Quality by design enabled formulation optimization of rabeprazole sodium mucoadhesive microcapsules for the treatment of gastroesophageal reflux disease

Abstract

The present research describes the implementation of quality by-design principles for developing the mucoadhesive microcapsules of rabeprazole sodium for treating gastroesophageal reflux disease conditions. In addition, a holistic QbD-based product development strategy was implemented, where the target product profile was defined based on desired product quality of mucoadhesive microcapsules. Based on TPP, the critical quality attributes were identified. The identification of CMAs was carried out with the help of risk assessment and factor screening exercises, which indicated drug-polymer ratio (X1), temperature (X2), and stirring speed (X3) as the influential factors. The mucoadhesive microcapsules of rabeprazole sodium were prepared by a solvent evaporation method, and 33 Box-Behnken optimization design was used for the optimization of the selected factors, and mucoadhesive microcapsules formulations were evaluated for particle size (µm), drug entrapment efficiency (%), mucoadhesion (%), and in vitro drug release (Q18h) in percentage characteristics. Mathematical data analysis was performed to fit the two-factor interaction model, and optimized mucoadhesive microcapsules formulation was selected. The optimized mucoadhesive microcapsules indicated desired formulation characteristics with smaller particle size, good entrapment efficiency, better mucoadhesion, and sustained drug release characteristics. In a nutshell, the studies vouch for the successful development of mucoadhesive microcapsules for oral delivery of rabeprazole sodium which could be used to manage gastroesophageal reflux disease condition.