Please use this identifier to cite or link to this item: http://hdl.handle.net/1942/17777
Title: Formulation of itraconazole nanococrystals and evaluation of their bioavailability in dogs
Authors: De Smet, Lieselotte
Saerens, Lien
De Beer, Thomas
CARLEER, Robert 
ADRIAENSENS, Peter 
Van Bocxlaer, Jan
Vervaet, Chris
Remon, Jean Paul
Issue Date: 2014
Publisher: ELSEVIER SCIENCE BV
Source: EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, 87 (1), p. 107-113
Abstract: The aim of the study is to increase the bioavailability of itraconazole (ITRA) using nanosized cocrystals prepared via wet milling of ITRA in combination with dicarboxylic acids. Wet milling was used in order to create a nanosuspension of ITRA in combination with dicarboxylic acids. After spray-drying and bead layering, solid state was characterized by MDSC, XRD, Raman and FT-IR. The release profiles and bioavailability of the nanococrystalline suspension, the spray-dried and bead layered formulation were evaluated. A monodisperse nanosuspension (549 +/- 51 nm) of ITRA was developed using adipic acid and Tween (R) 80. Solid state characterization indicated the formation of nanococrystals by hydrogen bounds between the triazole group of ITRA and the carboxyl group of adipic acid. A bioavailability study was performed in dogs. The faster drug release from the nanocrystal-based formulation was reflected in the in vivo results since T-max of the formulations was obtained 3 h after administration, while T-max of the reference formulation was observed only 6 h after administration. This fast release of ITRA was obtained by a dual concept: manufacturing of nanosized cocrystals of ITRA and adipic acid via wet milling. Formation of stable nanosized cocrystals via this approach seems a good alternative for amorphous systems to increase the solubility and obtain a fast drug release of BCS class II drugs. (C) 2013 Elsevier B.V. All rights reserved.
Notes: [De Smet, Lieselotte; Vervaet, Chris; Remon, Jean Paul] Univ Ghent, Lab Pharmaceut Technol, B-9000 Ghent, Belgium. [Saerens, Lien; De Beer, Thomas] Univ Ghent, Lab Pharmaceut Proc Analyt Technol, B-9000 Ghent, Belgium. [Carleer, Robert; Adriaensens, Peter] Hasselt Univ, Diepenbeek, Belgium. [Van Bocxlaer, Jan] Univ Ghent, Lab Med Biochem & Clin Anal, B-9000 Ghent, Belgium.
Keywords: itraconazole; wet milling; cocrystals; nanosuspension; dicarboxylic acids; poorly water soluble drugs;Itraconazole; Wet milling; Cocrystals; Nanosuspension; Dicarboxylic acids; Poorly water soluble drugs
Document URI: http://hdl.handle.net/1942/17777
ISSN: 0939-6411
e-ISSN: 1873-3441
DOI: 10.1016/j.ejpb.2013.12.016
ISI #: 000337861700012
Rights: © 2013 Elsevier B.V. All rights reserved.
Category: A1
Type: Journal Contribution
Validations: ecoom 2015
Appears in Collections:Research publications

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