Capmul MCM/Solutol HS15-based microemulsion for enhanced oral bioavailability of Rebamipide

Abstract

Rebamipide (RBP) is a potent anti-ulcer and anti-oxidative agent, which is a BCS class IV drug with a low oral bioavailability of less than 10%. Thus, the systemic absorption of RBP into the blood circulation is an essential prerequisite for exerting its pharmacological activities after oral dosing. Herein, we report on microemulsion (ME) systems for the enhancement of oral RBP bioavailability. In this study, MEs consisting of Capmul MCM (oil), Solutol HS15 (surfactant), and ethanol (co-surfactant) were prepared by the construction of pseudo-ternary phase diagram. The RBP-loaded MEs had spherical nano-sized droplets with narrow size distribution and neutral zeta potential. Moreover, the prepared MEs significantly enhanced the dissolution and oral bioavailability of RBP with no discernible intestinal toxicity. These results suggest that the present ME system could be further developed as an alternative oral formulation for RBP.