title: A pH dependent delivery of mesalazine from polymer coated and drug-loaded SBA-16 systems.
abstract: SBA-16 silica was synthesized and modified by post-synthesis method with amino groups. Wet milling in acidic media was applied for loading of poorly soluble drug mesalazine (5-aminosalicylic acid — 5-ASA) in different drug/carrier ratios (1:1; 0.75:1; 0.5:1; 0.25:1). The parent and drug loaded mesoporous silicas were characterized by XRD, TEM,N2 physisorption, thermal analysis, FT-IR and solid state NMR spectroscopy. The drug loaded mesoporous systems were single-coated with Eudragit S or double-coated with Eudragit S and Eudragit RL. The polymer coating significantly modified the rate of mesalazine release fromS BA-16NH2 materials. Applying the double coating method makes possible the sustained delivery of the drug in the intestinal area avoiding the burst release in the gastric fluid. The functionalized, polymer coated mesoporous system could be considered an appropriate oral delivery system for mesalazine. In addition, reduction of mesalazine cytotoxicity on epithelial cells could be achieved by its loading into mesoporous silica particles.
authors.affiliation: Institute of Organic Chemistry with Centre of Phytochemistry, Bulgarian Academy of Sciences, 1113 Sofia, Bulgaria.
authors.forename: Ivalina
authors.initials: I
authors.lastname: Trendafilova
authors.affiliation: Research Centre for Natural Sciences, Institute of Materials and Environmental Chemistry, Hungarian Academy of Sciences, 1117 Budapest, Magyar tudósok körútja 2, Hungary.
authors.forename: Ágnes
authors.initials: Á
authors.lastname: Szegedi
authors.affiliation: Faculty of Pharmacy, Medical University of Sofia, 1000 Sofia, Bulgaria.
authors.forename: Krassimira
authors.initials: K
authors.lastname: Yoncheva
authors.affiliation: Institute of Organic Chemistry with Centre of Phytochemistry, Bulgarian Academy of Sciences, 1113 Sofia, Bulgaria.
authors.forename: Pavletta
authors.initials: P
authors.lastname: Shestakova
authors.affiliation: Research Centre for Natural Sciences, Institute of Materials and Environmental Chemistry, Hungarian Academy of Sciences, 1117 Budapest, Magyar tudósok körútja 2, Hungary.
authors.forename: Judith
authors.initials: J
authors.lastname: Mihály
authors.affiliation: National Institute of Chemistry Slovenia, Hajdrihova 19, 1001 Ljubljana, Slovenia.
authors.forename: Alenka
authors.initials: A
authors.lastname: Ristić
authors.affiliation: Faculty of Pharmacy, Medical University of Sofia, 1000 Sofia, Bulgaria.
authors.forename: Spiro
authors.initials: S
authors.lastname: Konstantinov
authors.affiliation: Institute of Organic Chemistry with Centre of Phytochemistry, Bulgarian Academy of Sciences, 1113 Sofia, Bulgaria. Electronic address: mpopova@orgchm.bas.bg.
authors.forename: Margarita
authors.initials: M
authors.lastname: Popova
mesh_terms: D002470:Cell Survival / Q000187:drug effects; D004337:Drug Carriers / Q000737:chemistry* / Q000494:pharmacology; D004339:Drug Compounding; D065546:Drug Liberation; D019073:HT29 Cells; D006801:Humans; D006863:Hydrogen-Ion Concentration; D019804:Mesalamine / Q000737:chemistry* / Q000494:pharmacology; D053758:Nanoparticles / Q000737:chemistry; D011108:Polymers / Q000737:chemistry* / Q000494:pharmacology; D011109:Polymethacrylic Acids / Q000737:chemistry* / Q000494:pharmacology; D011437:Propylamines; D012821:Silanes / Q000737:chemistry / Q000494:pharmacology; D012822:Silicon Dioxide / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D004337:Drug Carriers; D011108:Polymers; D011109:Polymethacrylic Acids; D011437:Propylamines; C000600619:SBA-16; D012821:Silanes; C038300:methylmethacrylate-methacrylic acid copolymer; D019804:Mesalamine; C058665:Eudragit RL; D012822:Silicon Dioxide; C477625:amino-propyl-triethoxysilane
keywords: Drug–carrier interaction; Eudragit coating; Mesalazine; SBA-16NH(2); Surface modification