Generation of high drug loading amorphous solid dispersions by Spray Drying

Abstract : Amorphous solid dispersions (ASDs) refers to drug - carrier systems, where the drug is dispersed in the carrier at a molecular level. In this work, ASDs were formulated by spray drying. The aim was to achieve high drug loads of an amorphous hydrophobic drug (Efavirenz - EFV) in the carrier Soluplus (R). Solid state characterizations (mDSC, XRPD, DVS, Raman, SEM, stability and solubility studies) were done. EFV amorphisation in ASDs (20 to 85% EFV loads) resulted in improved drug solubility compared to unprocessed EFV crystals and tendency of properties evolution over time for ASDs with EFV loads higher than 70 wt%.