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Curr Drug Deliv. 2019;16(2):153-163. doi: 10.2174/1567201815666181017095708.

Utilization of Apatinib-Loaded Nanoparticles for the Treatment of Ocular Neovascularization.

Author information

1
Department of Pharmaceutical Sciences, College of Pharmacy, University of South Florida, Tampa, FL 33612, United States.
2
Faculty of Public Health, Universitas Airlangga, Surabaya, Indonesia.

Abstract

BACKGROUND:

The current treatment of ocular neovascularization requires frequent intravitreal injections of anti-vascular endothelial growth factor (VEGF) agents that cause severe side effects.

OBJECTIVE:

The purpose of this study is to prepare and characterize a novel nanoscale delivery system of apatinib for ocular neovascularization.

METHODS:

The optimized formulation showed a particle size of 135.04 nm, polydispersity index (PDI) of 0.28 ± 0.07, encapsulation efficiency (EE) of 65.92%, zeta potential (ZP) of -23.70 ± 8.69 mV, and pH of 6.49 ± 0.20. In vitro release was carried out to demonstrate a 3.13-fold increase in the sustainability of apatinib-loaded nanoparticles versus free apatinib solution.

RESULT:

Cell viability and VEGFA and VEGFR2 expression were analyzed in animal retinal pigment epithelial (ARPE-19) cells.

CONCLUSION:

The results confirmed the hypothesis that apatinib nanoparticles decreased toxicity (1.36 ± 0.74 fold) and efficient VEGF inhibition (3.51 ± 0.02 fold) via VEGFR2 mediation.

KEYWORDS:

Apatinib; nanoparticles; neovascularization; vascular endothelial growth factor receptor 2 (VEGFR2).; vascular endothelial growth factor (VEGF)

[Indexed for MEDLINE]

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