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Eur J Pharm Biopharm. 2021 Oct;167:89-103. doi: 10.1016/j.ejpb.2021.07.014. Epub 2021 Jul 28.

Mesalazine and inflammatory bowel disease - From well-established therapies to progress beyond the state of the art.

European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V

Pedro M Veloso, Raul Machado, Clarisse Nobre

Affiliations

  1. Centre of Biological Engineering, University of Minho, Campus de Gualtar, 4710-057 Braga, Portugal; CBMA - Centre of Molecular and Environmental Biology, Department of Biology, University of Minho, Campus de Gualtar, 4710-057 Braga, Portugal.
  2. CBMA - Centre of Molecular and Environmental Biology, Department of Biology, University of Minho, Campus de Gualtar, 4710-057 Braga, Portugal; IB-S - Institute of Science and Innovation for Sustainability, University of Minho, Campus de Gualtar, 4710-057 Braga, Portugal. Electronic address: [email protected].
  3. Centre of Biological Engineering, University of Minho, Campus de Gualtar, 4710-057 Braga, Portugal. Electronic address: [email protected].

PMID: 34329709 DOI: 10.1016/j.ejpb.2021.07.014

Abstract

Inflammatory bowel disease incidence has been constantly rising for the past few decades. Current therapies attempt to mitigate its symptoms since no cure is established. The most commonly prescribed drug for these patients is 5-aminosalicylic acid (5-ASA). Due to the low rate and seriousness of side effects compared to other therapies, 5-ASA is still largely prescribed in many stages of inflammatory bowel disease, including scenarios where evidence suggests low effectiveness. Although commercialized formulations have come a long way in improving pharmacokinetics, it is still necessary to design and develop novel delivery systems capable of increasing effectiveness at different stages of the disease. In particular, micro- and nano-sized particles might be the key to its success in Crohn's disease and in more serious disease stages. This review provides an overview on the clinical significance of 5-ASA formulations, its limitations, challenges, and the most recent micro- and nanoparticle delivery systems being designed for its controlled release. Emergent alternatives for 5-ASA are also discussed, as well as the future prospects for its application in inflammatory bowel disease therapies.

Copyright © 2021 Elsevier B.V. All rights reserved.

Keywords: 5-aminosalicylic acid; Crohn’s disease; Drug delivery; Inflammatory bowel disease; Mesalazine; Ulcerative colitis

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