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. 2007 Jun 15;8(2):E110–E118. doi: 10.1208/pt0802044

Effect of oppositely charged polymer and dissolution medium on swelling, erosion, and drug release from chitosan matrices

Kiran S Bhise 1, Ravindra S Dhumal 1, Bhaskar Chauhan 1, Anant Paradkar 1,✉, Shivajirao S Kadam 1
PMCID: PMC2750359  PMID: 17622119

Abstract

The purpose of this research was to investigate the potential use of anionick-carrageenan and nonionic hydroxypropyl-methylcellulose (HPMC, K4) to improve the matrix integrity of directly compressed chitosan tablets containing naproxen sodium, an anionic drug. The influence of buffer pH and drug:polymer ratio on the water uptake, matrix erosion, and drug release were studied. The rapid release of naproxen sodium was seen from matrices containing 100% chitosan due to loss in the matrix cohesiveness; whereas, it was relatively slow for matrices containing optimum concentration ofk-carrageenan. In-situ interaction between oppositely charged moieties resulted in the formation of polyelectrolyte complexes with stoichiometric charge ratios of unity. Fourier transform in frared (FTIR) spectroscopy and powder x-ray diffraction (PXRD) data confirmed the importance of ionic bonds in polyelectrolyte complexation. The ionic interactions between polymers were absent in matrices containing HPMC and the integrity of tablets was improved owing to the presence of viscous gel barrier.

The reasons for retarded release of naproxen sodium from the chitosan matrices at different pH include poor aqueous solubility of drug, the formation of a rate-limiting polymer gel barrier along the periphery of matrices, the interaction of naproxen sodium with protonated amino, groups of chitosan, and the interaction of ionized amino groups of chitosan with ionized sulfate groups ofk-carrageenan.

Keywords: Charged polymers, naproxen sodium, insitu complexation, sustained release matrices, chitosan, k-carrageenan

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