Abstract
Posaconazole is a recently Unites States Food and Drug Administration approved antifungal agent. It possesses poor oral bioavailability because of its poor aqueous solubility. The objective of this study was to develop nano-sized particles of posaconazole with the expectation that the nano-sized particles will have better aqueous solubility and, improved antifungal activity. Nano-sizing was done using Supercritical Anti-Solvent (SAS) technology. The average particle size of posaconazole before and after nano-sizing was determined using dynamic light scattering technique. The nano-sized particles were characterized by scanning electron microscopy, FTIR, differential scanning calorimetry, and the powder X-ray diffraction. A USP dissolution apparatus with a paddle operating at 100 rpm was used for the dissolution studies. A marked improvement in the aqueous solubility of posaconazole was observed after nano-sizing, wherein the nano-sized posaconazole showed about 25-fold higher solubility than posaconazole. Screening of antifungal activity was carried out using the well diffusion method, wherein it was observed that the nano-sized posaconazole had improved antifungal activity than posaconazole. It has been concluded that nano-sizing of posaconazole using SAS technology results in posaconazole nano-powder without change in the polymorphic characteristics of the drug, it has improved aqueous solubility, and improved antifungal activity. It is also expected that the nano-sized posaconazole might have improved bioavailability. Therefore, further bioavailability studies are recommended.