cR10-modified liposomes for efficient topical delivery of lenvatinib to the posterior segment: Enhanced suppression of choroidal neovascularization
- Int J Pharm. 2026 Jul 10:700:127029. doi: 10.1016/j.ijpharm.2026.127029.
- 1. Zhejiang University, Eye Center of Second Affiliated Hospital, School of Medicine, Zhejiang Provincial Key Laboratory of Ophthalmology, Zhejiang Provincial Clinical Research Center for Eye Diseases, Zhejiang Provincial Engineering Institute on Eye Diseases, China.
- 2. State Key Laboratory of Advanced Drug Delivery and Release Systems, School of Pharmacy, Zhejiang University, Hangzhou 310058, China.
- 3. Zhejiang University, Eye Center of Second Affiliated Hospital, School of Medicine, Zhejiang Provincial Key Laboratory of Ophthalmology, Zhejiang Provincial Clinical Research Center for Eye Diseases, Zhejiang Provincial Engineering Institute on Eye Diseases, China. Electronic address: [email protected].
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.