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

• Published in: Current drug delivery Vol. 16; no. 2; p. 153
• Main Authors: Halasz, Kathleen, Kelly, Shannon J, Iqbal, Muhammad Tajwar, Pathak, Yashwant, Sutariya, Vijaykumar
• Format: Journal Article
• Language: English
• Published: United Arab Emirates 01.01.2019
• Subjects: Apatinib; vascular endothelial growth factor (VEGF); vascular endothelial growth factor receptor 2 (VEGFR2); nanoparticles; neovascularization
• ISSN: 1875-5704
• DOI: 10.2174/1567201815666181017095708

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.