Formulation Development Characterization and Antidiabetic Activity of Alogliptin Floating Microspheres

Abstract

The present study has been performed to microencapsulate alogliptin, an antidiabetic drug newline(dipeptidyl peptidase-4; DPP-4 inhibitor) for enhancing gastric residence time of drug thereby newlineincreasing its bioavailability. The attempt of this study was to formulate the alogliptin loaded newlinefloating microspheres by emulsion solvent evaporation technique by varying the ratio of polymers newlinei.e. cellulose acetate butyrate (CAB) and polyethylene oxide (PEO), drug loading and newlineconcentration of poly(vinyl alcohol) (PVA) solution. The prepared formulations were studied for newlineentrapment efficiency, particle size, floating behavior, surface morphology by SEM and in vitro newlinedrug release. FTIR spectroscopy was done to confirm the chemical stability of drug after newlinepenetration of microspheres. Microspheres formed were spherical with smooth surfaces as newlinerevealed by SEM. Formulation F3 composed of CAB: PEO (80: 20 wt%) containing 1.5 wt% PVA newlinesolution and drug loading (10 wt%) gave the most advantageous entrapment (87.02 ± 1.06%) and newlinerelease results after 12 h (Q12h = 78.19 ± 0.90%) in simulated gastric fluid pH 1.2 as compared to newlineother compositions. The microspheres tend to float over the simulated gastric media for more than newline10 h. The % buoyancy of microspheres was found to be up to 89.50 ± 1.53% and showed newlinegastroretentive delivery of the drug. Floating microspheres of alogliptin with good floating ability newlineand gastroretentive release were developed.