摘要

Aim: The main objective of the current investigation was to develop nanostructured lipid carriers (NLC) based gel for the enhancement of transdermal absorption of meloxicam (MLX) to achieve local as well as systemic drug action without concurrent gastrointestinal toxicity. Main methods: NLC gel containing MIX was prepared and characterized for particle size, polydispersity, zeta potential, pH, rheology, entrapment efficiency, occlusion factor, and thermal behavior. In vitro drug release, in vitro skin permeation and deposition studies were carried out using Franz diffusion cells. Differential scanning calorimetiy (DSC) and Fourier transform infrared spectroscopy (FTIR) of MLX-NLC gel treated stratum corneum (SC) were undertaken to get an insight into the skin permeation enhancement mechanism of MLX-NLC gel. Toxicity potential of the developed gel formulation was assessed by in vitro hemolysis and histopathological examinations. The rat paw edema test was performed to evaluate the anti-inflammatory activity of MLX-NLC gel. Key findings: MLX-NLC gel demonstrated sustained release and enhanced the skin permeation and deposition of meloxicam especially into the dermis in comparison to meloxicam gel (control). MLX-NLC had an impact on the barrier properties of the skin and acted via protein and lipid modifications in the stratum corneum. MLX-NLC gel turned out to be hemocompatible, non-irritant, and non toxic with significant anti-inflammatory activity. Significance: The results suggest that NLC gel could be a promising carrier for the transdermal delivery of meloxicam.

  • 出版日期2013-11-13