Abstract
The wet type of age-related macular degeneration (AMD) accompanies the subfoveal choroidal neovascularization (CNV) caused by the abnormal extension or remodeling of blood vessels to the macula and retinal pigment epithelium (RPE). Vascular endothelial growth factor (VEGF) is known to play a crucial role in the pathogenesis of the disease. In this study, we tried to repurpose an investigational anticancer drug, rivoceranib, which is a selective inhibitor of VEGF receptor-2 (VEGFR2), and evaluate the therapeutic potential of the drug for the treatment of wet-type AMD in a laser-induced CNV mouse model using microsphere-based sustained drug release formulations. The PLGA-based rivoceranib microsphere can carry out a sustained delivery of rivoceranib for 50 days. When administered intravitreally, the sustained microsphere formulation of rivoceranib effectively inhibited the formation of subfoveal neovascular lesions in mice.
Highlights
The dry or non-neovascular type of age-related macular degeneration (AMD) is more prevalent than wet or neovascular AMD, wet AMD is often involved with severely reduced vision acuity and vision loss which occurs when the outgrowth of blood vessels in the choroidal region extends underneath the foveal avascular zone (subfoveal choroidal neovascularization (CNV)) [4,5]
Blocking the Vascular endothelial growth factor (VEGF) signaling pathway to prevent CNV has been popularly employed for the treatment of wet AMD [7]
Monoclonal antibodies targeting VEGF receptors (VEGFR) such as bevacizumab and ranibizumab are frequently used for CNV due to their desirable effectiveness and low incidence of serious ocular and systemic adverse events [8]
Summary
Publisher’s Note: MDPI stays neutral with regard to jurisdictional claims in published maps and institutional affiliations. Monoclonal antibodies targeting VEGF receptors (VEGFR) such as bevacizumab and ranibizumab are frequently used for CNV due to their desirable effectiveness and low incidence of serious ocular and systemic adverse events [8]. Pharmaceutics 2021, 13, 1548 injectable implants containing corticosteroids such as dexamethasone and fluocinolone acetamide could achieve sustained drug release in vitreous space for an extended period. A selective inhibitor of VEGFR tyrosine kinase, could be repositioned as a candidate for an anti-VEGF therapy for CNV. Conjugate-based nanoparticles containing rivoceranib effectively reduced retinal vascular leakage and corneal neovascularization by blocking VEGF/VEGFR2 signaling [21,22]. Injectable microsphere dosage forms of rivoceranib were developed for extended drug release in the vitreous space. The potential therapeutic effect of the rivoceranib microspheres for wet AMD was evaluated in a laser-induced CNV animal model
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