitric oxide inhibitory assay on RAW 264.7 cells and they produced a NO inhibition around 80% within the first seven days.

Copyright © 2011 Elsevier Masson SAS. All rights reserved.

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