title: Budesonide-loaded nanostructured lipid carriers reduce inflammation in murine DSS-induced colitis.
abstract: The challenge for the treatment of inflammatory bowel disease (IBD) is the delivery of the drug to the site of inflammation. Because nanoparticles have the ability to accumulate in inflamed regions, the aim of the present study was to evaluate nanostructured lipid carriers (NLCs) as nanoparticulate drug delivery systems for the treatment of IBD. Budesonide (BDS) was chosen as a candidate anti-inflammatory drug. BDS-loaded NLCs (BDS-NLC) produced by high-pressure homogenization had a size of 200 nm and a negative zeta potential. BDS-NLCs reduced the TNF-α secretion by activated macrophages (J774 cells). BDS-NLCs were more active in a murine model of dextran sulfate-induced colitis when compared with Blank-NLCs or a BDS suspension: BDS-NLCs decreased neutrophil infiltration, decreased the levels of the pro-inflammatory cytokines IL-1β and TNF-α in the colon and improved the histological scores of the colons. These data suggest that NLCs could be a promising alternative to polymeric nanoparticles as a targeted drug delivery system for IBD treatment.
authors.affiliation: Pharmacokinetics, Nanotechnology and Gene Therapy Group, School of Pharmacy, University of the Basque Country UPV/EHU, Vitoria-Gasteiz, Spain.
authors.forename: Ana
authors.initials: A
authors.lastname: Beloqui
authors.forename: Régis
authors.initials: R
authors.lastname: Coco
authors.forename: Mireille
authors.initials: M
authors.lastname: Alhouayek
authors.forename: María Ángeles
authors.initials: MÁ
authors.lastname: Solinís
authors.forename: Alicia
authors.initials: A
authors.lastname: Rodríguez-Gascón
authors.forename: Giulio G
authors.initials: GG
authors.lastname: Muccioli
authors.forename: Véronique
authors.initials: V
authors.lastname: Préat
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage* / Q000737:chemistry; D019819:Budesonide / Q000008:administration & dosage* / Q000737:chemistry; D002460:Cell Line; D003092:Colitis / Q000139:chemically induced / Q000188:drug therapy* / Q000276:immunology / Q000473:pathology; D003106:Colon / Q000187:drug effects / Q000276:immunology / Q000473:pathology; D016264:Dextran Sulfate; D004337:Drug Carriers / Q000008:administration & dosage* / Q000737:chemistry; D005260:Female; D007249:Inflammation / Q000139:chemically induced / Q000188:drug therapy / Q000276:immunology / Q000473:pathology; D053583:Interleukin-1beta / Q000276:immunology; D008055:Lipids / Q000737:chemistry; D051379:Mice; D008810:Mice, Inbred C57BL; D049329:Nanostructures / Q000008:administration & dosage* / Q000737:chemistry; D009195:Peroxidase / Q000276:immunology; D014409:Tumor Necrosis Factor-alpha / Q000276:immunology
chemical_list: D000893:Anti-Inflammatory Agents; D004337:Drug Carriers; D053583:Interleukin-1beta; D008055:Lipids; D014409:Tumor Necrosis Factor-alpha; D019819:Budesonide; D016264:Dextran Sulfate; D009195:Peroxidase
keywords: Budesonide; Colonic delivery; Inflammatory bowel disease; Macrophages; Nanostructured lipid carriers