MUCOADHESIVE MICROBEADS OF METFORMIN HCL: A PROMISING SUSTAINED DRUG DELIVERY SYSTEM

Abstract

The present work was investigated to reduce the dosing frequency, improve patient compliance, to improve gastric residence and to decrease GI side effects by designing and evaluating controlled Release Mucoadhesive (CRM) microbeads of Metformin hydrochloride for effective control of diabetes type-II. Microbeads were prepared by employing ionic gelation method by using various natural and synthetic polymers such as sodium alginate as main polymer and sodium carboxy methyl cellulose(SCMC), carboxy methyl cellulose(CMC), methyl cellulose (MC), poly vinyl pyrrolidine (PVP) as co-polymers which mainly containing mucoadhesive property. These polymers are used with various proportions using calcium chloride as across linking agent. The mucoadhesive property of four polymers is in the following order (SCMC > CMC > MC > PVP).Twenty formulations were prepared. The mucoadhesive beads were characterized for micromeritic properties such as bulk density, tapped density, hausner’s ratio, compressibility index, angle of repose, percentage drug content, entrapement effieciency, swelling index, In-vitro drug release, mucoadhesion test, drug kinetics and FT-IR studies. The drug entrapment efficiency increased progressively with increasing concentration of co - polymer resulting in the formation of larger microbeads entrapping greater amounts of the drug. No significant drug-polymer interactions were observed in FT-IR studies. The kinetics of drug release and their mucoadhesive nature in vitro using goat intestinal mucosa was also investigated at physiological pH 1.2 HcL. The effective mucoadhesion property with controlled release profile was observed from optimized mucoadhesive beads consisting of Sodium alginate and SCMC (1:5). The prepared microspheres exhibited prolonged drug release as the concentration of co- polymer increased, as the SCMC polymer concentration increases the mucoadhesion increased and the drug release rate decreased at higher concentration of sodium alginate.