文献：聚乙二醇化壳聚糖-氟尿嘧啶偶合物的制备及体外释放研究

作者：段萍萍，关鹏程，朱亮

文献链接：https://xueshu.baidu.com/usercenter/paper/show?paperid=e8e9248d8a8308862e3f1644f0d08328&site=xueshu_se

Objective: To synthesize PEGylated chitosan fluorouracil conjugate (5-FU-CS-mPEG) and investigate its in vitro release properties

Method: Carboxylated monomethoxypolyethylene glycol (mPEG COOH) was reacted with chitosan (CS) to prepare polyethylene glycol monomethyl ether modified chitosan (mPEGCS), which was then coupled with chloroacetic acid modified fluorouracil (FUA) in the presence of 1-ethyl - (3-dimethylaminopropyl) carbodiimide hydrochloride (EDC · HCl)/N-hydroxysuccinimide (NHS) to form the target product 5-FU-CS-mPEG; Characterize the structure using UV, 1H-NMR, FT-IR; UV method for calculating prodrug loading; Using dynamic dialysis method to study prodrug release rate

As a result of structural confirmation, 5-FU-CS-mPEG was successfully synthesized; The degree of substitution of mPEG was calculated to be 12.31% by 1H-NMR; The drug loading capacity is 4.83%; The cumulative release of macromolecular prodrug at 120 hours is 57% Conclusion: 5-FU-CS-mPEG has a certain sustained release effect

目的合成聚乙二醇化壳聚糖-氟尿嘧啶偶合物(5-FU-CS-mPEG),并考察其体外释放性能.

方法以羧基化单甲氧基聚乙二醇(mPEG-COOH)与壳聚糖(CS)反应制得聚乙二醇单甲醚改性壳聚糖(mPEGCS),再与经氯乙酸修饰的氟尿嘧啶(FUA)在1-乙基-(3-二甲基氨基丙基)碳酰二亚胺盐酸盐(EDC·HCl)/N-羟基琥珀酰亚胺(NHS)介导下与CS偶联,生成目标产物5-FU-CS-mPEG;用UV,1H-NMR,FT-IR对结构进行表征;UV法计算前药载药量;采用动态透析法研究前药释放度.

结果经结构确证,成功合成了5-FU-CS-mPEG;经1H-NMR计算mPEG的取代度为12.31%;载药量为4.83%;大分子前药在120 h的累积释放量为57%.结论 5-FU-CS-mPEG具有一定的缓释作用.

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