Characterizing eutectic mixtures of gliclazide with succinic acid prepared by electrospray deposition and liquid assisted grinding methods

Abstract

As a new method for improving dissolution, we have utilized electrospray deposition (ESD) to integrate eutectic formation with nanosizing. Gliclazide (GCZ) was used as a poorly soluble drug and succinic acid (SUC) as a water soluble carrier. A binary phase diagram was developed for the GCZ-SUC system. Eutectic mixtures (EMs) were prepared by liquid assisted grinding (LAG-EM) and electrospray deposition (ESD-EM). The effects of solvent type and feed concentration were evaluated on the properties of electrosprayed samples. EMs were characterized by DSC, powder X-ray diffraction (PXRD), Fourier-transform infrared spectroscopy (FTIR), surface area measurement and scanning electron microscopy. Dissolution rates of ESD-EM and LAG-EM were compared with GCZ. In addition, dissolution properties of the samples were evaluated in the presence of excipients. GCZ-SUC was found to form an EM at GCZ mole fraction of 0.5. FTIR and PXRD analyses revealed the absence of a new crystalline phase between GCZ and SUC. ESD successfully was used for the preparation of EMs. In the presence of excipients, ESD-EM with a mean size of 296 nm showed a superior dissolution rate than GCZ and LAG-EM. ESD, owing to its simplicity and being continuous, possesses great potentials for preparation of eutectics with submicron sizes.