| Literature DB >> 28274133 |
Tamás Vigh1, Balázs Démuth1, Attila Balogh1, Dorián L Galata1, Ivo Van Assche2, Claire Mackie2, Monica Vialpando2, Ben Van Hove2, Petros Psathas2, Enikő Borbás1, Hajnalka Pataki1, Peter Boeykens2, György Marosi1, Geert Verreck2, Zsombor K Nagy1.
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.Entities:
Keywords: Nanofiber; amorphization; bioavailability; dissolution; downstream; electrospinning; immediate release
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Year: 2017 PMID: 28274133 DOI: 10.1080/03639045.2017.1298121
Source DB: PubMed Journal: Drug Dev Ind Pharm ISSN: 0363-9045 Impact factor: 3.225