Stability, Cytotoxicity, and Retinal Pigment Epithelial Cell Binding of Hyaluronic Acid-Coated PLGA Nanoparticles Encapsulating Lutein

Abstract

The application of lutein was limited due to water insolubility and susceptible to heat and light degradation. In this study, hyaluronic acid (HA)-coated PLGA nanoparticles encapsulating lutein were fabricated by a solvent displacement method to improve the physicochemical properties and the stability of lutein. A biphasic release profile of lutein was observed, following zero-order release kinetics. The physical stability of lutein stored at 4°C, 30°C, and 40°C for 30 days was enhanced when lutein was encapsulated in the nanoparticles. The degradation of lutein in PLGA NPs coated with HA was fitted to a second-order kinetic model. The rate constant increased with increasing storage temperature. The activation energy of lutein-NPs was 63.26 kJ/mol. The half-lives of lutein in PLGA-NPs were about 49, 4, and 2 days at a storage temperature of 4°C, 30°C, and 40°C, respectively. The results suggested that lutein-NPs should be stored at 4°C to prevent physical and chemical degradation. The photodegradation of lutein in NPs followed a second-order kinetic model. The rate constant was 0.0155 mg -1 ml day -1 . Cell viability study revealed that HA-coated PLGA nanoparticles encapsulating lutein did not show toxicity against retinal pigment epithelial cells (ARPE-19). The NPs bound ARPE-19 cells in a time- and a dose-dependent manner. The binding efficiency of lutein-NPs decreased at higher concentrations, suggesting that the NPs might reach binding saturation capacity. In conclusion, HA-coated PLGA nanoparticles could be used to deliver lutein and improved physicochemical property of lutein. [Figure not available: see fulltext.]. © 2018, American Association of Pharmaceutical Scientists.