文獻：聚乙二醇化殼聚糖-氟尿嘧啶偶合物的制備及體外釋放研究

作者：段萍萍，關鵬程，朱亮

文獻鏈接：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殼聚糖-氟尿嘧啶偶合物(5-FU-CS-mPEG),并考察其體外釋放性能.

方法以羧基化單甲氧基聚乙二醇(mPEG-COOH)與殼聚糖(CS)反應制得聚乙二醇單甲醚改性殼聚糖(mPEGCS),再與經(jīng)氯乙酸修飾的氟尿嘧啶(FUA)在1-乙基-(3-二甲基氨基丙基)碳酰二亞胺鹽酸鹽(EDC·HCl)/N-羥基琥珀酰亞胺(NHS)介導下與CS偶聯(lián),生成目標產(chǎn)物5-FU-CS-mPEG;用UV,1H-NMR,FT-IR對結(jié)構(gòu)進行表征;UV法計算前藥載藥量;采用動態(tài)透析法研究前藥釋放度.

結(jié)果經(jīng)結(jié)構(gòu)確證,成功合成了5-FU-CS-mPEG;經(jīng)1H-NMR計算mPEG的取代度為12.31%;載藥量為4.83%;大分子前藥在120 h的累積釋放量為57%.結(jié)論 5-FU-CS-mPEG具有一定的緩釋作用.

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