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Title

Bioadhesive pellets increase local 5-aminosalicylic acid concentration in experimental colitis
Authors
Bautzova, Tereza
Rabišková, Miloslava
Béduneau, Arnaud
Pellequer, Yann
Lamprecht, Alf
Published in European Journal of Pharmaceutics and Biopharmaceutics. 2012, vol. 81, no. 2, p. 379-85
Abstract Topical delivery of 5-aminosalicylic acid (5-ASA) to the colonic mucosa is important in order to achieve effective drug concentration in the site of inflammation and to minimize its systemic availability. 5-ASA loaded pellets were prepared by an extrusion/spheronization method. Mucoadhesive biopolymer chitosan was incorporated into the pellets, and drug delivery to the colon was controlled by the pH-sensitive polymer Eudragit® FS. Dissolution profiles of coated pellets revealed no drug release at pH 1.2 within 2h and release as intended in the simulated distal ileum and colon. In vivo, chitosan-core drug loaded pellets (AMCh) showed 2.5-fold higher drug metabolite concentration than after chitosan free pellets (AM) administration in the inflamed colonic tissue. Additionally, AMCh demonstrated decreased in AUC in colitis group (1507 ± 400 ng h/ml) compared with AM (1907 ± 122 ng h/ml). In terms of therapeutic efficiency, administration of pellets markedly decreased the colon/body weight ratio (colitis: 0.0355 ± 0.0028; AM 0.0092 ± 0.0033; AMCh 0.0086 ± 0.0022) and myeloperoxidase activity (colitis: 3212 ± 294 U/g tissue; AM 796 ± 211 U/g; AMCh 552 ± 319 U/g). Bioadhesive chitosan pellets showed additional beneficial properties for colonic 5-ASA delivery in the treatment of inflammatory bowel disease by increasing the drug concentration locally.
Keywords Animals — Anti-Inflammatory Agents/administration & dosage/chemistry — Biopolymers/administration & dosage/chemistry/pharmacokinetics — Chitosan/administration & dosage/chemistry/pharmacokinetics — Colitis/drug therapy/metabolism — Colon/drug effects/metabolism — Drug Delivery Systems/methods — Drug Implants/administration & dosage/chemistry/pharmacokinetics — Hydrogen-Ion Concentration — Inflammation/drug therapy/metabolism — Male — Mesalamine/administration & dosage/chemistry/pharmacokinetics — Particle Size — Peroxidase/metabolism — Rats — Rats, Wistar — Solubility
Identifiers
PMID: 22386911
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(ISO format) 		BAUTZOVA, Tereza et al. Bioadhesive pellets increase local 5-aminosalicylic acid concentration in experimental colitis. In: European Journal of Pharmaceutics and Biopharmaceutics, 2012, vol. 81, n° 2, p. 379-85. doi: 10.1016/j.ejpb.2012.02.011 https://archive-ouverte.unige.ch/unige:94520

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Deposited on : 2017-05-30

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