title: Eudragit nanoparticles loaded with silybin: a detailed study of preparation, freeze-drying condition and in vitro/in vivo evaluation.
abstract: The objective of this work was use of silybin nanoparticles in treatment of ulcerative colitis (UC). Eudragit RL PO nanoparticles loaded with silybin were produced using solvent-evaporation emulsification technique. Then, they were coated by Eudragit FS30D. Drug release was studied in different physiological environments. Colitis was induced by 4% of acetic acid in rats which received freeze-dried nanoparticles of silybin (75 mg/kg/day), dexamethasone (1 mg/kg/day), blank nanoparticles and normal saline orally for 5 days. Then macroscopic, histopathological evaluation and biochemical analysis, including myeloperoxidase (MPO) activity, tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6) levels in colon tissues were determined using enzyme-linked immunosorbent assay (ELISA) kits. Macroscopic and histopathological scores were improved by the optimised nanoparticles. The optimised nanoparticles had a particle size of 109 ± 6 nm, zeta potential of 15.4 ± 2 mV, loading efficiency of 98.3 ± 12% and release efficiency of 40.8 ± 5.5% at 24 h. TNF-α, IL-6 and MPO activity were reduced significantly by nanoparticles compared to control group (p < 0.05).
authors.affiliation: Department of Pharmaceutics, School of Pharmacy and Novel Drug Delivery Systems Research Centre, Isfahan University of Medical Sciences , Isfahan , Iran and.
authors.forename: Jaleh
authors.initials: J
authors.lastname: Varshosaz
authors.forename: Mohsen
authors.initials: M
authors.lastname: Minaiyan
authors.forename: Nifiseh
authors.initials: N
authors.lastname: Khaleghi
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage / Q000627:therapeutic use; D000975:Antioxidants / Q000008:administration & dosage* / Q000627:therapeutic use; D003092:Colitis / Q000188:drug therapy* / Q000276:immunology / Q000473:pathology; D003106:Colon / Q000187:drug effects* / Q000473:pathology; D003907:Dexamethasone / Q000008:administration & dosage / Q000627:therapeutic use; D004337:Drug Carriers / Q000737:chemistry*; D005612:Freeze Drying; D007249:Inflammation / Q000188:drug therapy / Q000276:immunology / Q000473:pathology; D015850:Interleukin-6 / Q000032:analysis / Q000276:immunology; D008297:Male; D020944:Silybum marianum / Q000737:chemistry; D053758:Nanoparticles / Q000737:chemistry*; D009195:Peroxidase / Q000032:analysis / Q000276:immunology; D011109:Polymethacrylic Acids / Q000737:chemistry*; D017208:Rats, Wistar; D000077385:Silybin; D012838:Silymarin / Q000008:administration & dosage* / Q000627:therapeutic use; D014409:Tumor Necrosis Factor-alpha / Q000032:analysis / Q000276:immunology
chemical_list: D000893:Anti-Inflammatory Agents; D000975:Antioxidants; D004337:Drug Carriers; D015850:Interleukin-6; D011109:Polymethacrylic Acids; D012838:Silymarin; D014409:Tumor Necrosis Factor-alpha; C038300:methylmethacrylate-methacrylic acid copolymer; D000077385:Silybin; D003907:Dexamethasone; D009195:Peroxidase
keywords: Acetic acid-induced colitis; Eudragit FS30; Eudragit RL PO; nanoparticles; silybin