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

Kód výsledku v IS VaVaI

RIV/62157124:16370/12:43871259 - isvavai.cz

Výsledek na webu

http://dx.doi.org/10.1016/j.ejpb.2012.02.011

DOI - Digital Object Identifier

10.1016/j.ejpb.2012.02.011

Jazyk výsledku

angličtina

Název v původním jazyce

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

Popis výsledku v původním jazyce

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 (R) FS. Dissolution profiles of coated pellets revealed no drug release at pH1.2 within 2 h 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/bod

Název v anglickém jazyce

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

Popis výsledku anglicky

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 (R) FS. Dissolution profiles of coated pellets revealed no drug release at pH1.2 within 2 h 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/bod

Druh

J_x - Nezařazeno - Článek v odborném periodiku (Jimp, Jsc a Jost)

CEP obor

FR - Farmakologie a lékárnická chemie

OECD FORD obor

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Projekt

NS10222: Mikročásticová léková forma pro terapii nespecifických střevních zánětlivých onemocnění

Návaznosti

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Rok uplatnění

2012

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

European Journal of Pharmaceutics and Biopharmaceutics

ISSN

0939-6411

e-ISSN

—

Svazek periodika

81

Číslo periodika v rámci svazku

2

Stát vydavatele periodika

NL - Nizozemsko

Počet stran výsledku

7

Strana od-do

379-385

Kód UT WoS článku

000305591700018

EID výsledku v databázi Scopus

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