title: Oral bioavailability enhancement of flubendazole by developing nanofibrous solid dosage forms.
abstract: The bioavailability of the anthelminthic flubendazole was remarkably enhanced in comparison with the pure crystalline drug by developing completely amorphous electrospun nanofibres with a matrix consisting of hydroxypropyl-β-cyclodextrin and polyvinylpyrrolidone. The thus produced formulations can potentially be active against macrofilariae parasites causing tropical diseases, for example, river blindness and elephantiasis, which affect altogether more than a hundred million people worldwide. The bioavailability enhancement was based on the considerably improved dissolution. The release of a dose of 40 mg could be achieved within 15 min. Accordingly, administration of the nanofibrous system ensured an increased plasma concentration profile in rats in contrast to the practically non-absorbable crystalline flubendazole. Furthermore, easy-to-grind fibers could be developed, which enabled compression of easily administrable immediate release tablets.
authors.affiliation: a Department of Organic Chemistry and Technology , Budapest University of Technology and Economics , Budapest , Hungary.
authors.forename: Tamás
authors.initials: T
authors.lastname: Vigh
authors.affiliation: a Department of Organic Chemistry and Technology , Budapest University of Technology and Economics , Budapest , Hungary.
authors.forename: Balázs
authors.initials: B
authors.lastname: Démuth
authors.affiliation: a Department of Organic Chemistry and Technology , Budapest University of Technology and Economics , Budapest , Hungary.
authors.forename: Attila
authors.initials: A
authors.lastname: Balogh
authors.affiliation: a Department of Organic Chemistry and Technology , Budapest University of Technology and Economics , Budapest , Hungary.
authors.forename: Dorián L
authors.initials: DL
authors.lastname: Galata
authors.affiliation: b Drug Product Development, Janssen R&D , Beerse , Belgium.
authors.forename: Ivo
authors.initials: I
authors.lastname: Van Assche
authors.affiliation: b Drug Product Development, Janssen R&D , Beerse , Belgium.
authors.forename: Claire
authors.initials: C
authors.lastname: Mackie
authors.affiliation: b Drug Product Development, Janssen R&D , Beerse , Belgium.
authors.forename: Monica
authors.initials: M
authors.lastname: Vialpando
authors.affiliation: b Drug Product Development, Janssen R&D , Beerse , Belgium.
authors.forename: Ben
authors.initials: B
authors.lastname: Van Hove
authors.affiliation: b Drug Product Development, Janssen R&D , Beerse , Belgium.
authors.forename: Petros
authors.initials: P
authors.lastname: Psathas
authors.affiliation: a Department of Organic Chemistry and Technology , Budapest University of Technology and Economics , Budapest , Hungary.
authors.forename: Enikő
authors.initials: E
authors.lastname: Borbás
authors.affiliation: a Department of Organic Chemistry and Technology , Budapest University of Technology and Economics , Budapest , Hungary.
authors.forename: Hajnalka
authors.initials: H
authors.lastname: Pataki
authors.affiliation: b Drug Product Development, Janssen R&D , Beerse , Belgium.
authors.forename: Peter
authors.initials: P
authors.lastname: Boeykens
authors.affiliation: a Department of Organic Chemistry and Technology , Budapest University of Technology and Economics , Budapest , Hungary.
authors.forename: György
authors.initials: G
authors.lastname: Marosi
authors.affiliation: b Drug Product Development, Janssen R&D , Beerse , Belgium.
authors.forename: Geert
authors.initials: G
authors.lastname: Verreck
authors.affiliation: a Department of Organic Chemistry and Technology , Budapest University of Technology and Economics , Budapest , Hungary.
authors.forename: Zsombor K
authors.initials: ZK
authors.lastname: Nagy
mesh_terms: D000073738:2-Hydroxypropyl-beta-cyclodextrin; D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D003460:Crystallization; D008463:Mebendazole / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry; D057139:Nanofibers / Q000737:chemistry*; D011205:Povidone / Q000737:chemistry*; D051381:Rats; D013607:Tablets / Q000737:chemistry*; D047392:beta-Cyclodextrins / Q000737:chemistry*
chemical_list: D013607:Tablets; D047392:beta-Cyclodextrins; D000073738:2-Hydroxypropyl-beta-cyclodextrin; D008463:Mebendazole; D011205:Povidone; C018945:flubendazole
keywords: Nanofiber; amorphization; bioavailability; dissolution; downstream; electrospinning; immediate release