Development and characterization of miconazole-loaded lipid nanoparticles against pulmonary mycoses

Zsófia Edit Pápay1, Eszter Gulyás, Petra Füredi & István Antal

The responsible pathogens for pulmonary mycoses can be commonly found in the environment, mainly Aspergillus and Candida fungal strains. The development of this severe condition is associated with chronic lung diseases and immunodeficiency. Azoles such as miconazole, is one of the first-line treatment with broad antifungal activity, however, it belongs to the II. group of Biopharmaceutical Classification System (BCS) with low water solubility. Therefore there is a need for development of an effective delivery tool for the local administration of this antifungal agent. Among colloidal carrier systems, solid lipid nanoparticles (SLN) have outstanding properties in terms of small particles size, high drug encapsulation capacity and tolerability. Therefore the aim of this study was to develop and characterize miconazole-loaded SLN against lung mycoses. Witepsol® 35 was used as a lipid phase. For five high pressure homogenization cycles at 600 bar prove to be a suitable method for developing lipid nanoparticles with the optimal particle size (182.0 ± 1.9 nm), polydispersity index (0.297 ± 0.03) and as high encapsulation efficiency as 99%. The encapsulation of the miconazole was further verified by DSC thermograms and FTIR spectra. The antifungal study proved that miconazole maintained its effectiveness against A. flavus and C. glabra fungus strains, the clear zones of inhibition could be well observed. This study provides evidence that SLN are suitable carriers of the poorly water soluble miconazole and represents a promising delivery system against pulmonary mycoses with potential broad antifungal activity.

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