Self-assembly of glutamic acid linked paclitaxel dimers into nanoparticles for chemotherapy

Zhanfeng Wang,Miao Zhuang,Tingting Sun,Xin Wang,Zhigang Xie

doi:10.1016/j.bmcl.2017.03.101

Self-assembly of glutamic acid linked paclitaxel dimers into nanoparticles for chemotherapy

Zhanfeng Wang, Miao Zhuang + Show 3 more

https://doi.org/10.1016/j.bmcl.2017.03.101

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Journal: Bioorganic & Medicinal Chemistry Letters	Publication Date: Apr 3, 2017
Citations: 15

Affiliation: Union Hospital, Jilin University, State Key Laboratory of Polymer Physics and Chemistry, Chinese Academy of Sciences, Changchun Institute of Applied Chemistry, University of Chinese Academy of Sciences, First Hospital of Jilin University

#Paclitaxel #Confocal Laser Scanning Microscopy + Show 8 more

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Abstract

In this work, a glutamic acid linked paclitaxel (PTX) dimer (Glu-PTX2) with high PTX content of 88.9wt% was designed and synthesized. Glu-PTX2 could self-assemble into nanoparticles (Glu-PTX2 NPs) in aqueous solution to increase the water solubility of PTX. Glu-PTX2 NPs were characterized by electron microscopy and dynamic light scattering, exhibiting spherical morphology and favorable structural stability in aqueous media. Glu-PTX2 NPs could be internalized by cancer cells as revealed by confocal laser scanning microscopy and exert potent cytotoxicity. It is envisaged that Glu-PTX2 NPs would be an alternative formulation for PTX, and such amino acid linked drug dimers could also be applied to other therapeutic agents.

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