Synthesis of Ester-linked Docetaxel-glycoside Conjugate and Its Application to Drug Delivery System using Immunoliposome Targeted with Trastuzumab.

Chemo-enzymatic synthesis of the ester-linked monosaccharide conjugate of docetaxel, 7-glycolyldocetaxel 2"-O-ß-D-galactopyranoside, was achieved by using lactase as a biocatalyst. The water-solubility and, EE and LE values for the liposome of 7-glycolyldocetaxel 2"-O-ß-D-galactopyranoside were much higher than those of docetaxel. The immunoliposome containing 7-glycolyldocetaxel 2"-O-ß-D-galactopyranoside showed effective suppression of tumor growth.