Aspergillus fumigatus and C. albicans are the two most widespread fungal pathogens causing stern insidious infections surrounded by immuno compromised patients. Fluconazole is an antifungal drug of triazole class with incomparable bioavailability. This paper describes the performance of plain fluconazole and micronized fluconazole material for increasing health safety and its biological evaluation by using Aspergillus fumigatus and C. albicans. An active pharma ingredient having antifungal activity was selected and micronized using Microniser to reduce the particle size as low as possible. The product antifungal activity was reviewed between Plain material (heavy particle size, 200 microns) and reduced particle size (micro particles, 2.72 microns). Antifungal drugs with lowest particle size increases efficiency. The Determination of particle size to the micronized material (very fine powder) and its characteristics by laser diffraction and Scanning Electron Microscopy (SEM) and structural identification by Fourier transform Infrared spectroscopy (FT-IR). The efficiency of fluconazole in-terms of antifungal activity of micronized material shows increased efficiency when compared to fluconazole plain material (coarser type particles).