Potential treatment of arthritis with an optimized Mometasone Furoate loaded-ethosomal gel in carrageenan-induced rat joint arthritis

The aim of this work was to improve the transdermal delivery of Mometasone Furoate (MF) by developing an optimal ethosomal system for targeting inflammatory cases. The effects of Phospholipon 90G (PC90G) (X1), ethanol (X2), propylene glycol (PG) (X3) and sonication time (X4) were optimized for their effects on entrapment efficiency (Y1), vesicle size (Y2), zeta potential (Y3), skin flux (Y4) and skin accumulation (Y5) using Box Behnken design. The optimal MF formula (OMF) was characterized and underwent a comparative skin penetration study with the liposomal system and hydroalcoholic dispersion of MF. OMF was loaded into Carbopol gel for conducting a comparative in-vivo study with standard MF loaded gel and the market product using a carrageenan-induced rat joint arthritis model. The observed values of OMF were 68.44%, 62.87 nm, −15.92 mV, 7.42 μg/cm2/h and 16.63 μg/cm2/24h for Y1, Y2, Y3, Y4, and Y5; respectively. X2 and X3 were the main factors affecting Y1, Y3, Y4 and Y5 while Y2 was mainly affected by sonication time. TEM images showed ethosomal vesicles with multiple layers of the spherical structure. The skin flux of OMF was 2.33 and 3.53 folds of liposomes, hydroalcoholic dispersion; respectively. Moreover, the confocal laser scanning microscopy (CLSM) confirmed the penetration potential of OMF over other systems. Daily application of ethosomal gel for ten days significantly improved the arthritis degree while normal joint histological structures were observed after twenty days. Therefore, MF-loaded ethosomes represents a promising therapeutic approach for the treatment of arthritis. [Display omitted]