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Biomedicines 2018, 6(3), 92; https://doi.org/10.3390/biomedicines6030092

Aflibercept Nanoformulation Inhibits VEGF Expression in Ocular In Vitro Model: A Preliminary Report

1
Department of Pharmaceutical Sciences, College of Pharmacy, University of South Florida, Tampa, FL 33612, USA
2
Department of Ophthalmology, College of Medicine, University of Florida, Jacksonville, FL 32209, USA
*
Author to whom correspondence should be addressed.
Received: 8 August 2018 / Revised: 28 August 2018 / Accepted: 6 September 2018 / Published: 11 September 2018
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Abstract

Age-related macular degeneration (AMD) is one of the leading causes of blindness in the United States, affecting approximately 11 million patients. AMD is caused primarily by an upregulation of vascular endothelial growth factor (VEGF). In recent years, aflibercept injections have been used to combat VEGF. However, this treatment requires frequent intravitreal injections, leading to low patient compliance and several adverse side effects including scarring, increased intraocular pressure, and retinal detachment. Polymeric nanoparticles have demonstrated the ability to deliver a sustained release of drug, thereby reducing the necessary injection frequency. Aflibercept (AFL) was encapsulated in poly lactic-co-glycolic acid (PLGA) nanoparticles (NPs) via double emulsion diffusion. Scanning electron microscopy showed the NPs were spherical and dynamic light scattering demonstrated that they were uniformly distributed (PDI < 1). The encapsulation efficiency and drug loading were 75.76% and 7.76% respectively. In vitro release studies showed a sustained release of drug; 75% of drug was released by the NPs in seven days compared to the full payload released in 24 h by the AFL solution. Future ocular in vivo studies are needed to confirm the biological effects of the NPs. Preliminary studies of the proposed aflibercept NPs demonstrated high encapsulation efficiency, a sustained drug release profile, and ideal physical characteristics for AMD treatment. This drug delivery system is an excellent candidate for further characterization using an ocular neovascularization in vivo model. View Full-Text
Keywords: age-related macular degeneration; vascular endothelial growth factor; aflibercept; nanoparticles; PLGA age-related macular degeneration; vascular endothelial growth factor; aflibercept; nanoparticles; PLGA
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).
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Kelly, S.J.; Hirani, A.; Shahidadpury, V.; Solanki, A.; Halasz, K.; Varghese Gupta, S.; Madow, B.; Sutariya, V. Aflibercept Nanoformulation Inhibits VEGF Expression in Ocular In Vitro Model: A Preliminary Report. Biomedicines 2018, 6, 92.

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