Abstract

The number of topical fungal infections is growing, mostly owing to immunosuppressive therapy. Several topical fungal infections, such as eye mycoses, can be treated by local administration of antimycotic drugs. One major group of the antifungal agents is triazole, such as voriconazole (VCZ), which is used as the first line treatment of aspergillosis. A disadvantage of VCZ is its low water solubility making the drug difficult to administer in a liquid preparation.

The lipid-based nanoparticles (LNP) have attracted increasing attention due to their advantageous properties. Contrarily to the conventional carrier systems, LNP can improve the poor solubility of topically used drugs, such as VCZ. Therefore, LNP represents promising alternatives to traditional carrier systems.

Highlights

• All of the novel VCZ-LNP formulations inhibit the reproduction of fungus.

• FTIR revealed the chemical structure of VCZ was not affected by HPH.

• The developed VCZ-LNP can serve as the base of an ocular drug delivery system.

The aim of the study was to formulate VCZ loaded lipid-based nanoparticles (VCZ-LNP) by high pressure homogenization (HPH). The developed LNPs were characterized by particle size analysis, IR spectroscopy, differential scanning calorimetry, dialysis test and antifungal efficacy studies. The particle size of the optimized nanoparticles from the selected lipid base, Witepsol® W35, was 182 ± 4.1 nm after five cycles of homogenization at 600 bar. The antifungal study confirmed that the optimized VCZ-LNP inhibited the fungus reproduction.

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