Nanostructured lipid carrier for transdermal gliclazide delivery: development and optimization by Box-Behnken design

Abstract

The aim of current study was to prepare and optimize the nanostructured lipid carrier (NLC) for transdermal gliclazide (GCZ) delivery. The melt emulsification followed by ultrasonication technique was utilized to prepare GCZ–loaded-NLC. The optimization of NLC was achieved by Box-Behnken design. The surfactant (Tween 20) % (X1), total lipid (glyceryl monostearate + Lauroglycol™ 90) % (X2), and sonication time (min) (X3) were chosen as independent variables, while particles size (Y1), polydispersity index (Y2), and entrapment efficiency (Y3) were selected as response. Further, the prepared NLC was estimated for in vitro drug release study, ex vivo skin permeation and confocal laser scanning microscopy (CLSM) studies. Results of present study demonstrated that the optimized GCZ loaded NLC formulation presented the particles size, polydispersity index, zeta potential, and entrapment efficiency of 120.4 nm, 0.316, −5.58 mV, and 87.32% respectively. The in vitro drug release study indicated drug release of 68.27 ± 2.98% and 45.87 ± 2.85% for GCZ-NLC and conventional GCZ dispersion respectively. The GCZ-NLC-Gel formulation exhibited transdermal drug permeation of 76.89 ± 2.52% as compared to conventional gel (45.65 ± 2.79%). The CLSM of rat skin treated with NLC gel exhibited a deeper permeation (35 μm) in comparison to the conventional gel (15 μm). In conclusion, GCZ loaded NLC was successfully optimized using Box-Behnken design that contributed many advantages over conventional formulation and thus demonstrating NLC as propitious carriers for the transdermal GCZ delivery.