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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.

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



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


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


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.


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


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.


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

[Indexed for MEDLINE]

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