Polymeric Permeation Enhancers

Chapter

Abstract

There are enough low molecular permeation enhancers available to increase the absorption of hydrophilic drugs, but all of them have the disadvantage of strongly interfering with the phospholipid membranes and of damaging them. Polymeric permeation enhancers are a class of substances which are able to selectively trigger mechanisms to selectively open the watery channels of the tight junctions which allow the passage of hydrophilic drugs alongside the enterocytes. As these polymeric permeation enhancers are hydrophilic polymeric substances they are generally not absorbed and hence show basically no toxicity. They specifically act, e.g. by binding calcium ions (polyacrylates) and the reversible opening of the tight junctions is triggered. Others – like the chitosans and their quaternary analogues like trimethyl chitosan (TMC) – specifically interact with their positive charges of sialic acid or sulphuric acid of the mucosal linings to induce the same effect. As all the polymeric permeation enhancers have to show mucoadhesivity in order to be effective, their residence time on the mucosal surface is increased. This effect is even strongly increased when thiolated polymeric permeation enhancers are used, which are able to even further increase the mucus residence time of the permeation enhancer. Whereas delivery systems containing polymeric permeation enhancers for application at directly accessible mucous membranes are feasible the peroral application is still a challenge.

Keywords

Permeability Toxicity Oligomer Sodium Hydroxide Luminal 

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Copyright information

© Springer Science+Business Media, LLC 2009

Authors and Affiliations

  1. 1.Department of Pharmaceutics, Faculty of Pharmaceutical SciencesNaresuan UniversityPhitsanulokThailand

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