Abstract

Chitosan has been the subject of interest for its use as a polymeric drug carrier material in dosage form design due to its appealing properties such as biocompatibility, biodegradability, low toxicity and relatively low production cost from abundant natural sources. However, one drawback of using this natural polysaccharide in modified release dosage forms for oral administration is its fast dissolution rate in the stomach. Since chitosan is positively charged at low pH values (below its pKa value), it spontaneously associates with negatively charged polyions in solution to form polyelectrolyte complexes. These chitosan based polyelectrolyte complexes exhibit favourable physicochemical properties with preservation of chitosan’s biocompatible characteristics. These complexes are therefore good candidate excipient materials for the design of different types of dosage forms. It is the aim of this review to describe complexation of chitosan with selected natural and synthetic polyanions and to indicate some of the factors that influence the formation and stability of these polyelectrolyte complexes. Furthermore, recent investigations into the use of these complexes as excipients in drug delivery systems such as nano- and microparticles, beads, fibers, sponges and matrix type tablets are briefly described.

Highlights

  • Mixing oppositely charged polyelectrolytes in solution will result in their self assembly or spontaneous association due to the formation of strong, but reversible electrostatic links

  • This review focuses on polyelectrolyte complexes formed between chitosan and selected natural and synthetic polyanions that have been investigated as excipients in modified release drug delivery systems such as matrix type tablets, beads, sponges, microparticles or nanoparticles for different routes of administration

  • A comparison of matrix type tablets made of the polyelectrolyte complexes formed between chitosan and alginate and those formed between chitosan and carrageenan showed that the former was better in prolonging diltiazem release at lower concentration of the polymers [28]

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Summary

Introduction

Mixing oppositely charged polyelectrolytes in solution will result in their self assembly or spontaneous association due to the formation of strong, but reversible electrostatic links These direct interactions between the polymeric chains lead to the formation of polyelectrolyte complex networks with non-permanent structures while avoiding the use of covalent cross-linkers. Three dimensional polymeric networks or complexes prepared by non-covalent strategies rely on electrostatic, hydrophobic and/or hydrogen bonding forces between the polymeric chains rather than chemical bonds These inter-polymer chain interactions are physical in nature and reversible but can provide the required properties for optimal drug delivery if the correct polymers are combined [5,11,12]. This review focuses on polyelectrolyte complexes formed between chitosan and selected natural and synthetic polyanions that have been investigated as excipients in modified release drug delivery systems such as matrix type tablets, beads, sponges, microparticles or nanoparticles for different routes of administration

Polyelectrolyte Complexes between Chitosan and Natural Polymers
Chitosan-alginate polyelectrolyte complex
Chitosan-carrageenan polyelectrolyte complex
Chitosan-pectin polyelectrolyte complex
Chitosan-xanthan gum polyelectrolyte complex
Chitosan-hyaluronic acid polyelectrolyte complex
Chitosan-gum kondagogu polyelectrolyte complex
Chitosan-gelatine polyelectrolyte complex
Chitosan-maleic starch half-ester acid polyelectrolyte complex
Polyelectrolyte Complexes between Chitosan and Synthetic Polymers
Chitosan-polyalkylenoxide-maleic acid polyelectrolyte complex
Findings
Conclusions
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