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	Water-Soluble Poly(ethylene glycol) Prodrug of Pemetrexed: Synthesis, Characterization, and Preliminary Cytotoxicity
	Min, Tao ; Ye, Hai ; Zhang, Peng ; Liu, Jun ; Zhang, Can ; Shen, Wenbin ; Wang, Wan ; Shen, Longsheng
	2010-05-11 ; 2010-05-11
关键词	conjugated polymers drug delivery systems hydrophilic polymers water-soluble polymers synthesis Polymer Science
中文摘要	Pemetrexed is a novel antifolate of antimetabolite with multiple enzyme targets involved in both pyrimidine and purine synthesis. It has entered the clinical usage due to favorable profiles especially in the cancer treatment of mesothelioma and non-small-cell lung carcinoma. But it presents numerous challenges associated with poor water solubility and unstability in its original form of glutamic acid. The aim of this study is to solubilize pemetrexed by designing and synthesizing its aqueous-soluble prodrug using high aqueous-soluble polymeric carrier poly(ethylene glycol) (PEG). A new type of soluble pemetrexed prodrug was synthesized with dihydroxyl PEG and a single amino acid linkage, and was extensively characterized using H-1-NMR, C-13-NMR, Fourier-transform infrared, and matrix-assisted laser desorption time of flight mass spectrometry. In addition, the prodrugs were evaluated for the drug loading capability, the aqueous solubility, and the preliminary in vitro cytotoxicity. The results indicate that the new PEGylated pemetrexed conjugates possess enhanced water solubility and stability, and provide another feasible choice of the pharmaceutical form of pemetrexed in the clinical application. (C) 2008 Wiley Periodicals, Inc. J Appl Polym Sci 111: 444-451, 2009
语种	英语 ; 英语
出版者	JOHN WILEY & SONS INC ; HOBOKEN ; 111 RIVER ST, HOBOKEN, NJ 07030 USA
内容类型	期刊论文
源URL	[http://hdl.handle.net/123456789/26858]
专题	清华大学
推荐引用方式 GB/T 7714	Min, Tao,Ye, Hai,Zhang, Peng,et al. Water-Soluble Poly(ethylene glycol) Prodrug of Pemetrexed: Synthesis, Characterization, and Preliminary Cytotoxicity[J],2010, 2010.
APA	Min, Tao.,Ye, Hai.,Zhang, Peng.,Liu, Jun.,Zhang, Can.,...&Shen, Longsheng.(2010).Water-Soluble Poly(ethylene glycol) Prodrug of Pemetrexed: Synthesis, Characterization, and Preliminary Cytotoxicity..
MLA	Min, Tao,et al."Water-Soluble Poly(ethylene glycol) Prodrug of Pemetrexed: Synthesis, Characterization, and Preliminary Cytotoxicity".(2010).

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