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.

Nanoparticle-Based Drug Delivery Systems for Inflammatory Bowel Disease Treatment

“… [ 72 ] UC Passive Positive charges – Zingerone Zin-SLNPs RAW 264.7 cell line model Negative surface charge for better adhesion; superior biosafety. [ 73 ] UC Passive Positive charges and esterase Intrarectally administered Dex Inflammation targeting hydrogel DSS mice and TRUC mice model, Caco2, and HT-29 cell line model IT-hydrogel reduces systemic drug exposure, prolongs local drug release, and improves efficacy more than free Dex enemas. [ 74 ] Abbreviations : ST, Spleen targeting; H 2 S, H 2 S donor; NLCs, nanostructured lipid carriers; SiNP, silica nanoparticles; PPNP, polymers self-assembled nano-particle; IFX, infliximab; PLGA, poly(lactic-co-glycolic acid); 5-ASA, 5-Amino salicylic acid; siRNP, silica-containing redox nanoparticles; SeM, diselenide-bridged mesoporous silica nanoparticles; AC, aminoclay-liposome-coated; EAC, Eudragit S100-liposome-coated; MSMs, mesoporous silica materials; MSs, multilayer-coated mesoporous silica; Cur, curcumin; EM, Escherichia coli strain Nissle 1917-(EcN) membrane; Bud, budesonide; Azo.pu, azo-polyurethane; HES, hydroxyethyl starch; Tpl, tempol; OxbCD, Oxidation-responsive b-cyclodextrin; OVA, oval-bumin; BBR, berberine; HPMCAS, hydroxypropyl methylcellulose acetate succinate; GAR, garcinol; MSNs, mesoporous silica nanoparticles; OxiDEX, oxidation-sensitive dextran; TNF- α, tumor necrosis factor-α; PEG, polyethylene glycol; HEP, heparin; HAS, human serum albumin; NP, nanopolyplexe; SLNPs, solid lipid nanoparticles; MMT, montmorillonite.…”