Background/Objectives: Fungal keratitis remains a vision-threatening infection, and current amphotericin B (AmphB) eye drops suffer from low corneal residence time, poor aqueous solubility, and the need for frequent dosing. This study develops electrospun nanofiber-based ophthalmic inserts combining polyvinyl alcohol (PVA), gamma-cyclodextrin (γ-CD), and sodium taurocholate (STC) to enhance AmphB solubility and provide a non-invasive, rapidly dissolving ophthalmic dosage form. Methods: γ-CD and STC-enhanced AmphB-loaded PVA nanofiber-based ophthalmic inserts with varying γ-CD and STC concentrations were prepared by electrospinning and characterized by scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FTIR), and X-ray diffraction (XRD). Drug content, in vitro release (Weibull modeling), antifungal activity against Candida albicans, Fusarium solani, and Aspergillus fumigatus, ocular cytocompatibility using the Hen’s Egg Test on Chorioallantoic Membrane (HET-CAM), and accelerated stability (40 ± 2 °C, 75 ± 5% relative humidity, 4 weeks) were evaluated. Results: Bead-free nanofibers with mean diameters between 216 ± 33 nm and 310 ± 35 nm were obtained, and XRD confirmed complete amorphization of AmphB within the PVA nanofiber matrix, forming an amorphous solid dispersion. All formulations showed rapid and nearly complete AmphB release (≈100% within 60 min), with Weibull β values < 0.75, indicating Fickian diffusion-controlled release. AmphB-loaded PVA nanofiber-based ophthalmic inserts produced inhibition zones and broth susceptibility profiles comparable to AmphB in dimethyl sulfoxide (DMSO), demonstrating preserved antifungal activity. HET-CAM scores (0–0.9) classified the inserts as practically non-irritant, and SEM/FTIR after accelerated storage showed no relevant morphological or physicochemical changes. Conclusions: These γ-CD and STC-enhanced AmphB-loaded PVA nanofiber-based ophthalmic inserts provide a non-invasive, rapidly dissolving ophthalmic dosage form that combines amorphous AmphB, immediate drug availability, and good ocular tolerance, supporting their further development as a patient-friendly treatment option for fungal keratitis.
Omer et al. (Fri,) studied this question.