Abstract
In this study, a novel brain targeting ascorbic acid (AA) derivative with "lock-in" function was designed and synthesized as a liposome ligand to prepare novel liposomes to achieve the effective delivery of drug formulations to brain via glucose transporter 1 (GLUT1) and the Na+-dependent vitamin C transporter (SVCT2). The liposome was prepared and characterized in terms of the particle size, zeta potential, encapsulation efficiency, release profile, stability, hemolysis and cell cytotoxicity. The preliminary evaluation in vivo demonstrated that the AA-thiamine disulfide system (TDS)-coated liposome had an improved targeting ability and significantly increased the brain concentration of docetaxel (DTX) as compared to the naked docetaxel, the non-coated and the AA-coated liposomes. The relative uptake efficiency and concentration efficiency were enhanced by 3.24- and 5.62-fold compared to that of the naked docetaxel, respectively. Both distribution data and pharmacokinetic parameters suggested that the ascorbic acid thiamine disulfide delivery system was a promising carrier to enhance central nervous system (CNS) drug's delivery ability into brain.
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