Formulation development and solubility enhancement of voriconazole by solid dispersion technique

Abstract

The objective of the present investigation was to formulation development of solid dispersion of voriconazole using hot-melt, solvent evaporation and combination of these two methods together with Gelucire® 44/14, polaxamer 188 and polyvinyl pyrrolidone (PVP) K30 and the different characteristics like drug content analysis and in vitro release of the solid dispersions were investigated. The drug-carriers compatibility of the solid dispersions were investigated by Fourier transform infra-red spectroscopy (FTIR) and differential scanning calorimetry (DSC) study and crystal characteristic of solid dispersions were evaluated by X-ray diffraction (XRD) study. The in vitro release study revealed that among all the physical mixtures and solid dispersions prepared by using different carriers, solid dispersions that contained Gelucire® 44/14 and Poloxamer 188 as carrier in the ratio of 1:5 (voriconazole: carrier) were released voriconazole in simulated gastric fluid within short period of time. The FTIR spectrum and DSC thermograms indicated the compatibility of drug and carriers. The diffusion exponent (n) determined from in vitro release data of solid dispersions FCG5 and FCP5 were found 0.391 and 0.325, respectively, indicating Fickian drug release mechanism.