Formulation of novel niosomal repaglinide chewable tablets using coprocessed excipients: in vitro characterization, optimization and enhanced hypoglycemic activity in rats
Abstract
Repaglinide (RPG), a monotherapy insulin secretagogue used to treat diabetes mellitus-type II yet, it suffers from poor water solubility and variable bioavailability (~ 50%) due to hepatic first pass metabolism.In this study, 2FI I-Optimal statistical design was employed to encapsulate RPG into niosomal formulations using cholesterol,span 60 and peceol TM .The optimized niosomal formulation (ONF) showed particle size 306.60 ± 84.00 nm, zeta potential -38.60 ± 1.20 mV, polydispersity index 0.48 ± 0.05 and entrapment efficiency 92.00 ± 2.60%.ONF showed > 65% RPG release that lasted for 3.5 h, and significantly higher sustained release compared to Novonorm® tablets after 6 h (p < 0.0001).TEM for ONF showed spherical vesicles with dark core and light-colored lipid bilayer membrane.RPG peaks disappeared in FTIR confirming successful RPG entrapment.To eliminate dysphagia associating conventional oral tablets, chewable tablets loaded with ONF were prepared using coprocessed excipients; Pharmaburst® 500, F-melt® and Prosolv® ODT.Tablets showed friability <1%, hardness 3.9 ± 0.423-4.7 ± 0.410 Kg, thickness 4.1 ± 0.045-4.4± 0.017 mm and acceptable weight.All tablets showed robust RPG release at 30 min compared to Novonorm® tablets.At 6h, chewable tablets containing only Pharmaburst® 500 and F-melt® showed sustained and significantly increased RPG release compared to Novonorm® tablets (p < 0.05).Pharmaburst® 500 and F-melt® tablets showed rapid in vivo hypoglycemic effect with 5 and…
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