Chemo-enzymatic Synthesis of Ester-Linked Docetaxel-Glycoside Conjugate and its Drug Delivery System Using Hybrid-Bio-Nanocapsules Targeted With Trastuzumab and Cetuximab

Yuya Fujitaka, Hiroki Hamada, Hatsuyuki Hamada, Noriyoshi Masuoka, Kei Shimoda, Daisuke Uesugi, Takafumi Iwaki, Atsuhito Kuboki, Kohji Ishihara, Yuya Kiriake

Synthesis of ester-linked glucoside conjugate of docetaxel, 7-propionyldocetaxel 3"-O-α-D-glucopyranoside, was carried out by chemo-enzymic 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, resp. 

Natural Product Communications

Sage Journals

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