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Bioadhesive pellets increase local 5-aminosalicylic acid concentration in experimental colitis

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 AnimalsAnti-Inflammatory Agents/administration & dosage/chemistryBiopolymers/administration & dosage/chemistry/pharmacokineticsChitosan/administration & dosage/chemistry/pharmacokineticsColitis/drug therapy/metabolismColon/drug effects/metabolismDrug Delivery Systems/methodsDrug Implants/administration & dosage/chemistry/pharmacokineticsHydrogen-Ion ConcentrationInflammation/drug therapy/metabolismMaleMesalamine/administration & dosage/chemistry/pharmacokineticsParticle SizePeroxidase/metabolismRatsRats, WistarSolubility
PMID: 22386911
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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

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Deposited on : 2017-05-30

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