Akademik Veri Yönetim Sistemi
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, cilt.200, ss.106844, 2024 (SCI-Expanded)
Repaglinide (RPG) belongs to the class of drugs known as meglitinides and is used for improving and maintaining
glycemic control in the treatment of patients with Type 2 diabetes. RPG is a Class II drug (BCS) because of its high
permeability and low water solubility. It also undergoes hepatic first-pass metabolism. The oral bioavailability of
RPG is low (about 56 %) due to these drawbacks. Our aim in this study is to prepare two different nano-sized
drug carrier systems containing RPG (nanoparticle: RPG-PLGA-Zein-NPs or nanoemulsion: RPG-NE) and to
carry out a pharmacokinetic study for these formulations. We prepared NPs using PLGA and Zein. In addition, a
single NE formulation was developed using Tween 80 and Pluronic F68 as surfactants and Labrasol as co-
surfactant. The droplet size values of the blank-NE and RPG-NE formulations were found to be less than 120
nm. The mean particle sizes of blank-Zein-PLGA-NPs and RPG-Zein-PLGA-NPs were less than 260 nm. The Cmax
and tmax values of RPG-Zein-PLGA-NPs and RPG-NE (523 ± 65 ng/mL and 770 ± 91 ng/mL; 1.41 ± 0.46 h and
1.61 ± 0.37 h, respectively) were meaningfully higher than those of free RPG (280 ± 33 ng/mL; 0.72 ± 0.28 h)
(p < 0.05). The AUC0-∞ values calculated for RPG-Zein-PLGA-NPs and RPG-NE were approximately 4.04 and
5.05 times higher than that calculated for free RPG. These nanosized drug delivery systems were useful in
increasing the oral bioavailability of RPG. Moreover, the NE formulation was more effective than the NP
formulation in improving the oral bioavailability of RPG (p < 0.05).