title: Self-assembly of glutamic acid linked paclitaxel dimers into nanoparticles for chemotherapy.
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-PTX2could self-assemble into nanoparticles (Glu-PTX2NPs) in aqueous solution to increase the water solubility of PTX. Glu-PTX2NPs were characterized by electron microscopy and dynamic light scattering, exhibiting spherical morphology and favorable structural stability in aqueous media. Glu-PTX2NPs could be internalized by cancer cells as revealed by confocal laser scanning microscopy and exert potent cytotoxicity. It is envisaged that Glu-PTX2NPs would be an alternative formulation for PTX, and such amino acid linked drug dimers could also be applied to other therapeutic agents.
authors.affiliation: Department of Neurosurgery, China-Japan Union Hospital of Jilin University, Changchun 130033, PR China.
authors.forename: Zhanfeng
authors.initials: Z
authors.lastname: Wang
authors.affiliation: Department of Neurosurgery, China-Japan Union Hospital of Jilin University, Changchun 130033, PR China.
authors.forename: Miao
authors.initials: M
authors.lastname: Zhuang
authors.affiliation: State Key Laboratory of Polymer Physics and Chemistry, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, 5625 Renmin Street, Changchun, Jilin 130022, PR China; University of Chinese Academy of Sciences, Beijing 100049, PR China. Electronic address: suntt@ciac.ac.cn.
authors.forename: Tingting
authors.initials: T
authors.lastname: Sun
authors.affiliation: Department of Thyroid Surgery, The First Hospital of Jilin University, 71 Xinmin Street, Changchun, Jilin 130021, PR China.
authors.forename: Xin
authors.initials: X
authors.lastname: Wang
authors.affiliation: State Key Laboratory of Polymer Physics and Chemistry, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, 5625 Renmin Street, Changchun, Jilin 130022, PR China.
authors.forename: Zhigang
authors.initials: Z
authors.lastname: Xie
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D002470:Cell Survival / Q000187:drug effects; D019281:Dimerization; D000067493:Dynamic Light Scattering; D018698:Glutamic Acid / Q000737:chemistry*; D006367:HeLa Cells; D006801:Humans; D061986:MCF-7 Cells; D018613:Microscopy, Confocal; D053758:Nanoparticles / Q000737:chemistry*; D017239:Paclitaxel / Q000737:chemistry*; D012995:Solubility
chemical_list: D000970:Antineoplastic Agents; D018698:Glutamic Acid; D017239:Paclitaxel
keywords: Chemotherapy; Glutamic acid; Nanomedicine; Paclitaxel dimers; Self-assembly