6533b83afe1ef96bd12a708e

RESEARCH PRODUCT

N-Succinyl-chitosan systems for 5-aminosalicylic acid colon delivery: In vivo study with TNBS-induced colitis model in rats

Maria ManconiMatilde Merino-sanjuánMatilde Merino-sanjuánC. CardaAna Lúcia Tasca Gois RuizAnna Maria FaddaAmparo NácherAmparo NácherVirginia MerinoVirginia MerinoGiuseppe LoyCarla MuraOctavio Díez-salesOctavio Díez-sales

subject

Malemedicine.medical_specialtyAminosalicylic acidColonPolymersPharmaceutical ScienceLymphocyte ActivationInflammatory bowel diseaseGastroenterologyAbsorptionChitosanchemistry.chemical_compoundDrug Delivery SystemsIn vivoInternal medicinemedicineAnimalsIntestinal MucosaRats WistarMicroparticleColitisMesalaminePeroxidaseChitosanDrug CarriersChemistryAnti-Inflammatory Agents Non-SteroidalOrgan SizeColitismedicine.diseasedigestive system diseasesIn vitroRatsDisease Models AnimalFreeze DryingTrinitrobenzenesulfonic AcidSwellingmedicine.symptom

description

5-Aminosalicylic acid (5-ASA) loaded N-Succinyl-chitosan (SucCH) microparticle and freeze-dried system were prepared as potential delivery systems to the colon. Physicochemical characterization and in vitro release and swelling studies were previously assessed and showed that the two formulations appeared to be good candidates to deliver the drug to the colon. In this work the effectiveness of these two systems in the treatment of inflammatory bowel disease was evaluated. In vitro mucoadhesive studies showed excellent mucoadhesive properties of both the systems to the inflamed colonic mucosa. Experimental colitis was induced by rectal instillation of 2,4,6-trinitrobenzene sulfonic acid (TNBS) into male Wistar rats. Colon/body weight ratio, clinical activity score system, myeloperoxidase activity and histological evaluation were determined as inflammatory indices. The two formulations were compared with drug suspension and SucCH suspension. The results showed that the loading of 5-ASA into SucCH polymer markedly improved efficacy in the healing of induced colitis in rats.

yearjournalcountryeditionlanguage
2011-03-23International Journal of Pharmaceutics
https://doi.org/10.1016/j.ijpharm.2011.06.025