Characterization of muco- and bioadhesive properties of chitosan, PVP, and chitosan/PVP blends and release of amoxicillin from alginate beads coated with chitosan/PVP

Drug Dev Ind Pharm. 2011 Apr;37(4):408-18. doi: 10.3109/03639045.2010.518149.

Abstract

Purpose: To investigate the muco/bioadhesive properties of chitosan, polyvinylpyrrolidone (PVP), and chitosan/PVP blends and the release of amoxicillin (AMX) contained in AMX-alginate beads coated with these materials.

Method: Chitosan, PVP, and chitosan/PVP blends at various volume ratios were coated onto calcium alginate beads containing AMX. The muco/bioadhesive properties of all materials and the AMX-alginate beads coated with these materials were characterized.

Results: Measurements of their viscosity, texture, and adhesion to HT29 cells demonstrated that chitosan/PVP at a volume ratio of 5/5 had the best muco/bioadhesive properties when compared with chitosan, PVP, and blends of other ratios. Wash-off tests indicated that the mucoadhesive property of the coated AMX-alginate beads was significantly higher than that of the uncoated beads. Diffuse reflectance infrared Fourier transform spectroscopy showed that there were interactions between chitosan-PVP, chitosan-mucin, PVP-mucin, and chitosan/PVP blend-mucin. Scanning electron microscopy revealed that the surfaces of the coated beads were smoother than those of the uncoated beads. All coated AMX-alginate beads were able to provide a controlled release of AMX with Super Case II transport properties, at a pH of 4. This was probably a result of the rapid and extensive swelling of the alginate beads. The more rapid release of AMX at pH 1 was probably because of the rapid dissolution of the drug at this pH.

Conclusions: From the controlled drug release and muco/bioadhesive properties of these coated AMX-alginate beads, we suggest that the alginate-coated beads might be a promising drug delivery system to assist with the eradication of Helicobacter pylori infections.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alginates / administration & dosage*
  • Amoxicillin / administration & dosage*
  • Amoxicillin / chemistry
  • Anti-Bacterial Agents / administration & dosage*
  • Cell Adhesion / drug effects
  • Chitosan / administration & dosage*
  • Glucuronic Acid / administration & dosage
  • HT29 Cells
  • Hexuronic Acids / administration & dosage
  • Humans
  • Povidone / administration & dosage*
  • Solubility
  • Viscosity

Substances

  • Alginates
  • Anti-Bacterial Agents
  • Hexuronic Acids
  • Amoxicillin
  • Glucuronic Acid
  • Chitosan
  • Povidone