Abstract
Age-related macular degeneration (AMD) will be responsible for the vision impairment of more than five million late-aged adults in the next 30 years. Current treatment includes frequent intravitreal injections of anti-vascular endothelial growth factor (VEGF) agents. However, there are methods of drug delivery that can decrease the frequency of intravitreal injections by sustaining drug release. MPEG-PCL ((methoxypoly(ethylene glycol) poly(caprolactone)) has been reported as biocompatible and biodegradable. Polymeric micelles of MPEG-PCL can be useful in efficiently delivering anti-VEGF drugs such as sunitinib to the posterior segment of the eye. In this study, the novel micellar formulation exhibited an average dynamic light scattering (DLS) particle size of 134.2 ± 2.3 nm with a zeta potential of −0.159 ± 0.07 mV. TEM imaging further confirmed the nanoscopic size of the micelles. A sunitinib malate (SM)-MPEG-PCL formulation exhibited a sustained release profile for up to seven days with an overall release percentage of 95.56 ± 2.7%. In addition to their miniscule size, the SM-MPEG-PCL formulation showed minimal cytotoxicity onto the ARPE-19 human retinal pigment epithelial cell line, reporting a percent viability of more than 88% for all concentrations tested at time intervals of 24 h. The SM-MPEG-PCL micelles also exhibited exceptional performance during an anti-VEGF ELISA that decreased the overall VEGF protein expression in the cells across a 24–72 h period. Furthermore, it can be concluded that this type of polymeric vehicle is a promising solution to symptoms caused by AMD and improving the management of those suffering from AMD.
Highlights
Age-related macular degeneration (AMD) is an eye disease that gradually deteriorates the macula and is the leading causes of vision failure among late-aged adults [1,2]
The macula is located in the posterior segment of the eye near the retinal center, and it is a key component for central vision processing by using its photoreceptor cells [3]
Vascular endothelial growth factor (VEGF) is a protein that plays a major role in the formation of blood vessels within the eye in neovascular AMD
Summary
Age-related macular degeneration (AMD) is an eye disease that gradually deteriorates the macula and is the leading causes of vision failure among late-aged adults [1,2]. The macula is located in the posterior segment of the eye near the retinal center, and it is a key component for central vision processing by using its photoreceptor cells [3]. Vascular endothelial growth factor (VEGF) is a protein that plays a major role in the formation of blood vessels within the eye in neovascular AMD. Anti-VEGF drugs inhibit the expression of VEGF at the angiogenic site to prevent central vision damage induced by hyperoxic conditions [4]. Anti-VEGF drugs such as axitinib, pazopanib, and sorafenib are available for use in cancer treatments, but they recently have been propitious agents for treating AMD-induced neovascularization [5,6].
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