Lee, Jung Eun Kim, Koung Li Kim, Danbi Yeo, Yeongju Han, Hyounkoo Kim, Myung Goo Kim, Sun Hwa Kim, Hyuncheol Jeong, Ji Hoon Suh, Wonhee 2024-01-20T01:04:03Z 2024-01-20T01:04:03Z 2021-09-04 2017-07 1176-9114 https://pubs.kist.re.kr/handle/201004/122602 Pathological angiogenesis is one of the major symptoms of severe ocular diseases, including corneal neovascularization. The blockade of vascular endothelial growth factor (VEGF) action has been recognized as an efficient strategy for treating corneal neovascularization. In this study, we aimed to investigate whether nanoparticle-based delivery of apatinib, a novel and selective inhibitor of VEGF receptor 2, inhibits VEGF-mediated angiogenesis and suppresses experimental corneal neovascularization. Water-insoluble apatinib was encapsulated in nanoparticles composed of human serum albumin (HSA)-conjugated polyethylene glycol (PEG). In vitro angiogenesis assays showed that apatinib-loaded HSA-PEG (Apa-HSA-PEG) nanoparticles potently inhibited VEGF-induced tube formation, scratch wounding migration, and proliferation of human endothelial cells. In a rat model of alkali burn injury-induced corneal neovascularization, a subconjunctival injection of Apa-HSA-PEG nanoparticles induced a significant decrease in neovascularization compared to that observed with an injection of free apatinib solution or phosphate-buffered saline. An in vivo distribution study using HSA-PEG nanoparticles loaded with fluorescent hydrophobic model drugs revealed the presence of a substantial number of nanoparticles in the corneal stroma within 24 h after injection. These in vitro and in vivo results demonstrate that apatinib-loaded nanoparticles may be promising for the prevention and treatment of corneal neovascularization-related ocular disorders. English DOVE MEDICAL PRESS LTD TYROSINE KINASE INHIBITOR SUBCONJUNCTIVAL BEVACIZUMAB INJECTION RECURRENT PTERYGIUM TOPICAL BEVACIZUMAB VEGF RECEPTOR-1 EXPRESSION ALBUMIN A patinib-loaded nanoparticles suppress vascular endothelial growth factor-induced angiogenesis and experimental corneal neovascularization Article 10.2147/IJN.S135133 1 INTERNATIONAL JOURNAL OF NANOMEDICINE, v.12, pp.4813 - 4822 INTERNATIONAL JOURNAL OF NANOMEDICINE 12 4813 4822 scie scopus 000404891700002 2-s2.0-85023620763 Nanoscience & Nanotechnology Pharmacology & Pharmacy Science & Technology - Other Topics Pharmacology & Pharmacy Article TYROSINE KINASE INHIBITOR SUBCONJUNCTIVAL BEVACIZUMAB INJECTION RECURRENT PTERYGIUM TOPICAL BEVACIZUMAB VEGF RECEPTOR-1 EXPRESSION ALBUMIN apatinib corneal neovascularization nanoparticle vascular endothelial growth factor