title: Itraconazole-loaded nanostructured lipid carriers (NLC) for pulmonary treatment of aspergillosis in falcons.
abstract: Aspergillosis is the most common and most lethal disease in captive falcons, which is most effectively treated with the poorly soluble drug Itraconazole. To obtain a high drug concentration at the side of infection, the falcon's respiratory system, an isotonic, sterile, non-toxic NLC formulation loaded with Itraconazole was developed for pulmonary application. Itraconazole-loaded NLC had a particle size well in the nanometer range and possessed a narrow particle size distribution. An entrapment efficiency of 99.98% was achieved. A good storage stability of the formulation over 6months was found. Neither by MTS nor by LDH assay cytotoxic effects were determined on the cell line A549, indicating a good tolerability after inhalation. No physical instabilities of Itraconazole-loaded NLC could be detected nebulizing the formulation with a new nanonebulizer into a therapeutic chamber for the treatment of falcons. It could be shown, that the particle size of the aerosol generated nebulizing Itraconazole-loaded NLC with the nanonebulizer was in the nanometer range, providing the possibility to penetrate into the respiratory tract of falcons. By scintigraphy deposition of Itraconazole-loaded NLC in the lung and the air sacs of a patient was shown, being a prerequisite for the pulmonary treatment of aspergillosis in falcons.
authors.affiliation: Institute of Pharmaceutical Sciences, Department of Pharmaceutical Technology, Karl-Franzens Universität Graz, Humboldtstraße 46, 8010 Graz, Austria. Electronic address: jana-pardeike@web.de.
authors.forename: Jana
authors.initials: J
authors.lastname: Pardeike
authors.affiliation: Institute of Pharmaceutical Sciences, Department of Pharmaceutical Technology, Karl-Franzens Universität Graz, Humboldtstraße 46, 8010 Graz, Austria.
authors.forename: Sabrina
authors.initials: S
authors.lastname: Weber
authors.affiliation: Private Veterinary Surgery, Auen 23, 9400 Wolfsberg, Austria.
authors.forename: Hans Peter
authors.initials: HP
authors.lastname: Zarfl
authors.affiliation: Veterinärmedizinische Universität Wien, Veterinärplatz 1, 1210 Vienna, Austria.
authors.forename: Maximilian
authors.initials: M
authors.lastname: Pagitz
authors.affiliation: Institute of Pharmaceutical Sciences, Department of Pharmaceutical Technology, Karl-Franzens Universität Graz, Humboldtstraße 46, 8010 Graz, Austria.
authors.forename: Andreas
authors.initials: A
authors.lastname: Zimmer
mesh_terms: D000072283:A549 Cells; D000336:Aerosols; D000818:Animals; D000935:Antifungal Agents / Q000008:administration & dosage*; D001228:Aspergillosis / Q000188:drug therapy* / Q000662:veterinary*; D001717:Birds; D002152:Calorimetry, Differential Scanning; D045744:Cell Line, Tumor; D016503:Drug Delivery Systems; D005720:Gamma Rays; D006801:Humans; D017964:Itraconazole / Q000008:administration & dosage*; D045022:Lactate Dehydrogenases / Q000378:metabolism; D007834:Lasers; D008055:Lipids / Q000737:chemistry*; D008168:Lung / Q000187:drug effects / Q000382:microbiology; D049329:Nanostructures / Q000737:chemistry*; D009330:Nebulizers and Vaporizers; D010316:Particle Size; D017785:Photons; D011877:Radionuclide Imaging
chemical_list: D000336:Aerosols; D000935:Antifungal Agents; D008055:Lipids; D017964:Itraconazole; D045022:Lactate Dehydrogenases
keywords: Aspergillosis; Cell culture; Falcons; Lipid nanoparticles; Pulmonary; Scintigraphy