Synthesis and evaluation of glyco-coated liposomes as drug carriers for active targeting in drug delivery systems

•S-Glycosyl cholesterols were synthesized as targeting motifs for DDS.•Liposomes containing the glycosyl cholesterols were successfully prepared.•The liposomes were selectively taken up by liver and cancer cells.

Novel sugar-conjugated cholesterols, β-Gal-, α-Man-, β-Man-, α-Fuc-, and β-Man-6P-S-β-Ala-Chol, were synthesized and incorporated into liposomes. In vitro experiments using the glyco-coated liposomes showed that the glyco-coated liposomes are efficiently taken up by cells expressing carbohydrate-binding receptors selectively. Glyco-coated liposomes are promising candidates for drug delivery vehicles.

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