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.