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

• Published in: European journal of pharmaceutics and biopharmaceutics Vol. 88; no. 2; pp. 374 - 381
• Main Authors: Seth, Anjali, Lafargue, David, Poirier, Cécile, Péan, Jean-Manuel, Ménager, Christine
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 01.10.2014
• Subjects: Absorption; Alginate; Alginates - chemistry; Animals; Bioavailability; Biological Availability; Chitosan; Chitosan - chemistry; Drug delivery; Glucuronic Acid - chemistry; Hexuronic Acids - chemistry; Humans; Magnetic particles; Magnetics; Male; Microscopy, Electron, Scanning; Permeability; Pharmacokinetics; Rats; Rats, Wistar; Magnetic particles; Alginate; Drug delivery; Absorption; Bioavailability; Chitosan
• ISSN: 0939-6411; 1873-3441
• DOI: 10.1016/j.ejpb.2014.05.017

[Display omitted] •Magnetic chitosan–alginate core–shell beads were designed for oral administration.•Magnetic retention increases low permeable drug absorption.•The adsorbed fraction in human is expected to reach 70% thanks to a correlation low. 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%).