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The choline transporter (ChT) is used to transporte choline‐derivate‐modified nanoparticles across the blood‐brain barrier. It is demonstrated that ChT is an ideal Trojan horse. The choline‐derivate‐modified nanoparticles exhibit higher permeability across the brain capillary endothelial cells (BCECs) monolayer in vitro and higher gene distribution and expression in vivo.
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