Phage-displayed peptide-conjugated biodegradable nanoparticles enhanced brain drug delivery

Abstract Drug distribution to the brain is one of the most difficult challenges in the treatment of the central nervous system (CNS) diseases due to the presence of the blood-brain barrier (BBB). To enhance brain-specific drug delivery, a cyclic peptide CRTIGPSVC selectively interacting with apo-transferrin (apo-Tf), was modified to the surface of poly (ethyleneglycol)–poly (lactide acid) (PEG-PLA) nanoparticles to yield a novel delivery system (Pep-NP). The in vitro cytotoxicity of the delivery system was low. The cellular uptake of Pep-NP was significantly higher than that of NP. Following intravenous administration, much more notable fluorescence was found in the mice brains with Pep-NP than NP. The results indicated the cyclic peptide modified nanoparticles system had great potential in drug delivery across the BBB, thus providing a safe approach for brain targeting.