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Artif Cells Nanomed Biotechnol ; 43(5): 328-33, 2015.
Artículo en Inglés | MEDLINE | ID: mdl-24579883

RESUMEN

Metoprolol succinate is a very potent drug for the treatment of hypertension but suffers from poor bioavailability due to its erratic absorption in lower GI tract. Therefore, in the present study, it was hypothesized that by formulating mucoadhesive particles, the residence time in the GIT and release of drug may be prolonged that will enhance the bioavailability of metoprolol succinate. Metoprolol succinate loaded chitosan microparticles were prepared by ionic gelation method. The optimized microparticles were coated with sodium alginate to form a layer over chitosan microparticles to increase the mucoadhesive strength and to release the drug in controlled manner. Coated and uncoated microparticles were evaluated for particle size, zeta potential, morphology, entrapment efficiency, drug loading and in vitro drug release. The coated microparticles showed comparatively less drug release in the 0.1 N HCl while sustained release in PBS (pH 6.8) as compared to uncoated microparticles. The in vivo study on albino rats demonstrated an increase in bioavailability of the coated microparticles as compared to marketed formulation. From the study it can be concluded that alginate coated chitosan microparticles could be a useful carrier for the oral delivery of metoprolol succinate.


Asunto(s)
Alginatos , Portadores de Fármacos , Metoprolol , Alginatos/química , Alginatos/farmacocinética , Alginatos/farmacología , Animales , Portadores de Fármacos/química , Portadores de Fármacos/farmacocinética , Portadores de Fármacos/farmacología , Evaluación Preclínica de Medicamentos , Ácido Glucurónico/química , Ácido Glucurónico/farmacocinética , Ácido Glucurónico/farmacología , Ácidos Hexurónicos/química , Ácidos Hexurónicos/farmacocinética , Ácidos Hexurónicos/farmacología , Masculino , Metoprolol/química , Metoprolol/farmacocinética , Metoprolol/farmacología , Ratas , Ratas Wistar
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