Transdermal delivery of Etoricoxib through ethosomal formulation: An ingenious approach towards treatment of skin inflammation

•An ethosomal formulation of ET and CD complex for treatment of skin inflammation.•Maintained drug concentration in blood serum.•Deeper skin layer penetration ability of the ethosomal formulation.•Minimal change in residual drug content after 90 days.

Etoricoxib (ET) based formulations viz. physical mixture of ET with β-cyclodextrin (CD); ethosomal formulation of ET and CD complex (DCE); and ET are investigated against skin inflammation. These formulations are characterized using XRD, SEM, TEM and DSC, revealed the amorphous nature of DCE (particle size 0.3-0.4 μm). ET with ethosome (PDE) and ET, CD with ethosome (DCE) is prepared using varied concentrations of lecithin and ethanol; demonstrated entrapment efficiencies of 70.8 ± 4.4% and 77.5 ± 4.2% for PDE-8 and DCE-8 respectively. Kneaded complex (KC) exhibited 77.96% and 75.32% drug release in 30 min in PBS pH 7.4 and 5.5 respectively. In-vitro and ex-vivo drug permeation in phosphate buffer saline (PBS) revealed 63-82% ET permeation for DCE-8; while in rat serum DCE-8 produced higher plasma concentration of ET (3.26 ± 0.25 μg/ml) within 8 h that is maintained over 24 h. The percentage inhibition of carrageenan induced paw edema, 8 h after applying DCE-8 is found to be 77.74% higher than PDE-8 (54.1%) and one more formulation which is a mixture of ET and ethanol in proper proportion (CPD) (20.04%). Stability studies indicated that DCE-8 stored at 5 ± 3 °C shows <5% change in residual drug content after 90 days. Present work clearly demonstrates that the tailor-made formulation DCE-8 may exhibit potentiality towards transdermal delivery of ET in the treatment of skin inflammation.

Graphical abstractEx-vivo studies performed on Etoricoxib: β-cyclodextrin complex ethosomal formulation revealed improved skin penetration and ability of the complex to maintain the constant drug concentration over 24 h in rat serum.Download high-res image (260KB)Download full-size image