Pharmacokinetic and pharmacodynamic studies of etodolac loaded vesicular gels on rats by transdermal delivery

The present study includes the development of liposomal and ethosomal gels for transdermal delivery to overcome the side effects associated with oral route.

The liposomes and ethosomes were prepared by 32 factorial design using film hydration and cold methods, respectively. Different concentrations of liposomal (ETO-LG) and ethosomal (ETO-EG) gels were prepared at 1%, 2 and 3% (w/v) using carbopol 940 NF. 1%w/v ETO-LG & ETO-EG were optimized upon rheological studies of prepared gels. The optimized gels were further characterized for various physicochemical properties and biophysical studies using FTIR, pharmacokinetic (PK) and pharmacodynamic (PD) studies. The pharmacodynamic activity was performed using carrageenan paw oedema model. The prepared vesicular gels were compared with 45% v/v ethanolic ETO-solution and marketed gel PROXYM® in all the characteristic parameters.

The pharmacokinetic study reveals that the half life of etodolac in ETO-EG was 1.56 folds whereas ETO-LG showed 1.31 folds higher than PROXYM®. The mean residence time (MRT) of etodolac in ETO-EG and ETO-LG is increased in 1.57 and 1.25 folds, respectively, when compared to PROXYM®. The ETO-EG showed higher percentage reduction in oedema (81.67%) compared to other test products.

The pharmacokinetic and pharmacodynamic studies indicated that the vesicular gels show better results compared to PROXYM®. The correlation coefficient value between PK and PD was found to be 0.9635. Graphical abstract ᅟ.