DEMONSTRATION OF LYMPHATIC UPTAKE OF (6)-GINGEROL SOLID LIPID NANOPARTICLES

Abstract

(6)-Gingerol, a disease modifying anti-rheumatoid drug (DMARD) agent in the treatment of Rheumatoid Arthritis is a potent inhibitor of COX-1, COX-2 activity, inhibits PGE2 production. It also inhibits the production of TNF-α by blocking the cell associated conversion of TNF precursor to mature proteins thus, halting the proliferation of synovitis. (6)-Gingerol undergo extensive phase I metabolism & underlies low systemic exposure. The aim of the present study was to overcome these limitations and formulate and evaluate Ginger extract Solid Lipid Nanoparticles to improve bioavailability by enabling lymphatic uptake. (6)-Gingerol Solid Lipid Nanoparticles were prepared by melt emulsification-homogenization method and the particle size, Zeta potential PDI and % entrapment efficiency was optimized using Box Behnken design. The optimized SLN were found to be 237nm in size, bearing -25.3mv zeta potential, 0.350 PDI and entrapment efficiency of 91.33%.  Ex vivo endocytic uptake studies (everted intestine method) revealed involvement of endocytic pathways in the uptake of Solid Lipid Nanoparticles from intestine. Thus underlining the utility of SLN for enhancement of uptake of (6)-Gingerol.