Voriconazole Composited Polyvinyl Alcohol/Hydroxypropyl-β-Cyclodextrin Nanofibers for Ophthalmic Delivery

Abstract

Voriconazole (VRC) incorporated in composited polyvinyl alcohol (PVA)/hydroxypropyl-β-cyclodextrin (HPβCD) blended nanofibers were produced via electrospinning for efficient ophthalmic delivery. The VRC loading capacity increased with increasing HPβCD content. The optimal solution for electrospinning consisted of 8% (w/v) PVA, 4% (w/v) HPβCD and 0.5% (w/v) VRC. The nanofibers exhibited bead-free average fiber diameters of 307±31 nm and VRC was released in vitro in a sustained manner. The VRC nanofibers were characterized by infrared spectroscopy (FTIR), thermogravimetric analysis (TGA), differential scanning calorimetry (DSC) and scanning electron microscopy (SEM). The proton nuclear magnetic resonance (1H-NMR) was used to analyze the molar ratio of HPβCD/VRC in the nanofibers. Compared with a VRC solution, the nanofibers significantly prolonged the half life, and increased the bioavailability of VRC in rabbit tears. No obvious signs of irritation were observed after application in the conjunctival sac. VRC nanofibers are promising for ophthalmic drug delivery and further pharmacodynamics studies are needed.