This work aims to improve the antiarthritic activity of (-)-epigallocatechin gallate (EGCG) and glucosamine (GA) through fabrication and optimization of casein protein nanoparticles (EGC-NPs). Optimized EGC-NPs were obtained with a EGCG/GA/casein ratio of 1:2:8 (w/w/w). The EGC-NPs gave a mean size of 186 ± 3.5 nm and an entrapment efficiency of 86.8 ± 2.7%, and they exhibited a greater inhibitory activity against human fibroblast-like synoviocytes-osteoarthritis cells and human fibroblast-like synoviocytes-rheumatoid arthritis cells compared with that of the EGCG-GA mixture by 33.5% and 20.8%, respectively. Freeze-dried EGC-NPs stored at 25 °C during 12 months showed high dispersion stability. Moreover, the redispersion of the freeze-dried EGC-NPs produced almost no significant changes in their physicochemical properties and bioactivity. Rat experiments demonstrated that the antiarthritis effect of the EGC-NPs was significantly higher than that of EGCG-GA mixture, as assessed through an analysis of anti-inflammatory efficacy, radiographic images and histopathological assessments of paw joints, and immunohistochemical changes in serum cytokines. The enchanced antiarthritic activity in vivo was consistent with that in vitro. The EGC-NPs demonstrate potential as a food supplement for the treatment of arthritis.
Keywords: (−)-epigallocatechin gallate; arthritis; caseins; glucosamine; nanoparticle.