Interaction between Eudragit® E100 and anionic drugs: addition of anionic polyelectrolytes and their influence on drug release performance

Abstract

In this work, we report results concerning the study of solid complexes compounded by a cationic polymethacrylate (Eudragit® E100, Eu) and mesalazine (M) (Eu-M(x) complex). The influence of an anionic polyacrylic acid polymer (carbomer, C) on dissolution behavior of M from the complex was evaluated (Eu-M(x) C(y) complex). The dissolution profiles and solvent front movements of solid matrices in different media (water, buffer pH 7.4, 0.9% NaCl) were investigated and ionic interactions among Eu, M, and C were determined through Fourier transform infrared (FT-IR) spectroscopy. For Eu-M(x) complexes, the affinity between M and Eu modulated the delivery of free M in solution, with the dissolution media affecting the delivery rate mainly due to an ionic interchange process between M and anionic electrolytes (i.e., Cl(-)). FTIR spectroscopy allowed the ionic interaction between Eu and M to be verified. The addition of C (Eu-M(x) C(y) ) influenced the dissolution behavior of these matrices. As the amount of C was increased, the release mechanism changed from diffusion (Eu-M(50) ) or anomalous (Eu-M(100)) to zero order (Eu-M(x) C(50)). This variation in rate delivery was also affected by the dissolution media, as occurred with Eu-M(x) complexes. The formation of the gel layer during the dissolution process, as consequence of Eu-M(x) C(y) matrices hydration, was influenced by C amount and dissolution media.