Chemo-Enzymatic Synthesis of Glycolyl-Ester-Linked Taxol-Monosaccharide Conjugate and Its Drug Delivery System Using Hepatitis B Virus Envelope L Bio-Nanocapsules

Chemo-enzymatic synthesis of glycolyl-ester-linked taxol-glucose conjugate, ie, 7-glycolyltaxol 2"-O-α-D-glucoside, was achieved by using α-glucosidase as a biocatalyst. The water-solubility of 7-glycolyltaxol 2"-O-α-D-glucoside (21 μM) was 53 fold higher than that of taxol. The hepatitis B virus envelope L particles (bio-nanocapsules) are effective for delivering 7-glycolyltaxol 2"-O-α-D-glucoside to human hepatocellular carcinoma NuE cells.