N,N-Dimethyl chitosan/heparin polyelectrolyte complex vehicle for efficient heparin delivery

Int J Biol Macromol. 2015 Apr:75:186-91. doi: 10.1016/j.ijbiomac.2015.01.030. Epub 2015 Jan 24.

Abstract

Polysaccharide-based device for oral delivery of heparin (HP) was successfully prepared. Previously synthesized N,N-dimethyl chitosan (DMC) (86% dimethylated by (1)H NMR spectroscopy) was complexed with HP by mixing HP and DMC aqueous solutions (both at pH 3.0). The polyelectrolyte complex (PEC) obtention was confirmed by infrared spectroscopy (FTIR), thermogravimetric analysis (TGA/DTG) and wide-angle X-ray scattering (WAXS). In vitro controlled release assays of HP from PEC were investigated in the simulated intestinal fluid (SIF) and simulated gastric fluid (SGF). The PEC efficiently protected the HP in SGF condition in which HP is degraded. On the other hand, in SIF PEC promoted the releasing of 80 ± 1.5% of loaded HP. The promissory results indicated that the PEC based on DMC/HP presented potential as drug-carrier matrix, since biological activity of HP was improved at pH close to physiological condition.

Keywords: Heparin; N,N-Dimethyl chitosan; Polyelectrolyte complex.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Body Fluids / chemistry
  • Chitosan / analogs & derivatives*
  • Chitosan / chemical synthesis
  • Chitosan / chemistry*
  • Drug Carriers / chemistry*
  • Drug Delivery Systems*
  • Electrolytes / chemistry*
  • Heparin / chemistry*
  • Heparin / pharmacology*
  • Models, Theoretical
  • Proton Magnetic Resonance Spectroscopy
  • Spectroscopy, Fourier Transform Infrared
  • Thermogravimetry
  • X-Ray Diffraction

Substances

  • Drug Carriers
  • Electrolytes
  • N,N-dimethyl chitosan
  • Heparin
  • Chitosan