Design, Synthesis and In Vivo Evaluation of Sulfhydryl β-D-Glucose Cholesterols as Ligands for Brain Targeting Liposomes

A novel sulfhydryl-β-D-glucose cholesterol 10a-10f as ligand for brain targeting liposomes was designed and synthesized. 10e was applied to the preparation of liposomal delivery system for achieving the brain-targeted delivery of the model drug tegafur in mice utilizing the glucose transporter member 1 (GLUT1). The results suggest the feasibility to enhance liposomes ability of delivering drug to brain by using the designed compound as liposome ligands. Keywords: Blood-brain barrier, Liposome ligands, GLUT1, Brain-targeted delivery, Synthesis, Tegafur