Preparation and characterisation of gastroretentive alginate beads for targeting H. pylori

J Microencapsul. 2014;31(1):58-67. doi: 10.3109/02652048.2013.805840. Epub 2013 Jun 24.

Abstract

There are various obstacles in the eradication of Helicobacter pylori (H. pylori) infections including low drug levels due to short gastric residence times and poor accessibility of the drug at the site of the infection. In this study, calcium alginate beads containing metronidazole were prepared by ionotropic gelation with diameters ranging from 2 to 3 mm and bulk densities ranging from 0.11 to 0.23 g/cm(3). These beads failed buoyancy tests and released the drug rapidly. The formulation was modified in order to improve floating and modify their drug release profile through addition of oil and coating with chitosan. Upon modification, buoyancy improved and drug release was sustained. This novel formulation will ensure retention for a longer period in the stomach and control the release of drug, ensuring high local drug concentrations, leading to improved eradication of the bacteria.

MeSH terms

  • Alginates* / chemistry
  • Alginates* / pharmacology
  • Delayed-Action Preparations / chemistry
  • Delayed-Action Preparations / pharmacology
  • Drug Carriers / chemistry*
  • Drug Carriers / pharmacology*
  • Glucuronic Acid / chemistry
  • Glucuronic Acid / pharmacology
  • Helicobacter Infections / drug therapy*
  • Helicobacter pylori*
  • Hexuronic Acids / chemistry
  • Hexuronic Acids / pharmacology

Substances

  • Alginates
  • Delayed-Action Preparations
  • Drug Carriers
  • Hexuronic Acids
  • Glucuronic Acid