Solid self-emulsifying drug delivery system for artemether with improved physicochemical properties: design and characterization

Background: The oral delivery of hydrophobic drugs presents a major challenge because of the low aqueous solubility of such compounds.

Objectives: The purpose of this study was to formulate artemether self-emulsifying drug delivery system (SEDDS) with natural oil from sesame seeds as one of the lipidic component, transform it into powder and evaluate its potential in improving the release rate of artemether, a hydrophobic drug.

Methods: A self-emulsifying formulation of artemether composed of oil, surfactant, and co-surfactant was formulated and characterized with respect to globule size, polydispersity index (PDI), emulsification time, ® ingredients compatibility and stability. The formulation was converted to powder by adsorption on Aerosil , evaluated for flow and surface morphology using a scanning electron microscope. The formulation in vitro drug release was determined and compared with a marketed product.

Results: The formulation was stable, showed excellent emulsification time of 6.0 s, had a mean globule size of ® w 33.59 nm and PDI of 0.182. Direct incorporation of artemether-SEDDS into Aerosil at a ratio of 2:1/w (artemether- ® SEDDS: Aerosil ) resulted in a dry powder with good flow according to the Carr's scale, with a mean particle size of 268.33µm, which were mostly spherical, with highly rough and porous surfaces. At 30 min, the marketed formulation released 46 % drug lower than the solidify artemether-SEDDS

Conclusion: The study substantiates the usefulness of SEDDS for overcoming some of the physicochemical challenges associated with the delivery of artemether.