A Study of Compressibility, Compactability and Mucoadhesivity of Tableting Materials for Matrix Systems Based on Chitosan.

Jitka Muzikova,Juraj Martiska,Andrea Veris,Eva Snejdrova,Bara Doubkova

doi:10.3390/polym13213636

Abstract

The objective of the present research is to evaluate directly compressible chitosan-based tableting materials for the formulation of mucoadhesive matrix tablets intended for targeted drug release to distal segments of the GIT. The influence of sodium alginate, hypromellose, and silicified microcrystalline cellulose (P90) on compressibility, compactability and lubricant sensitivity ratio was tested. Furthermore, the rheological properties of the hydrated surface layer of the matrix tablets and the mucoadhesion to a mucin substrate were analysed. Compressibility was evaluated using the energy profile of the compression process, compactability by means of the tensile strength of tablets, and lubricant sensitivity ratio was calculated to assess the sensitivity to lubricant. Addition of P90 to chitosan improved compressibility, which is demonstrated by the increase in the energy of plastic deformation and the higher tensile strength of tablets. P90 also significantly reduced the high lubricant sensitivity of chitosan. Presence of retarding components led to a decrease in Emax. All tested matrix tablets revealed a good mucoadhesion without a negative effect of P90 content. The viscosity of a gel layer on the surface of matrix tablets containing hypromellose was higher compared to those with sodium alginate. This was not reflected in the adhesive strength of the tablets. The formulated tableting materials combining chitosan and P90 are a suitable matrix for incorporation of an active ingredient, whose delayed release in the intestine can be achieved by the functionality of the chitosan-sodium alginate complex.

Highlights

Natural polysaccharides and their analogues are substances with a great potential for use in the pharmaceutical industry
The directly compressible chitosan-based tableting materials for the formulation of mucoadhesive matrix tablets intended for targeted drug release to the distal segments of the GIT were formulated and evaluated
The results showed that the addition of silicificated microcrystalline cellulose to chitosan improves the compressibility by increasing the energy of plastic deformation responsible for the formation of bonds and their strength

Summary

Introduction

Natural polysaccharides and their analogues are substances with a great potential for use in the pharmaceutical industry. In solid dosage forms they have been employed as excipients in the delivery systems with a modified release With these oral systems, a targeted release of the active ingredient in the distal segment of the gastrointestinal tract can be achieved [1,2,3,4,5,6]. Chemically (1→4)—2 amino-2-deoxy-β-D-glucan, ranks among cation-active polysaccharides and it is a linear copolymer composed of acetylated and deacetylated units connected with β-(1→4) glycosidic bonds [10,11,12,13]. It is obtained by deacetylation of chitin, its abundant natural resource. This mechanism of action has been successfully used to achieve the targeted release of the active ingredient in the distal segment of the GIT [16,17]

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Methods

Conclusion