Itraconazole nanosuspension meant for oral use: Development of formulation, characterization and in vitro comparison with some marketed formulations 

By Shivanand Pandey

Abstract

Itraconazole was formulated in a nanosuspension to increase the aqueous solubility and to improve its formulation related parameters, dissolution and hence oral bioavailability. Itraconazole Nanosuspension was prepared by pearl milling technique using zirconium oxide beads as a milling media, Poloxamer 407 as a stabilizer and Gycerol as a wetting agent. Effect of various process parameters like, stirring time and ratio of the beads were optimized by keeping Drug:surfactant:milling media (1:3.0:50) as a constant initially then optimized process parameters were used to optimize formulation parameters by 32 factorial designs. The optimized nanosuspension was lyophilized using mannitol (1:1 ratio) as a cryoprotectant. Characterization of nanosuspension was performed by particle size and size distribution, drug content, Scanning electron microscopy, Differential scanning colorimetry and X-ray diffraction technique. Optimized nanosuspension showed a mean particle diameter of 294nm, spherical shape with surface oriented surfactant molecules, which were stabilized formulation, high drug content, no chemical instability and no significant change in crystalline nature after formulation also. The in vitro dissolution profile of optimized formulation compared to pure drug and marketed formulation (Canditral Capsule) using 0.1N Hydrochloric acid as dissolution medium showed higher drug release compared to the pure drug and marketed formulation. 

 

Key Words : Nanosuspension, Itraconazole, Pearl milling technique.

 

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