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Pyrrolidone-modified PAMAM dendrimers enhance anti-inflammatory potential of indomethacin in vitro

Author:
Gorzkiewicz, Michał, Janaszewska, Anna, Ficker, Mario, Svenningsen, Søren W., Christensen, Jørn B., Klajnert-Maculewicz, Barbara
Source:
Colloids and surfaces 2019 v.181 pp. 959-962
ISSN:
0927-7765
Subject:
anti-inflammatory activity, cell membranes, dendrimers, genetic markers, in vitro culture, indomethacin, models, nonsteroidal anti-inflammatory agents, prostaglandin synthase, prostaglandins, secretion, solubility, therapeutics, transcription factor NF-kappa B
Abstract:
The therapeutic effect of indomethacin, a water-insoluble non-steroidal anti-inflammatory drug, requires its efficient transport through cellular membranes and accumulation inside the target cells. The application of dendritic polymers has been proposed for the improvement of the drug’s solubility and intracellular delivery. In this study we evaluated the anti-inflammatory potential of novel, highly-biocompatible 4-carbomethoxypyrrolidone-coated PAMAM dendrimers loaded with indomethacin. Our results indicate that complexation with dendrimers do not hamper the inhibitory action of indomethacin towards cyclooxygenases. Drug-dendrimer formulations exhibited improved anti-inflammatory activity in in vitro-cultured cellular models, showing enhanced inhibition of prostaglandin secretion and significantly decreased expression of NF-κB marker genes compared to free drug.
Agid:
6484269