Development And Optimization of a Nanostructured Lipid Carrier - Based Anti - Inflammatory Topical Gel for Enhanced Drug Delivery

Abstract

The present study was carried out to develop a transdermal drug delivery system of optimized prepared Meloxicam loaded nanostructured lipid carriers to enhance topical drug delivery and to reduce the possible systemic adverse effect. NLCs were prepared by using modified hot high - speed homogenization technique and were optimized by using 3² factorial designs coupled with response surface methodology by using design expert® software. The independent variables like solid lipid to liquid lipid ratio (X₁) and su rfactant concentration (X₂) and dependent variables like particle size (Y₁) and entrapment efficiency (Y₂) were selected. Total nine formulations were prepared by using 3² factorial designs and were subjected to statistical analysis. The prepared NLCs were characterized for their particle size, zeta potential, polydispersity index (PDI) , drug entrapment efficiency. The optimized NLCs were further loaded into the gel formulations as a drug reservoir system for transdermal delivery of the drug. The gel formulations were examined for physical appearance, pH, viscosity, spreadability , homogeneity, in vitro drug diffusion and in vivo studies. The NLC formulation consisting of 2% total lipid with a solid to liquid lipid ratio of 70:30 and 2% surfactant was found to be the optimized formulation with the particle size of 334.0 ± 1.41 nm a nd PDI of 0.319 ± 0.11%, while the zeta potential was found to be −48.3 ± 1.9 mV indicating that the formulation has good physical stability. The optimized NLCs showed a high drug entrapment efficiency of 91.57 ± 1.1%. Moreover, the pharmacokinetics proper ties of the optimized Meloxicam transdermal formulation were significantly enhanced as compared to the pure drug. The results of this study illustrate the potential for transdermal delivery of Meloxicam using NLCs, as a strategy to obtain a prolonged relea se of the drug and, therefore, enhance its topical therapeutic efficacy.