Nanostructured Lipid Carriers of Eperisone Hydrochloride using Quality By Design Approach

Abstract

Objective: The current work involves formulation development of nanostructured lipid carrier (NLC) of eperisone hydrochloride (EPE) using quality by design (QbD) approach.
 Materials and Methods: Initial screening of solid and liquid lipids was performed based on the Hansen solubility parameters of EPE and the lipids and later confirmed using saturation solubility studies. The optimum formulation was identified using three-squared randomized full factorial design. High shear homogenization coupled with ultrasonication was used to prepare the NLCs. The effect of the independent variables on the dependent variables was analyzed using response surface graphs and ANOVA. The optimized formulation is characterized for mean particle size, zeta potential, entrapment efficiency, in vitro drug release and subjected to stability testing.
 Results and Discussion: Precirol® ATO 5, CapryolTM 90, and Pluronic® F127 are found to be ideal solid lipid, liquid lipid and surfactant respectively based on the initial screening. Amount of lipid mixture (X1) and the amount of surfactant (X2) were selected as independent variables and the entrapment efficiency (Y1), mean particle size (Y2) and zeta potential (Y3) were selected as dependent variables. The optimized NLC formulation has mean particle size of 175 nm, zeta potential -24.4 mV and entrapment efficiency of 78.64%. The in vitro drug release data suggested that the drug release follows Quasi-Fickian diffusion. The stability data showed that the NLCs are stable up to 3 months at refrigerated conditions.
 Conclusions: The Hansen solubility parameter approach coupled with QbD is a powerful tool for formulation of sustained release NLCs of highly soluble poorly soluble drugs.
 Keywords: Nanostructured lipid carrier, Solubility Parameters, Nanoparticles, Lipid based drug delivery, Quality by Design