Development and Optimization of Macitenan Loaded Self-Micro Emulsifying Tablets

Abstract

Macitentan is an orally administered endothelin receptor antagonists used for the treatment of pulmonary arterial hypertension. As it is fall under BCS class 2 medicine, its solubility and oral bioavailability are poor. Here, a self micro-emulsifying drug delivery system (SMEDDS) was developed to improve its solubility and drug dissolution. The objective of our investigation was to formulate a self micro-emulsifying drug delivery system (SMEDDS) of Macitentan using minimized quantity of oil, surfactant and co-surfactant that could improve its solubility, stability, and dissolution. The composition of optimized Liquid SMEDDS formulation by BBD, consists of Capmul PG 8® as oil, Acrysol EL135® as surfactant and Propylene Glycol as cosurfactant, containing 100 mg of Macitentan showing mean droplet size (140.52 nm), rate of self-emulsification (53 sec) and Polydispersibility index (0.394). This optimized liquid SMEDDS is converted into the tablet dosage form using solid carrier technique. Macitentan SMEDDS tablet is optimized by 32 factorial designs, has desired hardness, disintegration time and dissolution rate more than 95% within 30 min.