摘要
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。
Objective To synthesize a prodrug named N-methoxy poly （ethylene glycol ）-grafted-chitosan-5- fluorouracil acetic acid conjugate, and study its release in vitro. Methods mPEG-COOH was firstly combined with chitosan, and then reacted with 5-fluorouracil aceticaeid （FUA） modified with chloroaeetie acid by 1-ethyl- 3 （3-dimethyllaminopropyl） earbodiie hydrochlide （ EDC ~ HC1 ）/N-hydroxysueeinimide （NHS）. The structures were identified by UV, 1H-NMR and FT-IR. The re^ease of the 5-FU-CS-mPEG in vitro was evaluated by using a dialysis method. Results After determination, the reaction product was 5-FU-CS-mPEG. The degrees of substitution of mPEG were 12.31% ,and the drug-loading rate was 4.83%. The total release was 57% in 120 h. Conclusion 5-FU-CS-mPEG can be used as a new carrier for sustained release drug systems.
出处
《广东药学院学报》
CAS
2013年第6期579-583,共5页
Academic Journal of Guangdong College of Pharmacy
关键词
氟尿嘧啶
大分子前药
表征
体外释放
fluorouracil
macromolecular prodrug
characterization
release in vitro
