Beta-glucan and arabinogalactan-based xerogels for abuse-deterrent opioid formulations

Eur J Pharm Sci. 2019 Mar 1:129:132-139. doi: 10.1016/j.ejps.2019.01.003. Epub 2019 Jan 6.

Abstract

Novel polysaccharide hydrogels based on Methocel and beta-glucan or arabinogalactan and corresponding xerogels were prepared and described. Phase stability of hydrogels was confirmed over multiple freeze-thaw cycles. Binary beta-glucan:Methocel hydrogels showed the highest freeze-thaw stability in terms of their syneresis. The viscosity of binary hydrogels was further increased by adding water-soluble resin. Freeze drying of polysaccharide gels yields xerogels suitable as abuse-deterrent vehicles for opioid delivery. The xerogels were characterized by infrared spectroscopy, X-ray diffraction, differential scanning calorimetry, scanning electron microscopy and by their swelling behavior. As a model opioid, tramadol hydrochloride formulations were prepared with various xerogel matrices and dissolution-release profiles were determined. The xerogel matrix acts as a functional excipient that forms a viscous gel barrier with decreased rate of tramadol release. Moreover, slower drug release with no dose dumping is observed in the presence of ethanol. The release kinetics demonstrated that hydrophilic gels with beta-glucan or arabinogalactan are effective for controlling and prolonging the drug release for 12 h which could reduce the required number of administrations.

Keywords: Drug abuse; Drug delivery; Opioids; Release kinetics; Xerogel.

MeSH terms

  • Analgesics, Opioid / chemistry*
  • Chemistry, Pharmaceutical / methods
  • Delayed-Action Preparations / chemistry
  • Drug Carriers / chemistry
  • Drug Liberation
  • Excipients / chemistry
  • Freeze Drying / methods
  • Freezing
  • Galactans / chemistry*
  • Hydrogels / chemistry*
  • Kinetics
  • Polysaccharides / chemistry
  • Viscosity
  • Water / chemistry
  • beta-Glucans / chemistry*

Substances

  • Analgesics, Opioid
  • Delayed-Action Preparations
  • Drug Carriers
  • Excipients
  • Galactans
  • Hydrogels
  • Polysaccharides
  • beta-Glucans
  • Water
  • arabinogalactan