Development of a naringenin microemulsion as a prospective ophthalmic delivery system for the treatment of corneal neovascularization: <i>in vitro</i> and <i>in vivo</i> evaluation

Yu Ma, Jingjing Yang, Yali Zhang, Chunyan Zheng, Zhen Liang, Ping Lü, Fei Song, Yuwei Wang, Junjie Zhang

Drug Delivery · 2021 · 30 citations · 35 references

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Abstract

corneal permeation study. Human corneal epithelial cells (HCECs) toxicity study showed no toxicity with NAR-ME, which is consistent with the result of ocular irritation study. NAR-ME had high bioavailability 1.45-fold, 2.15-fold, and 1.35-fold higher than NAR-Susp in the cornea, conjunctiva, and aqueous humor, respectively. Moreover, NAR-ME (0.5% NAR) presented efficacy comparable to that of dexamethasone (0.025%) in the inhibition of CNV in mice CNV model induced by alkali burning, resulting from the attenuation of corneal vascular endothelial growth factor (VEGF) and matrix metalloproteinase (MMP-14) expression. In conclusion, the optimized NAR-ME formulation demonstrated excellent physicochemical properties and good tolerance, enhanced ocular bioavailability and corneal permeability. This formulation is promising, safe, and effective for the treatment of CNV.

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