Enhanced Brain Targeting of Tegafur Using Novel Lactyl Cholesterol Liposome as a Carrier

A series of lactyl cholesterols as targeting liposome ligands for brain-specific delivery were synthesized. The lactic acid protected by benzyl group was coupled with cholesteryl oligoethylene carboxylate derivatives 3, then deprotected in tetrahydrofuran by Pd/C with H2 to obtain the title compounds La-Lf. As a model drug, tegafur was entrapped by liposmes and lipsomes coated with these ligands for in vivo study, which showed that the ligand could enhance the ability of liposome delivering tegafur across the blood-brain barrier.