Development of α-tocopherol nanomicellar formulation using polyethylene glycol monostearate for the oxidative stress-related disease

Abstract α-Tocopherol (Toc), one isoform of vitamin E, reportedly possesses diverse biological functions, including antioxidant and anticancer activities. However, therapeutic applications of Toc are considerably limited owing to poor solubility in aqueous media. In this study, a new intravenous Toc-containing micellar formulation was developed using polyethylene glycol monostearate (stPEG). The micellar formulations (stPEG/Toc micelles) were prepared using five different stPEGs with 10, 25, 40, 55, and 140 polyethylene glycol repeat units. The stPEG25-140/Toc micelles demonstrated extremely high-water solubility. Furthermore, micellar properties, including Toc content, particle size, zeta potential, stability, and biodistribution, were measured. Finally, the in vitro and in vivo antioxidant characteristics of these micelles were measured using the 2,2-diphenyl-1-picrylhydrazyl method and acetaminophen-induced oxidative stress mouse model, revealing that these micelles demonstrated antioxidant ability in a dose-dependent manner. In conclusion, the intravenous administration of the newly developed stPEG/Toc micellar formulations is potentially useful for the treatment of diseases associated with oxidative stress.