title: Novel Curcumin Diclofenac Conjugate Enhanced Curcumin Bioavailability and Efficacy in Streptococcal Cell Wall-induced Arthritis.
abstract: Curcumin-diclofenac conjugate as been synthesized by esterification of phenolic group of curcumin with the acid moiety of diclofenac, and characterized by mass spectrometry, NMR, FTIR, DSC, thermogravimetric analysis and X-ray diffraction analysis. The relative solubility of curcumin-diclofenac conjugate, curcumin and diclofenac; stability of curcumin-diclofenac conjugate in intestinal extract; permeability study of curcumin-diclofenac conjugate using the everted rat intestinal sac method; stability of curcumin-diclofenac conjugate in gastrointestinal fluids and in vitro efficacy have been evaluated. In vivo bioavailability of curcumin-diclofenac conjugate and curcumin in Sprague-Dawley rats, and antiarthritic activity of curcumin-diclofenac conjugate, curcumin and diclofenac in modified streptococcal cell wall-induced arthritis model in Balb/c mice to mimic rheumatoid arthritis in humans have also been studied. In all of the above studies, curcumin-diclofenac conjugate exhibited enhanced stability as compared to curcumin; its activity was twice that of diclofenac in inhibiting thermal protein denaturation taken as a measure of in vitro antiinflammatory activity; it enhanced the bioavailability of curcumin by more than five folds, and significantly (P<0.01) alleviated the symptoms of arthritis in streptococcal cell wall-induced arthritis model as compared to both diclofenac and curcumin.
authors.affiliation: National Institute of Pharmaceutical Education and Research (NIPER), SAS Nagar-160062, India.
authors.forename: S K
authors.initials: SK
authors.lastname: Jain
authors.affiliation: Department of Pharmaceutical Technology (Formulation), SAS Nagar-160062, India.
authors.forename: M S
authors.initials: MS
authors.lastname: Gill
authors.affiliation: National Institute of Pharmaceutical Education and Research (NIPER), SAS Nagar-160062, India.
authors.forename: H S
authors.initials: HS
authors.lastname: Pawar
authors.affiliation: National Institute of Pharmaceutical Education and Research (NIPER), SAS Nagar-160062, India.
authors.forename: Sarasija
authors.initials: S
authors.lastname: Suresh
keywords: Curcumin; diclofenac; drug conjugate; oral bioavailability; rheumatoid arthritis