Development of innovative electrospun nepafenac-loaded nanofibers-based ophthalmic inserts.

Chemical compounds studied in this article. Nepafenac (PubChem CID 151075); Polyvinyl alcohol (PubChem CID 11199); Poloxamer 407 (PubChem CID 24751); Chloroform (PubChem CID 6212); Methanol (PubChem CID 887); L-α-phosphatidylcholine (PubChem CID 10425706); Ethylenediaminetetraacetic acid (PubChem CID 6049). [Display omitted] • Electrospun nepafenac-loaded nanofibrous ophthalmic inserts were developed. • The composition has good cytocompatibility on hen chorioallantoic membrane. • The optimized formula was comparable to Nevanac® in term of corneal permeation. • Accelerated stability test under stressful conditions revealed stable nanofibers. • Electrospun nanofibers can be utilized as patient-centric ophthalmic formulations. 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. Nine different formulations were prepared by electrospinning and investigated for morphology, physicochemical properties, drug release, cytocompatibility, and in vitro and ex vivo permeability. The scanning electron microscopy images showed fibrous samples. Fourier transform infrared spectroscopy and X-ray diffraction confirmed the polymer cross-linking and the formation of amorphous solid dispersion. All formulations showed complete and fast release of nepafenac (≤60 min), and the release followed first-order kinetics (β values for all formulations were < 1). The formulations (F3, F6, and F9) showed considerable in vitro and ex vivo permeability. The Raman studies revealed comparable corneal distributions of F3 and the commercial Nevanac® suspension at 60 min (p value = 0.6433). The fibrous composition remains stable under stress conditions (40 ± 2 °C, 75 ± 5 % relative humidity). The formulation composition showed good cytocompatibility with hen eggs tested on the chorioallantoic membrane of chick embryos. The developed nanofiber webs could be a promising candidate for nepafenac-loaded ophthalmic inserts. [ABSTRACT FROM AUTHOR]