FORMULATION AND EVALUATION OF COX-2 INHIBITOR LOADED GOLD NANOPARTICLES ENRICHED HYDROGEL FOR TREATMENT OF RHEUMATOID ARTHRITIS.

Jessy Shaji* and Seema Darade

ABSTRACT

In the present study, we synthesized Piroxicam Monoethanolamine (PRX-MEA) conjugated gold nanoparticles (PM-AuNPs) by a simple economic, nontoxic green synthesis using Camellia sinesis (green tea) extract as reducing agent and Tween 80 as stabilizer. PM-AuNPs were developed using 19 run, 3 factors and 2-level full factorial design. The particle size and zeta potential of the optimized batch were 51.2 ± 33.8 nm and -30.2 ± 14.2 mV respectively. The loading efficiency of PRX-MEA was found to be 89.05 ± 0.41%. The surface morphology of gold nanoparticles was investigated by TEM. The synthesized particles were largely spherical in shape with a smooth morphology. Selected area electron diffraction (SAED) pattern revealed diffraction patterns of crystalline gold structure. FTIR spectroscopy identified the conjugation of PRX-MEA to the surface of AuNPs. The structural characterization and crystalline nature of PM-AuNPs was determined by XRD. Furthermore, in this study PM-AuNPs enriched hydrogel was fabricated and evaluated for pH, drug content and spreadability. PM-AuNPs dispersion and hydrogel were studied for an in- vitro drug release and skin permeation potential. The cumulative percentage drug released at the end of 48 h was found to be 91.24 ± 3.48%. In transdermal experiments, the steady state flux and the permeability coefficient of PM-AuNPs and PM-AuNPs hydrogel were significantly higher than plain drug solution (p<0.01). In the in-vitro antioxidant assay and in-vivo anti-inflammatory activity PM-AuNPs showed superior activity over PRX-MEA. The results indicate that the developed formulation offers significant protection towards inflammatory effects in rheumatoid arthritis.

Keywords: Piroxicam monoethanolamine, rheumatoid arthritis, gold nanoparticles, green tea, hydrogel, anti-inflammatory.