Preparation of nanoparticles of poorly water soluble dronedarone by antisolvent addition technique using natural polymer as a stabilizer.

Department of Pharmaceutics, JSPM’s Rajarshi Shahu College of Pharmacy and Research, Tathawade, Pune411033, Maharashtra, India. ABSTARCT The aim of this study was to enhance the solubility, dissolution rate and bioavailability of poorly water soluble drug Dronedarone (DRO) by preparing nanoparticles with antisolvent precipitation process. In this Caesalpinia pulcherrima gum (CPG) was used as a stabilizer. The influence of operation parameter such as solvent to antisolvent ratio, stirring speed, stabilizer concentration was experimentally investigated. The results indicated that increasing solvent to antisolvent ratio, stirring speed, stabilizer concentration affected the particle size. The prepared nanoparticles of DRO were characterized by scanning electron microscopy (SEM), Fourier transform Infrared(FT-IR) spectroscopy, differential scanning calorimetry (DSC), Xray diffraction(XRD), in vitro drug release and in vivo study in suitable animal model. The SEM image exhibited some aggregation of individual nanoparticles, FT-IR analysis confirmed that molecular structure of nanoparticles of DRO and observed no change after precipitation. The DSC and XRD indicate that crystallinity of DRO nanoparticles which was lower than the pure drug. The dissolution of DRO nanoparticles in pH 4.5 phosphate buffer was faster than pure drug in 15 min. These nanoparticles showed dramatically increase oral bioavailability in wistar rat. Nanoparticles of dronedarone prepared by antisolvent precipitation technique proved to be effective in improving oral bioavailability as a result of enhanced solubility and dissolution rate.