Abstract: The main purpose of this study was to facilitate the delivery of kynurenic acid (KYNA) across the blood–
brain barrier (BBB) by applying micelles as nanoscale containers. Non-ionic amphiphilic molecules were used for
preparation of spherical micelles for delivery of kynurenic acid in aqueous solution in physiological condition. It was
established that Triton X 100 and Lutensol AP 20 nonionic surfactants are able to produce stable nanocontainers
for delivery of kynurenic acid molecules. The incorporation of KYNA molecules was investigated by dynamic
light scattering and the size of micelles were calculated between 5 and 10 nm in 150 mM NaCl and pH 7.5–7.6
solutions. Encapsulated kynurenic acid showed a significantly higher blood–brain barrier permeability compared
with non-encapsulated kynurenic acid. The in vivo experiments showed that the encapsulated kynurenic acid is able
to display effects within the central nervous system, even after its peripheral administration.