title: Development and characterization of the voriconazole loaded lipid-based nanoparticles.
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. 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±4.1nm after five cycles of homogenization at 600bar. The antifungal study confirmed that the optimized VCZ-LNP inhibited the fungus reproduction.
authors.affiliation: Semmelweis University, Department of Pharmaceutics, H-1092 Budapest Hőgyes Endre St 7., Hungary.
authors.forename: Petra
authors.initials: P
authors.lastname: Füredi
authors.affiliation: Semmelweis University, Department of Pharmaceutics, H-1092 Budapest Hőgyes Endre St 7., Hungary.
authors.forename: Zsófia Edit
authors.initials: ZE
authors.lastname: Pápay
authors.affiliation: Semmelweis University, Department of Pharmaceutics, H-1092 Budapest Hőgyes Endre St 7., Hungary.
authors.forename: Kristóf
authors.initials: K
authors.lastname: Kovács
authors.affiliation: Semmelweis University, Department of Pharmaceutics, H-1092 Budapest Hőgyes Endre St 7., Hungary.
authors.forename: Borbála Dalmadi
authors.initials: BD
authors.lastname: Kiss
authors.affiliation: Semmelweis University, Department of Pharmaceutics, H-1092 Budapest Hőgyes Endre St 7., Hungary.
authors.forename: Krisztina
authors.initials: K
authors.lastname: Ludányi
authors.affiliation: Semmelweis University, Department of Pharmaceutics, H-1092 Budapest Hőgyes Endre St 7., Hungary.
authors.forename: István
authors.initials: I
authors.lastname: Antal
authors.affiliation: Semmelweis University, Department of Pharmaceutics, H-1092 Budapest Hőgyes Endre St 7., Hungary. Electronic address: klebovich.imre@pharma.semmelweis-univ.hu.
authors.forename: Imre
authors.initials: I
authors.lastname: Klebovich
mesh_terms: D000935:Antifungal Agents / Q000737:chemistry; D001228:Aspergillosis / Q000188:drug therapy; D002152:Calorimetry, Differential Scanning; D016503:Drug Delivery Systems; D008055:Lipids / Q000737:chemistry; D050997:Nanomedicine / Q000379:methods*; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D011312:Pressure; D015203:Reproducibility of Results; D012709:Serum Albumin / Q000737:chemistry; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013696:Temperature; D065819:Voriconazole / Q000032:analysis / Q000737:chemistry*
chemical_list: D000935:Antifungal Agents; D008055:Lipids; D012709:Serum Albumin; D065819:Voriconazole
keywords: Antifungal study; Dialysis test; Differential scanning calorimetry (DSC); FTIR spectroscopy; High pressure homogenization; Particle size analysis