A pH dependent delivery of mesalazine from polymer coated and drug-loaded SBA-16 systems

Eur J Pharm Sci. 2016 Jan 1:81:75-81. doi: 10.1016/j.ejps.2015.10.003. Epub 2015 Oct 8.

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.

Keywords: Drug–carrier interaction; Eudragit coating; Mesalazine; SBA-16NH(2); Surface modification.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Survival / drug effects
  • Drug Carriers / chemistry*
  • Drug Carriers / pharmacology
  • Drug Compounding
  • Drug Liberation
  • HT29 Cells
  • Humans
  • Hydrogen-Ion Concentration
  • Mesalamine / chemistry*
  • Mesalamine / pharmacology
  • Nanoparticles / chemistry
  • Polymers / chemistry*
  • Polymers / pharmacology
  • Polymethacrylic Acids / chemistry*
  • Polymethacrylic Acids / pharmacology
  • Propylamines
  • Silanes / chemistry
  • Silanes / pharmacology
  • Silicon Dioxide / chemistry*
  • Silicon Dioxide / pharmacology

Substances

  • Drug Carriers
  • Polymers
  • Polymethacrylic Acids
  • Propylamines
  • SBA-16
  • Silanes
  • methylmethacrylate-methacrylic acid copolymer
  • Mesalamine
  • Eudragit RL
  • Silicon Dioxide
  • amino-propyl-triethoxysilane