Ziprasidone nanocrystals by wet media milling followed by spray drying and lyophilization: Formulation and process parameter optimization

The aim of work was to prepare and characterize Ziprasidone nanosuspension to achieve enhance solubility and in vitro dissolution. The media milling technique was utilized for production of nanosuspension and the effect of amount of milling agent, milling time, volume of water, stirring speed and type of stabilizers on particle size and size distribution was studied. The optimized nanosuspension was subjected to spray drying and lyophilization which than characterized for fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), in vitro dissolution study, X-ray diffraction (XRD) and field emission scanning electron microscopy (FE-SEM). FTIR and DSC studies showed compatibility of Ziprasidone with selected excipients. DSC study also revealed that crystalline form of Ziprasidone in spray dried and lyophilized nanosuspension was remained same as to that of pure Ziprasidone. XRD of spray dried and lyophilized nanosuspension showed same diffraction pattern as that of the pure Ziprasidone only crystallinity was decreased. Around 8 fold increase in saturation solubility was observed. In vitro dissolution of spray dried and lyophilized nanosuspension was significantly higher. The rod like nanocrystals were observed in FE-SEM studies which were present on surface of sphere in spray dried nanosuspension and dispersed in matrix like structure in lyophilized nanosuspension.

187