Zingerone‐encapsulated Solid Lipid Nanoparticles as Oral Drug‐delivery Systems to Potentially Target Inflammatory Diseases

Abstract Currently, various anti‐inflammatory drugs are used in intestinal bowel disease (IBD) treatment as first‐line management therapies. Although beneficial effects were observed with these drugs, unwanted exposure to healthy tissue causes side‐effects. Therefore, targeted delivery of anti‐inflammatory drugs to the inflamed tissue is still an unmet need. Herein, we have developed solid lipid nanoparticles with negative surface charge that can specifically adhere to transferrin, a protein that overexpressed at the inflamed tissue. Zingerone, a natural product based anti‐inflammatory agent, has been encapsulated into solid lipid nanoparticles (Zin‐SLNPs) and protected from the degradation by stomach and intestinal fluids. The Zin‐SLNPs consists of 250–350 nm in size, have negative surface charge (‐44.08 mV). These Zin‐SLNPs have shown appreciable cyto‐compatibility, they did not show any cytotoxicity even as high as 1000 μM concentration. Native zingerone and zingerone that released from Zin‐SLNPs show efficient anti‐inflammatory property by reducing the production of pro‐inflammatory cytokines from lipopolysaccharide (LPS)‐induced RAW 264.7 macrophages, in vitro. Based on these results, in the future studies, Zin‐SLNPs could be tested for their potential therapeutic efficacy in ulcerative colitis in vivo model.