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 György, Verreck Geert, Nagy Zsombor K
a Department of Organic Chemistry and Technology , Budapest University of Technology and Economics , Budapest , Hungary.
b Drug Product Development, Janssen R&D , Beerse , Belgium.
Drug Dev Ind Pharm. 2017 Jul;43(7):1126-1133. doi: 10.1080/03639045.2017.1298121. Epub 2017 Mar 8.
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.
通过制备完全无定形的电纺纳米纤维，其基质由羟丙基-β-环糊精和聚乙烯吡咯烷酮组成，驱虫药氟苯达唑的生物利用度与纯结晶药物相比显著提高。由此制备的制剂可能对引起热带疾病（如河盲症和象皮病）的大型丝虫寄生虫具有活性，这些疾病在全球共影响超过一亿人。生物利用度的提高基于显著改善的溶解性。40毫克剂量可在15分钟内释放。因此，与几乎不吸收的结晶氟苯达唑相比，纳米纤维系统的给药确保了大鼠体内血浆浓度的增加。此外，可以开发易于研磨的纤维，从而能够压制易于给药的速释片剂。
