International journal of pharmaceutics · 2026
cR10-modified liposomes for efficient topical delivery of lenvatinib to the posterior segment: Enhanced suppression of choroidal neovascularization.
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Xie Youxuan, Zhang Xiuwen, Yin Qichuan, Chen Ruoqi, Chen Fuyao, Huang Yuxin, Shentu Xingchao
Аннотация
Choroidal neovascularization (CNV) is a key pathological process underlying multiple retinal diseases and remains difficult to treat due to physiological barriers that limit drug delivery to the posterior segment of the eye. Current anti-vascular endothelial growth factor (VEGF) therapies rely on intravitreal injection, which is invasive and associated with potential complications. lenvatinib, a multi-targeted tyrosine kinase inhibitor, exhibits potent anti-angiogenic activity; however, its poor aqueous solubility and limited ocular bioavailability restrict its ophthalmic application. In this study, cR10-modified lenvatinib-loaded liposomes (cR10-LL) were developed to improve topical ocular delivery. The physicochemical properties, encapsulation efficiency, and stability of the liposomal formulation were systematically characterized. In vitro cellular studies demonstrated that cR10 modification significantly enhanced cellular uptake and improved the inhibitory effects on endothelial cell migration and tube formation. In a choroidal neovascularization animal model, topical administration of cR10-LL effectively suppressed neovascular lesion formation and reduced vascular leakage. Ocular distribution studies further confirmed improved drug penetration into posterior ocular tissues, while biocompatibility assessments indicated favorable safety. Overall, these results suggest that cR10-LL represent a promising non-invasive drug delivery strategy for the treatment of CNV.