Gold nanoparticles with a core size of 2nm covalently coated with glycans to maintain solubility, targeting molecules for brain endothelium, and cargo molecules hold great potential for delivery of therapies into the CNS. They have low toxicity, pass through brain endothelium in vitro and in vivo, and move rapidly through the brain parenchyma. Within minutes of infusion the nanoparticles can be detected in neurons and glia. These nanoparticles are relatively easy to synthesize in association with their surface ligands. They can be detected by electron microscopy, ICP-mass spectrometry, and spectroscopy. However, modification of the basic gold nanoparticle is required for in vivo imaging by MR or radioactive methods. Depending on their surface coat, the nanoparticles cross the brain endothelium by the plasma membrane/cytosolic route (passive transport) or by vesicular transcytosis (active transport). A primary aim of current research is to improve the biodistribution of the nanoparticles for CNS drug delivery. Smaller gold nanoparticles are removed rapidly via the kidney, while larger nanoparticles are taken up by mononuclear phagocytes in various tissues. Receptors selectively located on brain endothelium can act as targets for the nanoparticles, to increase their delivery to the brain.
Keywords: Blood–brain barrier; Brain endothelium; Central nervous system; Gold nanoparticles; Nanocarriers.
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