Physical stabilization of amorphous itraconazole in solid dispersions for improved dissolution profile.

The main objective of the present investigation was to improve dissolution efficiency and stabilize amorphous form of itraconazole (ITR) through formulation of ternary solid dispersion system (SDs) with polyvinylpyrrolidone K30 (PVP K30) and sylysia®350 using spray drying technique. The prepared ternary SD system was characterized for solid state properties, in vitro dissolution efficiency and accelerated stability study at 40 °C/75% RH for the period of 3 months to explore extent of stabilization of amorphous itraconazole (AITR). Surprisingly, AITR was found to have no significant improvement in its dissolution characteristics compared to pure drug. The formation of cohesive supercooled liquid state might be the reason for poor solubility. Hence a combined approach of SD system with an antiplasticizing agent and surface adsorption technique was employed to prevail over functional inabilities of AITR. The binary and ternary SDs of AITR were prepared employing PVP K30 as antiplasticizer and/or sylysia®350 as adsorbent in the ratio 1:1:1 w/w using spray drying technique. The prepared systems have shown significant improvement in dissolution characteristics when compared to pure drug. Accelerated stability studies confirmed the absence of crystallization events over a period of 3 months endorsing excellent stabilization of AITR.

Physicochemical characterization of spray dried cefixime polymeric nanoparticles using factorial design approach.

The objective of the present study was to improve the physicochemical properties of poorly water soluble cefixime by preparing its nanoparticles using a hydrophilic polymer polyvinylpyrrolidone K30 (PVP). The nanoparticles of cefixime were prepared by spray drying technique. A 32 factorial design approach was employed for the optimization of nanoparticle batches. The present model demonstrated significance of factors such as drug to polymer ratio (X1) and feed flow rate (X2) of spray dryer on the production yield (Y1), particle size (Y2) and % drug release at 15 min (Y3). The pure drug and prepared nanoparticles were characterized by Fourier transformation infrared spectroscopy (FTIR), Differential scanning calorimetry (DSC), X-ray powder diffraction (XPRD), Scanning electron microscopy (SEM), particle size, saturation solubility and in vitro drug release. The results of DSC and XPRD revealed transformation of the crystalline nature of cefixime into an amorphous form which was supported by SEM. A significant improvement in solubility and dissolution rate was noticed in case of prepared nanoparticles as compared to pure cefixime. These results suggested that preparation of polymeric nanoparticles by spray drying technique might be a promising approach for improving the physicochemical properties of cefixime.