Development of PLGA-based biodegradable ocular drug delivery system for sustained release of anti-VEGF drug

Abstract

Intravitreal injection of anti-vascular endothelial growth factor (anti-VEGF) has been identified as an effective treatment for various ocular diseases such as wet age-related macular degeneration (AMD) and diabetic maculopathy in recent years. However, because of the high clearance rate and short half-life of anti-VEGF in human vitreous, the patients are required to receive monthly intravitreal injection to sustain the treatment effect. Not only the medical cost is increased due to multiple injections, but the patients are also subjected to the risk of multiple complications such as infection, retinal detachment, hemorrhage, and cataract. A drug delivery system for controlled and sustained release of anti-VEGF could potentially solve the problem. Poly(lactic-co-glycolic acid) (PLGA) is a biomaterial well-known of its good biocompatibility and biodegradability in physiological environment. In this study, three PLGA-based drug delivery systems, PLGA microparticles, PLGA mini capsules and PLGA microfibers, have been developed and their performance in drug encapsulation and release profile are evaluated. It is shown that each drug delivery system could encapsulate anti-VEGF with their specific properties and advantages. Further optimizations of each of the drug delivery systems are needed to improve the encapsulation capacity and prolong the release profile in order to reach the clinically useful level.