Self-Nanoemulsifying Drug Delivery System Combined with a Polymeric Amorphous System of Glibenclamide for Enhanced...

Self-nanoemulsifying drug delivery systems (SNEDDS) have been widely applied to improve the dissolution and bioavailability of hydrophobic medications like glibenclamide (GB). However, the acid liability of GB limits its loading in SNEDDS formulation owing to the expected drug degradation. The present study investigated the ability of a polymeric amorphous system (PAS) to amorphize raw GB and facilitate its integration within dispersed SNEDDS. Liquid-SNEDDS (L-SNEDDS), solid-SNEDDS (S-SNEDDS), and combined systems (SNEDDS + PAS) were prepared for this purpose. The physicochemical properties of the prepared formulations were examined using a zeta-sizer, SEM, DSC, PXRD, and dissolution apparatus. In addition, GB integrity within formulations following incubation in a stability chamber was also investigated. The prepared formulations were able to be dispersed within the nanosize range. SEM, DSC, and PXRD showed that freeze-drying (FD) was superior to the microwave (MW) method in GB amorphization. Even though L-SNEDDS and S-SNEDDS were able to increase the dissolution efficiency (DE) of GB, drug degradation was observed. However, PAS prepared using FD was able to increase the DE of GB from 2.5% to 84.2% and protect the drug from chemical degradation. The present study revealed that a combined system (SNEDDS + PAS) is a promising approach to enhance the stability of acid-labile drugs and facilitate the integration of amorphous drugs within a dispersed SNEDDS formulation.