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

INTERNATIONAL JOURNAL OF PHARMACEUTICS(2023)

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摘要
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 deliver y 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 e x 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. A l l formulations showed complete and fast release of nepafenac (<= 60 min), and the release followed first-order kinetics (beta values for al l 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 (R) suspension at 60 min (p value = 0.6433). The fibrous composition remains stable under stress conditions (40 +/- 2 degrees 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.
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关键词
Nepafenac-loaded formulation s,Electrospun nanofiber-based ocular insert,Morphological and solid-state characterization,Cytocompatibility study,In vitro dissolution study,Accelerated stability test,Ex vivo permeability study
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