Therapeutic potential of cationic bilosomes in the treatment of carrageenan-induced rat arthritis via fluticasone propionate gel

Abstract

Arthritis is a debilitating disease that affects the patient's mobility and quality of life. This study focused on the development and optimization of a cationic nanosized bilosomal formula for the efficient transdermal treatment of arthritis. An optimum Fluticasone Propionate-loaded bilosomes (OFP) was developed using the Draper-Lin small composite design based on the optimization of 4 factors and evaluation of entrapment efficiency (Y1), vesicle size (Y2), skin flux (Y3), and skin accumulation (Y4). The OFP was characterized against the drug suspension, loaded into a Carbopol gel, and a histopathological assessment was conducted on a carrageenan-induced rat joint arthritis in comparison with cultivate® cream and traditional gel. Interluekin-1β and TNF-α levels were also measured. The optimal formula was formulated using 2.99% phospholipon90G, 0.04% sodium deoxycholate, and 0.29% stearylamine, and showed 84.72%, 268.13 nm, 5.89 µg/cm2/h, and 16.21 µg/cm2 /24 h for Y1, Y2, Y3, and Y4, respectively. The thermal analysis of OFP demonstrated a single broad endothermic peak for bilosomes with no detectable peak for the amorphous drug. TEM images revealed the spherical structures of the nanosized OFP, while CLSM demonstrated enhanced permeation efficiency over the drug suspension. The in-vivo study further proved the promising efficacy of the optimum OFP, where a complete recovery of the normal histological structure of a rat joint and normal levels of the inflammatory markers were observed within 20 days following once daily application of the optimum bilosomal gel. Therefore, OFP represents a competent nanocarrier for efficient transdermal management of joint arthritis.