earticle

영어

Choroidal neovascularization (CNV) is the primary cause of visual defect for the most of patients severely suffering from age-related macular degeneration (AMD). Recent research on drug delivery to the choroid where CNV originates demonstrates that has limitation on a drug penetrated into the outer retina. The objective of this study was to improve a drug delivery system for an integrin-antagonist peptide to the sub-retinal region. We developed nanoparticles that were fabricated by blending polylactic acid/polylactic acid-polyethylene oxide(PLA/PLA-PEO), and water-soluble integrin-antagonist peptide, C16Y, were encapsulated in nanoparticles(C16Y-NP). The PLA/PLA-PEO nanoparticles were 302 ± 85. 1-sized and continuously released C16Y encapsulated into NPs for over 2 weeks in in vitro. The nanoparticles did not exhibit any retinal toxicity as examined by histopathology. Either C16Y-NPs or C16Y peptide solution were separately injected to rodent models 5 or 9 days post laser photocoagulation. Both intravitreal injections of C16Y peptide and C16Y-NPs statistically suppressed CNV (p<0.05) at 5days and 9 days post laser photocoagulation. In the case of C16Y-NPs injection on day 12, however, the area of choroidal neovascularization on the day 12 was smaller than single injection of C16Y peptide solution (p<0.05) due to the short half-life in vitreous body. The result in this paper indicates that sustained release type of drug delivery is important to treat CNV derived from AMD. The intravitreally administered PLA/PLA-PEO nanoparticles encapsulating coumarin were revealed to penetrate the retina and localize to the RPE. These results propose that nanoparticles fabricated by biodegradable polymers are promising materials as carrier and potential drug delivery system may be established for treatment of AMD.