Formulation, Optimization and Evaluation of Solid SMEDDS of Itraconazole in Effervescent Granules Form

Abstract

This investigation assessed nine formulations of liquid self-micro-emulsifying drug delivery systems (L-SMEDDS) for itraconazole (ITZ). The most effective formulation (ILS6) consisted of 40% clove as the oil, 40% Kolliphor CS 20 as the surfactant, and 20% polyethylene glycol (PEG) 400 as the co-surfactant. ILS6 displayed a droplet size of 130 to 165 nm, well below 200 nm, and a polydispersity index (PDI) value of 0.47 to 0.73, indicating the development of an emulsion with nanosized droplets and even spreading. The finalized formulation demonstrated stability under numerous conditions and achieved supreme drug loading capacity. The optimized L-SMEDDS was solidified into solidified SMEDDS (S-SMEDDS) utilizing sylloid 244 FP, resulting in a free-flowing powder without drug interactions. The effervescent system was successfully formulated by incorporating S-SMEDDS with different excipients. The selected effervescent system passed quality control and stability tests. The effervescent system exhibited a rapid and pH-independent release profile. The combined impact of SMEDDS and the effervescent system collectively enhanced the solubility and dissolution of itraconazole.