Posted by Electrospun nanofibers can be utilized to develop patient-centric ophthalmic formulations with reasonable bioavailability at the targeted site. The current study aimed to develop 0.1 % w/w of nepafenac-loaded electrospun nanofibrous webs as potential candidates for ocular delivery of nepafenac with improved solubility and stability. Nepafenac (NEPA)/hydroxypropyl-beta-cyclodextrin (HPβCD), was loaded in different ratios of polyvinyl alcohol (PVA): Poloxamer 407 to get electrospinning solutions. Bead-free, randomly oriented fiber depositions and no gel droplets on the fibers’ surfaces, with fiber diameters ranging from 124 ± 20 nm to 464 ± 49 nm were obtained. The results reflect that the selected polymers (PVA/Poloxamer 407) and the drug complex (NEPA/HPβCD) are appropriate for fiber formation. The HPβCD not only improved the solubility of NEPA through inclusion complex formation, but also enhanced the spinnability of the precursor solution. SEM results showed that smooth fibers can be obtained. Formation of amorphous solid dispersion was confirmed by FTIR spectra and XRD analysis. The release and in vitro kinetics studies showed immediate release of the drug, which was characterized by the model-independent Weibull distribution. The porous feature of nanofiber webs, along with their high surface-to-volume ratio, resulted in rapid dissolution of the proposed ophthalmic inserts upon contact with the phosphate buffer solution. The permeability results showed a good penetration of the developed formulation to the corneal layers and the component of the developed polymeric matrix displayed a good compatibility with HET_CAM of fertilized chicken embryos. In conclusion, the obtained results reflect that the electrospun NEPA-loaded nanofibers-based ocular inserts could be a promising alternative to conventional systems with better bioavailability and stability.
Safaa Omer, Nándor Nagy, Emőke Szőcs, Szabina Kádár, Gergely Völgyi, Balázs Pinke, László Mészáros, Gábor Katona, Anna Vincze, Péter Dormán, Zoltán Zs. Nagy, György T. Balogh, Adrienn Kazsoki, Romána Zelkó (2023) Development of innovative electrospun nepafenac-loaded nanofibers-based ophthalmic inserts. International Journal of Pharmaceutics 647, 123554. https://doi.org/10.1016/j.ijpharm.2023.123554.