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

Utilization of Apatinib-Loaded Nanoparticles for the Treatment of Ocular Neovascularization. Curr Drug Deliv. 2018 Oct 16;: Authors: Halasz K, Kelly SJ, Iqbal MT, Pathak Y, Sutariya V Abstract 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 sustainability of apatinib-loaded nanoparticles versus free apatinib solution. Cell viability and VEGFA and VEGFR2 expression was analyzed in animal retinal pigment epithelial (ARPE-19) cells and 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. PMID: 30332959 [PubMed - as supplied by publisher]
Source: Current Drug Delivery - Category: Drugs & Pharmacology Authors: Tags: Curr Drug Deliv Source Type: research