Study of Different Chitosan/Sodium Carboxymethyl Cellulose Proportions in the Development of Polyelectrolyte Complexes for the Sustained Release of Clarithromycin from Matrix Tablets.

Víctor Guarnizo-Herrero,Norma Sofía Torres Pabón,Santiago Torrado-Santiago,Javier Morales,Guillermo Torrado Durán,Carlos Torrado-Salmerón

doi:10.3390/polym13162813

Víctor Guarnizo-Herrero, Norma Sofía Torres Pabón + Show 4 more

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https://doi.org/10.3390/polym13162813

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Abstract

This study investigated the combination of different proportions of cationic chitosan and anionic carboxymethyl cellulose (CMC) for the development of polyelectrolyte complexes to be used as a carrier in a sustained-release system. Analysis via scanning electron microscopy (SEM) Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and powder X-ray diffraction (PXRD) confirmed ionic interactions occur between the chitosan and carboxymethyl cellulose chains, which increases drug entrapment. The results of the dissolution study in acetate buffer (pH 4.2) showed significant increases in the kinetic profiles of clarithromycin for low proportions of chitosan/carboxymethyl cellulose tablets, while the tablets containing only chitosan had high relaxation of chitosan chains and disintegrated rapidly. The Korsmeyer–Peppas kinetic model for the different interpolymer complexes demonstrated that the clarithromycin transport mechanism was controlled by Fickian diffusion. These results suggest that the matrix tablets with different proportions of chitosan/carboxymethyl cellulose enhanced the ionic interaction and enabled the prolonged release of clarithromycin.

Highlights

Sustained-release systems prolong the time taken for a drug to reach maximum plasma concentrations, allowing for a reduced frequency of dosage, and they are associated with decreased adverse side effects and good safety profiles
Intermolecular CS/carboxymethyl cellulose (CMC) ionic interactions were observed via scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and Powder X-ray Diffraction (PXRD)
According to SEM morphological studies, the different polyelectrolyte complexes (PECs) tablets with CS/CMC exhibited changes in the density of their porous structures, which are related to the gel layer formed in the dissolution medium

Summary

Introduction

Sustained-release systems prolong the time taken for a drug to reach maximum plasma concentrations, allowing for a reduced frequency of dosage, and they are associated with decreased adverse side effects and good safety profiles. Since the development of polyelectrolyte complexes (PECs), there has been growing interest in their use in the control and modulation of drug release from hydrogel matrices. Electrostatic attractions between the ionized amino (NH3 + ) group of chitosan and the carboxylic (COO− ) groups of the anionic polymer are the main interactions in the formation of polyelectrolyte hydrogels with a high swelling ratio in the dissolution medium [1,2]. Chitosan (CS) is the most widely used cationic polymer; it has good biocompatibility and is nontoxic and biodegradable [3]. Its molecular weight control and degree of deacetylation allow its use in PECs for the sustained release of drugs [4,5]

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