Anti‐VEGF‐Aptamer Modified C‐Dots—A Hybrid Nanocomposite for Topical Treatment of Ocular Vascular Disorders

The vascular endothelial growth factor (VEGF) induces pathological angiogenetic ocular diseases. It is a scientific challenge to develop carriers for the controlled release of inhibitors for VEGF present in the back of the eye domain. Carbon dots (C‐dots) functionalized with the VEGF aptamer are int...

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Bibliographic Details
Published in:Small (Weinheim an der Bergstrasse, Germany) Germany), 2019-10, Vol.15 (40), p.e1902776-n/a
Main Authors: Shoval, Asaf, Markus, Amos, Zhou, Zhixin, Liu, Xia, Cazelles, Rémi, Willner, Itamar, Mandel, Yossi
Format: Article
Language:English
Subjects:
age‐related macular degeneration (AMD)
Biocompatibility
Blood vessels
Carbon dots
Controlled release
Cornea
Diabetic retinopathy
drug carriers
Eye diseases
Fluorescence
Growth factors
Monoclonal antibodies
Nanocomposites
Nanomaterials
nanomedicines
Nanoparticles
Nanotechnology
Toxicity
Vascular endothelial growth factor
vascular endothelial growth factor (VEGF)
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Summary:The vascular endothelial growth factor (VEGF) induces pathological angiogenetic ocular diseases. It is a scientific challenge to develop carriers for the controlled release of inhibitors for VEGF present in the back of the eye domain. Carbon dots (C‐dots) functionalized with the VEGF aptamer are introduced and the hybrid nanoparticles are used for ocular nanomedicine. The C‐dots are applied as effective carriers of the anti‐VEGF aptamer across the cornea, yielding therapeutic levels upon topical administration. The hybrids show no toxicity for both in vitro and in vivo murine animal model, and further enable noninvasive intraocular concentration monitoring through the C‐dots inherent fluorescence. In addition, the hybrid C‐dots effectively inhibit VEGF‐stimulated angiogenesis in choroidal blood vessels. This inhibition is comparable to two commercially available anti‐VEGF drugs, bevacizumab and aflibercept. The hybrid aptamer‐modified C‐dots provide a versatile nanomaterial to treat age‐related macular degeneration and diabetic retinopathy. Age‐related macular degeneration and diabetic retinopathy are macular diseases induced by the vascular endothelial growth factor (VEGF). Nontoxic anti‐VEGF aptamer‐functionalized C‐dots penetrate the cornea into the intravitreal space, where the VEGF‐driven angiogenesis is effectively inhibited. The aptamer C‐dots conjugates provide promising therapeutic materials for ocular nanomedicines.
ISSN:1613-6810
1613-6829
DOI:10.1002/smll.201902776