title: Nanonized itraconazole powders for extemporary oral suspensions: Role of formulation components studied by a mixture design.
abstract: Itraconazole (ITZ) nanocrystal-containing powders were prepared through the combined use of high pressure homogenization (HPH) and spray drying (SD). These powders were intended as base materials for the preparation of extemporary oral suspensions of the drug. The role and the effect of stabilizers on the size of re-dispersed particles were studied using a mixture design and a Scheffé model relating the dried nanosuspension composition to the mean particle diameters. The homogenization process required a surface active agent (Tween 20) to obtain the efficient comminution of itraconazole micronized powder. SD was carried out on ITZ nanosuspensions after addition of a cellulose derivative (Methocel(®) E5) that allowed the prompt re-dispersion of nanoparticles under "in use" conditions. The powders obtained by drying of homogenized systems showed in vitro dissolution profile faster than that of the micronized drug, suggesting a potential ameliorated GI absorption of itraconazole released from the nanosuspensions.
authors.affiliation: Università degli Studi del Piemonte Orientale "A. Avogadro", Dipartimento di Scienze del Farmaco, Largo Donegani 2/3, 28100 Novara, Italy.
authors.forename: Andrea
authors.initials: A
authors.lastname: Foglio Bonda
authors.affiliation: Università degli Studi del Piemonte Orientale "A. Avogadro", Dipartimento di Scienze del Farmaco, Largo Donegani 2/3, 28100 Novara, Italy.
authors.forename: Maurizio
authors.initials: M
authors.lastname: Rinaldi
authors.affiliation: Università degli Studi del Piemonte Orientale "A. Avogadro", Dipartimento di Scienze del Farmaco, Largo Donegani 2/3, 28100 Novara, Italy.
authors.forename: Lorena
authors.initials: L
authors.lastname: Segale
authors.affiliation: Università degli Studi di Milano, Dipartimento di Scienze Farmaceutiche, via G. Colombo 71, 20133 Milano, Italy.
authors.forename: Luca
authors.initials: L
authors.lastname: Palugan
authors.affiliation: Università degli Studi di Milano, Dipartimento di Scienze Farmaceutiche, via G. Colombo 71, 20133 Milano, Italy.
authors.forename: Matteo
authors.initials: M
authors.lastname: Cerea
authors.affiliation: Pharmaceutical Technologies & Development, Via Comignago 2B, Revislate, 28010 Veruno, NO, Italy.
authors.forename: Carlo
authors.initials: C
authors.lastname: Vecchio
authors.affiliation: Università degli Studi del Piemonte Orientale "A. Avogadro", Dipartimento di Scienze del Farmaco, Largo Donegani 2/3, 28100 Novara, Italy. Electronic address: franco.pattarino@uniupo.it.
authors.forename: Franco
authors.initials: F
authors.lastname: Pattarino
mesh_terms: D000284:Administration, Oral; D000935:Antifungal Agents / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical; D017964:Itraconazole / Q000737:chemistry*; D008747:Methylcellulose / Q000737:chemistry; D008855:Microscopy, Electron, Scanning; D008962:Models, Theoretical; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D010316:Particle Size; D011136:Polysorbates / Q000737:chemistry; D011208:Powders; D012995:Solubility; D013535:Suspensions; D013678:Technology, Pharmaceutical
chemical_list: D000935:Antifungal Agents; D011136:Polysorbates; D011208:Powders; D013535:Suspensions; D017964:Itraconazole; D008747:Methylcellulose
keywords: High pressure homogenization; Itraconazole; Mathematical model; Mixture design; Nanosuspensions; Spray drying