2017 Jul;43(7):1126-1133. doi: 10.1080/03639045.2017.1298121. Epub 2017 Mar 8.

Author information

1
a Department of Organic Chemistry and Technology , Budapest University of Technology and Economics , Budapest , Hungary.
2
b Drug Product Development, Janssen R&D , Beerse , Belgium.

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.

KEYWORDS:

Nanofiber; amorphization; bioavailability; dissolution; downstream; electrospinning; immediate release

PMID:
28274133
DOI:
10.1080/03639045.2017.1298121

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