NDLI: Targeted High Lung Concentrations of Itraconazole Using Nebulized Dispersions in a Murine Model

Content Provider	Springer Nature Link
Author	McConville, Jason T. Overhoff, Kirk A. Sinswat, Prapasri Vaughn, Jason M. Frei, Bradi L. Burgess, David S. Talbert, Robert L. Peters, Jay I. Johnston, Keith P. Williams, Robert O.
Copyright Year	2006
Abstract	The purpose of this study was to investigate the delivery of itraconazole (ITZ) particles to a murine lung model by nebulization.Three ITZ formulations were prepared and characterized in the dry state using contact angle, dissolution, X-ray powder diffraction, scanning electron microscopy, and Brunauer–Emmett–Teller surface area analysis. Aerodynamic particle size distributions and lung deposition studies in 14 outbred male ICR mice were performed using aqueous dispersions of all the formulations. A separate dosing uniformity study was also performed to qualify use of the chamber.All formulations had an aggregated particle size of approximately 30 μm in diameter. Two formulations showed that 80% of the drug dissolved in less than 5 min. The remaining ITZ formulation had a slower dissolution and the lowest total emitted dose from the nebulizer used. High concentrations of ITZ were shown to be present in the mouse lung during the lung deposition study, up to 16.8 ± 0.13 μg/g (± SE) were achieved. Concentrations of up to 0.76 ± 0.03 μg/g (± SE) could be maintained from the single nebulized dose for at least 24 h.An effective method of targeted delivery of ITZ to the deep lung is presented that may be useful for the treatment and prevention of acute fungal infections.
Starting Page	901
Ending Page	911
Page Count	11
File Format	PDF
ISSN	07248741
Journal	Pharmaceutical Research
Volume Number	23
Issue Number	5
e-ISSN	1573904X
Language	English
Publisher	Springer-Verlag
Publisher Date	2006-05-05
Publisher Place	New York
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	antifungal fungal infection nanoparticle nebulization poorly water-soluble Pharmacology/Toxicology Pharmacy Biochemistry Medical Law Biomedical Engineering
Content Type	Text
Resource Type	Article
Subject	Organic Chemistry Pharmacology Molecular Medicine Pharmacology (medical) Biotechnology Pharmaceutical Science

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