The 3<sup>rd</sup> International Conference on Drug Discovery & Therapy: Dubai, February 7 - 11, 2011

Anti-Infectives (Track)



In vitro activity of a novel propiconazole derivative (MXP-4509) nanoparticle-formulated

Mihai Mares
"Ion Ionescu de la Brad" University, IASI, Romania

Abstract:

MXP 4509 is a novel investigational antifungal drug derived from a triazole compound (propiconazole), formulated in nanoparticles in order to improve its hydrosolubility. In vitro susceptibility was assessed by following the guidelines of AFST-EUCAST E. Def. 7.1 and E. Def. 9.1 methods. Testing was performed with RPMI-1640 medium buffered with MOPS and supplemented with 2% glucose and also using a modified medium with low pH in an experimental model of biomimetism. The final concentrations of antifungal ranged between 0.0156-8 mg/L. As test strains, we used clinical isolates of yeasts and filamentous fungi belonging to seven genera (i.e. Candida, Cryptococcus, Geotrichum, Rhodotorula, Saccharomyces, Trichosporon, and Aspergillus). To assure the quality of test results it was used two control strains (Candida krusei ATCC 6258 and C. parapsilosis ATCC 22019) each time when the susceptibility testing was performed. The minimum inhibitory concentration (MIC) for the tested drug was considered the lowest concentration giving rise to an inhibition of growth of more 50% comparing with that of the drug-free control. The MIC90 values were lower for C. albicans (0.0312 mg/L) and higher for Aspergillus flavus (16 mg/L). The new azole MXP-4509 proved to have a good antifungal in vitro activity raising the interest for further pharmacological and microbiological investigations in order to assess its advantages for therapy.

Keywords: MXP-4509, propiconazole, nanoparticles, antifungal activity