Abstract

Gaurav Kumar, Yatendra Kumar, Mohammad Rashid, Swamita Arora, Sanjar Alam

ABSTRACT

Rheumatoid Arthritis (RA) is a chronic autoimmune inflammatory disease that involves a sustained inflammatory response of the joints and the eventual destruction of the connective tissues. Naringin, a naturally occurring flavonoid, has strong anti-inflammatory and antioxidant properties, but is hampered in its therapeutic use by poor solubility and low bioavailability. Hence the present study aimed at the formulation and evaluation of naringin loaded nanoemulsion gel for improving the anti-inflammatory efficacy and transdermal drug delivery for RA. The aqueous titration method was used to formulate the nanoemulsion with oleic acid as the oil phase, Tween 80 as the surfactant and ethanol as the co-surfactant. To define the nanoemulsion region and the nanoemulsion formulation composition, a pseudo-ternary phase diagram was drawn. The optimized nanoemulsion was incorporated in a Carbopol 934 gel base to get the nanoemulsion gel. Characterized: Particle size, 203.7 nm; Polydispersity index (PDI), 0.277 – 0.390; zeta potential, ?27.2 ± 1.3 mV (SK-2); surface morphology is Clear, transparent, smooth and homogeneous nanoemulsion droplets, without aggregation or phase separation; physical stability is No phase separation, turbidity, precipitation or color change after centrifugation and freeze – thaw cycles. Permeation studies of the drug diffusion through the skin was done in vitro using Franz diffusion cell. The anti-inflammatory activity of the formulation was assessed by protein denaturation assay. The nanoemulsion gel exhibited good protein denaturation inhibitory activity, showing dependence on concentration, which demonstrated that the nanoemulsion gel had a good anti-inflammatory activity and prevented protein degradation. Furthermore, the formulation showed improved permeation and physiological stability as compared to the conventional formulation. Overall, the developed naringin loaded nanoemulsion gel exhibited enhanced solubility, enhanced transdermal permeation and better anti-inflammatory activity which indicate that it can be used as a potential topical therapeutic system for the management of rheumatoid arthritis.