A major challenge for treatment of neurodegenerative disorders is the need to overcome the restrictive mechanism of the blood-brain-barrier (BBB) for delivery of therapeutic agents into the brain. Our goal was to develop an efficient nanoparticle-based system with the ability to bypass the BBB by targeting insulin receptors. We demonstrate that insulincoated gold-nanoparticles (INS-GNPs) can serve as an effective endogenous BBB transport system for delivering therapeutics into the brain. We further conducted a quantitative in-vivo investigation of the effect of nanoparticle size (20, 50 and 70nm) on the ability of INS-GNPs to cross the BBB. The most widespread bio-distribution and highest accumulation within the brain (5% of the injected dose) was observed using 20nm INS-GNPs, two hours post-injection. In-vivo CT imaging revealed that particles migrated to specific brain regions, rich in insulin receptors, which are important targets for the treatment of various neurodegenerative disorders. The findings described herein suggest the potential beneficial use of INS-GNPs as nano-vehicles for the transport of drugs through the BBB.