Solidification of carvedilol loaded SEDDS by high-shear granulation

Carvedilol (CRV) is a BCS class II drug with low oral bioavailability. Self-emulsifying drug delivery systems (SEDDS) have been proposed to increase CRV bioavailability; however, liquid SEDDS often show stability problems. This study aimed to investigate the effects of the substrate type (microcrystalline cellulose, lactose and aerosil) and process factors (chopper and impeller speed) on the properties of solid SEDDS prepared by high-shear granulation. Angle of repose, Carr and Hausner indexes, droplet size and polydispersity index were studied. After dilution, emulsion droplets showed a uniform size distribution (177.9 nm average size and 0.219 PdI), whereas solid SEDDS showed a polydisperse size distribution after reconstitution. Flow properties and size distribution of the reconstituted droplets were affected by formulation and process factors. Therefore, the quality of the solid-SEDDS prepared by high-shear granulation depends on the proper selection of formulation and process factors.