Performance of magnetic chitosan-alginate core-shell beads for increasing the bioavailability of a low permeable drug

Eur J Pharm Biopharm. 2014 Oct;88(2):374-81. doi: 10.1016/j.ejpb.2014.05.017. Epub 2014 May 22.

Abstract

This work reports the synthesis and performance of magnetic chitosan-alginate core-shell beads for oral administration of small molecules in order to increase their bioavailability. For this purpose, we designed magnetic core-shell beads suitable for oral delivery that are resistant in acidic media (stomach pH), mucoadhesive, exhibit a superparamagnetic behavior and a very high entrapment efficiency. Ex vivo experiments were performed in Ussing chambers, to emphasize the effect of magnetic accumulation. The amount of drug permeated through the membrane exhibited a threefold increase with our novel drug delivery system. According to a correlation law, our ex vivo model showed that the adsorbed fraction (FA) in human is expected to reach 70% when using the magnetic retention system which is a great improvement when compared to the controls (FA=20%).

Keywords: Absorption; Alginate; Bioavailability; Chitosan; Drug delivery; Magnetic particles.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alginates / chemistry*
  • Animals
  • Biological Availability
  • Chitosan / chemistry*
  • Glucuronic Acid / chemistry
  • Hexuronic Acids / chemistry
  • Humans
  • Magnetics*
  • Male
  • Microscopy, Electron, Scanning
  • Permeability
  • Pharmacokinetics*
  • Rats
  • Rats, Wistar

Substances

  • Alginates
  • Hexuronic Acids
  • Glucuronic Acid
  • Chitosan