Formulation and optimization of Ambrisentan self-micro emulsifying drug delivery system (SMEDDS) tablet by wet granulation

Abstract

Ambrisentan is an orally administered endothelin receptor antagonists used for the treatment of pulmonary hypertension. As it is fall under BCS class 2 medicine, its solubility, stability and oral bio availability 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 Ambrisentan using minimized quantity of oil, surfactant and co-surfactant that could improve its solubility, stability, and dissolution. The composition of optimized formulation consists of Maisine CC as oil, Acrysol EL 135 as surfactant and Capryol PGMC as cosurfactant, containing 200 mg of Ambrisentan showing mean droplet size (155.12 nm), rate of self-emulsification (56 sec) and Polydispersibility index (0.331). This optimized liquid SMEDDS is used as a liquid component in wet granulation and prepare tablet of Ambrisentan having 5 mg strength. A prepared tablet is evaluated further for tablet evaluation tests and dissolution. This research results in good dissolution and stability.