Anti-VEGFR2 Antibody-modified Micelle for Triggered Drug Delivery and Effective Therapy of Choroidal Neovascularization

• Published in: Current neurovascular research Vol. 16; no. 3; p. 258
• Main Authors: Takahashi, Kei, Masuda, Tomomi, Harada, Mitsunori, Inoue, Tadashi, Nakamura, Shinsuke, Naito, Kenichiro, Hara, Hideaki, Shimazawa, Masamitsu
• Format: Journal Article
• Language: English
• Published: United Arab Emirates 01.01.2019
• Subjects: antibody-modified micelle; E7974; motesanib; drug delivery system; Age-related macular degeneration; choroidal neovascularization
• ISSN: 1875-5739
• DOI: 10.2174/1567202616666190619150956

This study aimed to examine whether DC101 (anti-VEGFR2 antibody)- modified micelles have applications as novel drug delivery devices, which allow small molecule antiangiogenic agents to deliver to angiogenic sites on a murine laser-induced choroidal neovascularization (CNV) model. CNV was induced by photocoagulation on the unilateral eye of each mouse under anesthesia. Immediately after laser coagulation, E7974-loaded DC101-modified micelles and motesanib-loaded DC101-modified micelles were intravitreally administrated. Two weeks after photocoagulation, CNV was visualized using fluorescein-conjugated dextran (MW=2,000 kDa), and the CNV area was measured in retinal pigment epithelium (RPE)-choroidal flat mounts. Intravitreal administration of both DC101-modified micelles loaded with E7974 at 2 µM and motesanib at 2 µM significantly reduced CNV area in the murine laser-induced CNV model at a clearly lower concentration than the effective dose of each agent. These results suggest that DC101-modified micelle might be effective drug carrier system for treating CNV and other ocular angiogenic diseases.