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
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.