Formulation of novel niosomal repaglinide chewable tablets using coprocessed excipients: in vitro characterization, optimization and enhanced hypoglycemic activity in rats

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 3.5 fold significant reduction in blood glucose compared to Novonorm^® tablets (p < 0.05) at 30 min. Also, at 6h the same tablets showed 1.5 and 1.3 fold significant extended reduction in blood glucose compared to the same market product (p < 0.05). It could be concluded that chewable tablets loaded with RPG ONF represent promising novel oral drug delivery systems for diabetic patients suffering from dysphagia.

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Shahinaze A. Fouad,Mahmoud H. Teaima,Mostafa I. Gebril,Fathy I. Abd Allah,Mohamed A. El-Nabarawi &Sammar Fathy Elhabal, Formulation of novel niosomal repaglinide chewable tablets using coprocessed excipients: in vitro characterization, optimization and enhanced hypoglycemic activity in rats, Article: 2181747 | Received 04 Jan 2023, Accepted 06 Feb 2023, Published online: 20 Feb 2023, https://doi.org/10.1080/10717544.2023.2181747

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