apatinib and Eye-Diseases

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.

Topics: Antineoplastic Agents; Cell Line; Drug Carriers; Eye Diseases; Humans; Nanoparticles; Neovascularization, Pathologic; Protein Kinase Inhibitors; Pyridines; Vascular Endothelial Growth Factor A; Vascular Endothelial Growth Factor Receptor-2