Abstract

Synthesis of ester-linked glucoside conjugate of docetaxel, 7-propionyldocetaxel 3''- O-α-D-glucopyranoside, was carried out by chemo-enzymatic procedures. The EE and LE values for hybrid-bio-nanocapsules of 7-propionyldocetaxel 3''- O-α-D-glucopyranoside were much improved rather than those of docetaxel. The hybrid-bio-nanocapsules targeted with trastuzumab and cetuximab, which contained 7-propionyldocetaxel 3''- O-α-D-glucopyranoside, showed high in vivo anti-cancer activity, ie, effective suppression of tumor growth, respectively.

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