Convergent synthesis and characterization of fatty acid-conjugated poly(ethylene glycol)-block-poly(epsilon-caprolactone) nanoparticles for improved drug delivery to the brain

Abstract Herein, for the first time, we report the synthesis, preparation, and characterization of fatty acid-conjugated poly(ethylene glycol)-block-poly(epsilon-caprolactone) nanoparticles (FA-NPs), with the ultimate goal of improving drug delivery to the brain. These nanoparticles had a nano-size ( 5.4 × 10 5 x. They showed moderate stability in serum and exhibited zero-order drug release. As a proof-of-concept, the brain uptake of oleic acid-NPs (OA-NPs) was examined in rats after intravenous injections. Relative to 1% DMSO and PEG-NPs formulations, the OA-NPs enhanced the brain accumulation of the loaded cargo by 4.28 and 1.94x, respectively. Apparently, these nanoparticles hold considerable promise in drug delivery to the brain and their potential applications for disorders of the central nervous system should be explored.