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.

Scaled-up preparation of drug-loaded electrospun polymer fibres and investigation of their continuous processing to tablet form

“…especially favourable in the field of pharmaceutical application [7][8][9][10][11][12][13][14][15][16][17][18]. Although the electrospinning (ES) is fast developing with appearance of tri-axial, coaxial, side-by-side and their combination processes [19][20][21][22] the most common and facile ES equipment is the single needle apparatus [23,24].…”

Homogenization of Amorphous Solid Dispersions Prepared by Electrospinning in Low-Dose Tablet Formulation

“…The manufacture of fibers was carried out at ambient temperature (25 °C). More details about HSES can be found in the literature [ 44 ].…”

Scale‐up of electrospinning technology: Applications in the pharmaceutical industry

“…It has been shown that rational selection of the applied polymer can ensure the Vass et al (2020) stability of the amorphous drug in the matrix which meets the strict requirements of the pharmaceutical industry . The technology proved to be appropriate for the formation of flubendazole containing electrospun product as well (Vigh et al, 2017). Both the drug-loaded nanofibers and the tablets filled with the fibers had outstanding dissolution properties.…”