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Title: Increasing the oral bioavailability of the poorly water soluble drug itraconazole with ordered mesoporous silica
Authors: Mellaerts, Randy ×
Mols, Rafaƫl
Jammaer, Jasper
Aerts, Caroline
Annaert, Pieter
Van Humbeeck, Jan
Van den Mooter, Guy
Augustijns, Patrick
Martens, Johan #
Issue Date: May-2008
Publisher: Wissenschaftliche Verlagsgesellschaft
Series Title: European Journal of Pharmaceutics and Biopharmaceutics vol:69 issue:1 pages:223-230
Abstract: This study aims to evaluate the in vivo performance of ordered mesoporous silica (OMS) as a carrier for poorly water soluble drugs. Itraconazole was selected as model compound. Physicochemical characterization was carried out by SEM, TEM, nitrogen adsorption, DSC, TGA and in vitro dissolution. After loading itraconazole into OMS, its oral bioavailability was compared with the crystalline drug and the marketed product Sporanox(R) in rabbits and dogs. Plasma concentrations of itraconazole and OH-itraconazole were determined by HPLC-UV. After administration of crystalline itraconazole in dogs (20 mg), no systemic itraconazole could be detected. Using OMS as a carrier, the AUC(0-8) was boosted to 681 +/- 566 nM h. In rabbits, the AUC(0-24) increased significantly from 521 +/- 159 nM h after oral administration of crystalline itraconazole (8 mg) to 1069 +/- 278 nM h when this dose was loaded into OMS. T-max decreased from 9.8 +/- 1.8 to 4.2 +/- 1.8 h. No significant differences (AUC, C-max, and T-max) could be determined when comparing OMS with Sporanox(R) in both species. The oral bioavailability of itraconazole formulated with OMS as a carrier compares well with the marketed product Sporanox(R), in rabbits as well as in dogs. OMS can therefore be considered as a promising carrier to achieve enhanced oral bioavailability for drugs with extremely low water solubility. (C) 2007 Elsevier B.V. All rights reserved.
URI: 
ISSN: 0939-6411
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Physical Metallurgy and Materials Engineering Section (-)
Centre for Surface Chemistry and Catalysis
Drug Delivery and Disposition
× corresponding author
# (joint) last author

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