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Synthesis of ester-linked glycoside prodrug of taxol, i.e., 7-glycolyltaxol 2″- O-α-D-glucopyranoside, was investigated by chemical synthetic procedure. The encapsulation efficiency and loading efficiency of taxol for liposomes was much improved by modification with glucosyl ester group. The immunoliposomes containing the glycoside prodrug of taxol, i.e., 7-glycolyltaxol 2″- O-α-D-glucopyranoside, exhibited effective anti-tumor activities.

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Synthesis of Ester-linked Taxol-glycoside Conjugate and Its Application to Drug Delivery System Using Immunoliposome Targeted with Trastuzumab and Cetuximab