Bioavailability enhancement of repaglinide from transdermally applied nanostructured lipid carrier gel: Optimization, in vitro and in vivo studies
Repaglinide (RG) is an effective anti-diabetic drug (BCS class II) with limited oral bioavailability < 55% due to poor solubility and high first-pass hepatic metabolism. The aim of the paper was to formulate repaglinide loaded nanostructured lipid carrier-gel (RG-NLCs-gel) system to improve the bioavailability by transdermal route.
The RG-NLCs was prepared by high speed homogenizer technique and characterized for size, drug entrapment, viscosity, texture analysis, pH, SEM, XRD, transdermal flux and in vivo pharmacokinetic studies. Box- Behnken design was applied to optimize the RP-NLCs-gel for sustained transdermal delivery. The optimized batch was obtained at X1 [Gelucire (solid lipid)] = 180.41 mg, X2 (Tween 80) = 0.75% and X3 (drug) = 13.97 mg to achieve Y1 (particle size) = 165.08 nm, Y2 (entrapment efficacy) = 70.22% and Y3 (transdermal flux) = 16.12 μg/(cm2/h).
The optimized RG-NLCs gel showed sustained release up to 24 h. The in vivo pharmacokinetic study showed 2 times improvement in the bioavailability in comparison to marketed oral tablet in rat model. The data suggest the potential of RG-NLCs gel for transdermal drug delivery to manage diabetes mellitus, and the system can be utilized for other BCS class II drugs to substitute oral route for patient compliance.
Article Information: Author links open overlay panelSonia S. Pandey, Mayuri A. Patel, Ditixa T. Desai, Hetal P. Patel, Arti R. Gupta, Shrikant V. Joshi, Dinesh O. Shah, Furqan A. Maulvi; Journal of Drug Delivery Science and Technology, 2020.