Gastrointestinal transition and anti-diabetic effect of Isabgol husk microparticles containing gliclazide

•Isabgol husk with sodium alginate was crosslinked with calcium ions for microparticles development.•More release of encapsulated gliclazide was observed in SIF than SGF and distilled water.•Gliclazide was found compatible with polymeric backbone of microparticles.•Anti-diabetic effect of preparatio...

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Veröffentlicht in:International journal of biological macromolecules 2014-05, Vol.66, p.15-25
Hauptverfasser: Sharma, Vipin Kumar, Mazumder, Bhaskar
Format: Artikel
Sprache:eng
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Zusammenfassung:•Isabgol husk with sodium alginate was crosslinked with calcium ions for microparticles development.•More release of encapsulated gliclazide was observed in SIF than SGF and distilled water.•Gliclazide was found compatible with polymeric backbone of microparticles.•Anti-diabetic effect of preparation was more than conventional immediate release tablet.•The prolonged retention time of microparticles was observed by X-ray imaging analysis. Isabgol husk with sodium alginate was formulated into gliclazide loaded microparticles which were characterized for particle size, swelling index, entrapment efficiency, in vitro release, release kinetics, stability, hypoglycemic effect, surface morphology, and gastrointestinal transition. The particle size in different formulations varied from 752.83±0.630 to 872.03±0.293μm. It was analyzed by dissolution study that up to 98% of loaded gliclazide was released in simulated intestinal fluid (SIF, pH 7.4) within 8h. The formulations containing sodium alginate and Isabgol husk–sodium alginate showed bioequivalency with marketed sustained release tablets (Glizid MR 60®) in terms of release pattern. The drug maintained its integrity in terms of functional groups after fabrication in formulations as observed by FTIR analysis. The hypoglycemic effect of gliclazide loaded Isabgol husk–sodium alginate microparticles was found to be 37±6.356% in terms of changes of blood glucose level from base glucose level (100%) in diabetic condition after 24h of oral administration and it was more than marketed conventional tablets (95.5±3.286%). The retention of microparticles was observed in small intestine up to 10h during whole body X-ray imaging. The study revealed that microparticles composing of Isabgol husk may have the potential for regulating blood glucose level in diabetic animals with controlled release of gliclazide.
ISSN:0141-8130
1879-0003
DOI:10.1016/j.ijbiomac.2014.02.014