【摘 要】
：
Gemcitabine (GEM) is a nucleoside analogue anticancer agent which acts against a wide range of solid tumors such as pancreatic,bladder,non-small lung and br
【机 构】
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Key Laboratory of Biomedical Polymers of Ministry of Education,Department of Chemistry,Wuhan Univers
【出 处】
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The Third Symposium on Innovative Polymers for Controlled De
论文部分内容阅读
Gemcitabine (GEM) is a nucleoside analogue anticancer agent which acts against a wide range of solid tumors such as pancreatic,bladder,non-small lung and breast cancers.It is known to be rapidly de-aminated to the inactive form by cytidine deaminase (CDA) in blood.Chemical modifications of gemcitabine,particularly on two sites of the molecule (4-(N)-and 5-sites),have been performed to improve the plasma half life of GEM.For example,modifications of the 4-(N)-position of gemcitabine with valeroyl,heptanoyl,lauroyl,and stearoyl linear acyl derivatives confer protection to gemcitabine from deamination by cytidine deaminase,leading to improved stability [1].However,the conversion of GEM to lipophilic derivatives also brings some drawbacks such as a very limited watersolubility.Lipophilic GEM prodrugs have been encapsulated into liposomes or particulate carriers [2].
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