Preparation, Characterization, and In Vitro Release of Chitosan-Ecabet Electrolyte Complex for the Mucosal Delivery.

Abstract

Ecabet has a mucosal protection and anti-Helicobacter pylori effect only by local action in the gastric mucous layer, due to an extremely poor absorption into the systemic blood circulation. The aim of the present work was to develop chitosan-ecabet electrolyte complex (ChE) for the enhanced mucosal drug delivery. ChEs were prepared with various ecabet-chitosan concentration ratios. Entrapment efficiency (%), sedimentation volume (%), transmission electron microscopy (TEM), FT-IR spectrum, and drug release were investigated. ChEs were prepared by the simple mixing method in a pH-adjusted solution based on the electrostatic interaction between the sulfonate (negatively charged) group from ecabet and the amine (positively charged) group from chitosan. Sedimentation volume and entrapment efficiency at the same concentration of ecabet sodium with that of chitosan resulted in 53.6% and 86.75%, respectively, suggesting a high degree of forming complex. In TEM images, the complex was approximately 200 nm in particle size and had loosely entangled particles. Forming complex of ChEs was supported by new bands appearance in the FT-IR spectrum. In the drug release study using dialysis membrane sac, ChEs showed a sustainable release up to 80% during 12 h as compared to ecabet sodium suspension at pH 1.2 medium. Based on the results of this work, ChE would be a promising drug delivery system for gastric mucosa.