Itraconazole-loaded nanostructured lipid carriers (NLC) for pulmonary treatment of aspergillosis in falcons

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• 作者：Jana Pardeike^a ; ^{jana-pardeike@web.de" class="auth_mail" title="E-mail the corresponding author} ; Sabrina Weber^a ; Hans Peter Zarfl^b ; Maximilian Pagitz^c ; Andreas Zimmer^a
• 关键词：Pulmonary ; Scintigraphy ; Cell culture ; Lipid nanoparticles ; Aspergillosis ; Falcons
• 刊名：European Journal of Pharmaceutics and Biopharmaceutics
• 出版年：2016
• 出版时间：November 2016
• 年：2016
• 卷：108
• 期：Complete
• 页码：269-276
• 全文大小：1034 K

文摘

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 6 months 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.