article · Drug Delivery
Repaglinide is an oral medication used for type II diabetes that suffers from poor water solubility and variable bioavailability due to liver metabolism. To address these issues and provide an alternative for patients with swallowing difficulties, repaglinide was encapsulated into niosomes and prepared as chewable tablets using coprocessed excipients. The optimised niosomal formulation achieved high entrapment efficiency and sustained drug release. Chewable tablets prepared with Pharmaburst 500 and F-melt exhibited good physical characteristics, along with rapid initial drug release and sustained release over six hours compared to commercial Novonorm tablets. In rat trials, these chewable tablets produced a significantly faster and more sustained reduction in blood glucose levels than the commercial product, offering a promising oral delivery system.
Patients with type II diabetes frequently experience difficulty swallowing standard tablets, which can reduce adherence to treatment. Formulating repaglinide into chewable tablets using niosomes overcomes poor drug solubility and provides both faster and more sustained blood sugar control. This approach could offer a more comfortable and reliable treatment option for diabetic individuals affected by dysphagia.
This delivery system could enable pharmaceutical manufacturers to produce chewable diabetes therapies designed for patients who struggle to swallow standard tablets. The technology is applied and tested, with proven laboratory release characteristics and validated hypoglycaemic efficacy in rat models. Further pre-clinical development and human clinical trials will be required to demonstrate safety and efficacy before commercial adoption.
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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 peceolTM. 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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DOI: 10.1080/10717544.2023.2181747
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