Transdermal delivery of lornoxicam via transethosomal gel as a novel strategy for management of rheumatoid arthritis.

Abstract

Objective: This study aimed to develop and optimize lornoxicam-loaded transethosomal vesicles (LOR-TES) to improve the solubility, skin permeation, and transdermal delivery of lornoxicam for potential use in the treatment of rheumatoid arthritis.

Methods: LOR-TES formulations were prepared using the thin-film hydration method. A Box-Behnken design (BBD) was employed to evaluate the influence of formulation variables, such as lipid content, ethanol concentration, and surfactant amount. The optimized vesicles were incorporated into a Carbopol-based gel using the soaking method and refined through a hit-and-trial approach. The formulations were characterized for particle size (PS), polydispersity index (PDI), zeta potential (ZP), and entrapment efficiency (%EE). Surface morphology was assessed using scanning electron microscopy (SEM), while compatibility and encapsulation were confirmed via Fourier-transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC). In vitro drug release, ex vivo skin permeation using Franz diffusion cells, and stability studies over six months were conducted.

Results: The optimized LOR-TES showed a PS of 150.7 ± 1.2 nm, PDI of 0.326 ± 0.04, a ZP of -23.3 ± 0.9 mV, and %EE of 80.9 ± 0.2%. SEM revealed spherical morphology, while FTIR and DSC confirmed compatibility and successful encapsulation. In vitro release studies showed sustained drug release, and ex vivo studies demonstrated a fourfold increase in skin permeation from the LOR-TES gel compared to the conventional formulation. Stability testing confirmed formulation stability.

Conclusions: The developed LOR-TES gel enhanced transdermal drug delivery, offering sustained release and improved permeation. It presents a promising strategy for effective management of rheumatoid arthritis through the transdermal route.