Anti-Angiogenic Nanomicelles For the Topical Delivery of Aflibercept to Treat Retinal Neovascular Disease.

Abstract

The traditional intravitreal injection delivery of anti-vascular endothelial growth factor (anti-VEGF) to the posterior segment of the eye for treatment of retinal diseases is invasive and associated with sight-threatening complications. To avoid such complications, there has been significant interest in developing polymers for topical drug delivery to the retina. This study reports a nanomicelle drug delivery system made of a co-polymer EPC (nEPCs), which is capable of delivering aflibercept to the posterior segment topically through corneal-scleral routes. EPC is comprised of polyethylene glycol (PEG), polypropylglycol (PPG) and polycaprolactone (PCL) segments. In this study, aflibercept-loaded nEPCs (nEPCs+A) is capable of penetrating the cornea in ex-vivo porcine eye models and deliver a clinically significant amount of aflibercept to the retina of laser-induced choroidal neovascularisation (CNV) murine models, causing CNV regression. nEPCs+A also demonstrates biocompatibility in-vitro and in-vivo. Interestingly, this study also suggests that nEPCs have intrinsic anti-angiogenic properties. The ability to deliver anti-VEGF drugs and the intrinsic anti-angiogenic properties of nEPCs may result in synergistic effects which can be harnessed for effective therapeutics. nEPCs may be a promising topical anti-VEGF delivery platform for the treatment of retinal diseases. This article is protected by copyright. All rights reserved.