Oral bioavailability enhancement of flubendazole by developing nanofibrous solid dosage forms

Tamás Vigh, Balázs Démuth, Attila Balogh, Dorián L. Galata, Ivo Van Assche, Claire Mackie, Monica Vialpando, Ben Van Hove, Petros Psathas, Enikő Borbás, Hajnalka Pataki, Peter Boeykens, G. Marosi, Geert Verreck, Zsombor K. Nagy

Research output: Contribution to journalArticle

8 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)1-8
Number of pages8
JournalDrug Development and Industrial Pharmacy
DOIs
Publication statusAccepted/In press - Mar 8 2017

Fingerprint

Dosage Forms
Biological Availability
Ocular Onchocerciasis
Elephantiasis
Crystalline materials
Nanofibers
Povidone
Cyclodextrins
Tablets
Rats
Dissolution
Parasites
Compaction
Rivers
Plasmas
Fibers
Pharmaceutical Preparations
flubendazole

Keywords

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

ASJC Scopus subject areas

  • Medicine(all)
  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

Cite this

Vigh, T., Démuth, B., Balogh, A., Galata, D. L., Van Assche, I., Mackie, C., ... Nagy, Z. K. (Accepted/In press). Oral bioavailability enhancement of flubendazole by developing nanofibrous solid dosage forms. Drug Development and Industrial Pharmacy, 1-8. https://doi.org/10.1080/03639045.2017.1298121

Oral bioavailability enhancement of flubendazole by developing nanofibrous solid dosage forms. / Vigh, Tamás; Démuth, Balázs; Balogh, Attila; Galata, Dorián L.; Van Assche, Ivo; Mackie, Claire; Vialpando, Monica; Van Hove, Ben; Psathas, Petros; Borbás, Enikő; Pataki, Hajnalka; Boeykens, Peter; Marosi, G.; Verreck, Geert; Nagy, Zsombor K.

In: Drug Development and Industrial Pharmacy, 08.03.2017, p. 1-8.

Research output: Contribution to journalArticle

Vigh, T, Démuth, B, Balogh, A, Galata, DL, Van Assche, I, Mackie, C, Vialpando, M, Van Hove, B, Psathas, P, Borbás, E, Pataki, H, Boeykens, P, Marosi, G, Verreck, G & Nagy, ZK 2017, 'Oral bioavailability enhancement of flubendazole by developing nanofibrous solid dosage forms', Drug Development and Industrial Pharmacy, pp. 1-8. https://doi.org/10.1080/03639045.2017.1298121
Vigh, Tamás ; Démuth, Balázs ; Balogh, Attila ; Galata, Dorián L. ; Van Assche, Ivo ; Mackie, Claire ; Vialpando, Monica ; Van Hove, Ben ; Psathas, Petros ; Borbás, Enikő ; Pataki, Hajnalka ; Boeykens, Peter ; Marosi, G. ; Verreck, Geert ; Nagy, Zsombor K. / Oral bioavailability enhancement of flubendazole by developing nanofibrous solid dosage forms. In: Drug Development and Industrial Pharmacy. 2017 ; pp. 1-8.
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