A considerable portion (40%) of drugs fail full development, because of Poor water solubility of drug molecules, insufficient bioavailability, fluctuating plasma levels and high food dependency. Itraconazole is one of such agent, a poorly water soluble drug indicates insufficient bioavailability following oral administration. The purpose of the present study was to formulate and optimize Itraconazole nanosuspension. In the present work Itraconazole nanosuspension was prepared by pearl milling technique using zirconium oxide beads as a milling media. A series of polymers and surfactants were screened and finally HPC-EF as a polymer and SDS were finalized. To optimize formulation parameters, 33 factorial design was adopted. Effects of various process parameters like, stirring time and the ratio of the beads were optimized using final formulation. The optimized nanosuspension was lyophilized using mannitol (1:1 ratio) as a cryoprotectant. Nanosuspension was characterized by particle size and size distribution, drug content, scanning electron microscopy, differential scanning colorimetry and its dissolution profile was compared with marketed product. Optimized nanosuspension showed spherical shape with surface oriented surfactant molecules and a mean particle diameter of 302 nm. There was no significant change in crystalline nature after formulation and it was found to be chemically stable with high drug content.The in vitro dissolution profile of the optimized formulation compared to the pure drug and marketed formulation (Canditral Capsule) by using 0.1N Hydrochloric acid as release medium showed higher drug release.\r\nKeywords: Nanosuspension, Itraconazole, Pearl milling technique, optimization
Loading....