Fabrication of electrospun nanofibres of BCS II drug for enhanced dissolution and permeation across skin

Abstract

The present work reports preparation of irbesartan (IBS) loaded nanofibre mats using electrospinning technique. The prepared nanofibres were characterized by scanning electron microscopy, Fourier transform infrared spectroscopy, differential scanning calorimetry, X-ray diffraction analysis, in vitro diffusion and ex vivo skin permeation studies. FTIR studies revealed chemical compatibility of IBS and polyvinyl pyrrolidine (PVP K-30). SEM images confirmed formation of nanofibres wherein IBS existed in amorphous form as revealed by DSC and XRD analyses. The prepared nanofibre mats of IBS were found to be superior to IBS loaded as cast films when analysed for in vitro IBS release and ex vivo skin permeation studies since the flux of IBS loaded nanofibres was 17 times greater than as cast film. The improvement in drug delivery kinetics of IBS loaded nanofibres could be attributed to amorphization with reduction in particle size of IBS, dispersion of IBS at molecular level in PVP matrix and enormous increase in the surface area for IBS release due to nanonization. Thus transdermal patch of IBS loaded nanofibres can be considered as an alternative dosage form in order to improve its biopharmaceutical properties and enhance therapeutic efficacy in hypertension.

Electrospinning Nanofibers for Therapeutics Delivery

“…It has been reported that electrospun nanofibers could enhance solubility and form a transdermal patch for the biopharmaceutics classification systems II drugs with a high therapeutic efficiency and no cytotoxicity. Hydrophilic polymers with great permeation are the strength of TDDS, and several in vitro and in vivo evaluations suggest the possibility of using drug-loaded electrospun nanofibers in establishing TDDS [59].…”

Hybrid transdermal drug delivery patch made from poly(p‐phenylene vinylene)/natural rubber latex and controlled by an electric field

“…The release−permeation of Ibu from the Ibu‐loaded NR patch and Ibu‐doped PPV/NR patch was investigated next. The release−permeation characteristic of Ibu from the Ibu‐loaded NR patch and Ibu‐doped PPV/NR patch were investigated using a modified Franz diffusion cell at pH 7.4 at 37 °C for the duration of 48 h . Each patch (area 3.14 cm 2 and thickness 0.5 cm) was placed on pigskin, which was mounted on a receptor chamber of the modified Franz cell and covered on top by an anode electrode.…”

Electrospun nanofibers: A nanotechnological approach for drug delivery and dissolution optimization in poorly water-soluble drugs

“…Amidon et al classified drug molecules as a function of their aqueous solubility and intestinal permeability in the Biopharmaceutics Classification System (BCS) [139]. Classes II and IV in the BCS have poor solubility due to their complete dose not being possible to dissolve when ingested with a glass of water (250 ml) [140][141][142]. A great majority of new drug molecules and lead compounds are within Class II and IV, and thus present limited oral absorption, slow in vivo dissolution, and low bioavailability [141,[143][144][145].…”