Development of Poly Lactic/Glycolic Acid (PLGA) Microspheres for Controlled Release of Rho-Associated Kinase Inhibitor

Purpose. the purpose of this study was to investigate the feasibility of poly lactic/glycolic acid (plga) as a drug delivery carrier of rho kinase (rock) inhibitor for the treatment of corneal endothelial disease. method. rock inhibitor y-27632 and plga were dissolved in water with or without gelatin (w1),and a double emulsion [(w1/o)/w2] was formed with dichloromethane (o) and polyvinyl alcohol (w2). drug release curve was obtained by evaluating the released y-27632 by using high performance liquid chromatography. plga was injected into the anterior chamber or subconjunctiva in rabbit eyes,and ocular complication was evaluated by slitlamp microscope and histological analysis. results. y-27632 incorporated plga microspheres with different molecular weights,and different composition ratios of lactic acid and glycolic acid were fabricated. a high molecular weight and low content of glycolic acid produced a slower and longer release. the y-27632 released from plga microspheres significantly promoted the cell proliferation of cultured corneal endothelial cells. the injection of plga did not induce any evident eye complication. conclusions. rock inhibitor-incorporated plga microspheres were fabricated,and the microspheres achieved the sustained release of rock inhibitor over 7-10 days in vitro. our data should encourage researchers to use plga microspheres for treating corneal endothelial diseases. © 2017 sho koda et al.