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引用本文:方加龙,许军,张雁雯,刘燕华,黄黎敏,胡越.功能化氧化石墨烯负载氟尿嘧啶制备及体外释放研究[J].中国现代应用药学,2014,31(10):1215-1219.
FANG Jialong,XU Jun,ZHANG Yanwen,LIU Yanhua,HUANG Limin,HU Yue.Preparation and in Vitro Release of Functionalized Graphene Oxide Loading Fluorouracil[J].Chin J Mod Appl Pharm(中国现代应用药学),2014,31(10):1215-1219.
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功能化氧化石墨烯负载氟尿嘧啶制备及体外释放研究
方加龙, 许军, 张雁雯, 刘燕华, 黄黎敏, 胡越
江西中医药大学药学院,南昌 330004
摘要:
目的 通过β环糊精(β-CD)功能化氧化石墨烯(graphene oxide,GO)负载氟尿嘧啶(5-Fu),以增加5-Fu释放时间。方法 采用改进Hummers方法制备GO,使GO与β-CD酯化得到功能化GO-β-CD负载5-Fu。采用高效液相色谱法(HPLC)测定GO-β-CD-5-Fu的体外释放度。利用紫外、傅立叶变换红外、透射电镜、扫描电镜和拉曼光谱分别对GO,GO-β-CD,GO-β-CD-5-Fu表征测定。结果 GO功能化、负载均成功,负载率为105%。HPLC测定结果表明GO-β-CD-5-Fu突释效应减弱,呈梯度释放。T1/2为(4.5±0.08)d。结论 GO-β-CD负载5-Fu成功,体外释放时间增加,T1/2提高了324倍。
关键词:  功能化石墨烯  氟尿嘧啶  纳米粒  体外释放
DOI:
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基金项目:江西省教育厅2013年科学研究项目(GJJ13608)
Preparation and in Vitro Release of Functionalized Graphene Oxide Loading Fluorouracil
FANG Jialong, XU Jun, ZHANG Yanwen, LIU Yanhua, HUANG Limin, HU Yue
Pharmacy College, Jiangxi University of Traditional Chinese Medicine, Nanchang 330004, China
Abstract:
OBJECTIVE To prolong the release time of 5-Fluorouracil(5-Fu) in vitro, β-cyclodextrin(β-CD) was used to functionalize graphene oxide(GO) and then loaded with 5-Fu. METHODS By using a modified hummers method to prepare GO, and the resulting GO could subsequently be esterified with β-CD to afford the β-CD functionalized GO(GO-β-CD). In addition, In vitro release of functionalized graphene oxide loading fluorouracil(GO-β-CD-5-Fu) could be determined by high performance liquid chromatography(HPLC). The structures and morphologies of GO, GO-β-CD and GO-β-CD-5-Fu were characterized by ultraviolet-visible(UV-vis) absorption spectroscopy, Fourier transform infrared(FTIR) spectroscopy, Transmission Electron Microscopy(TEM), Scanning Electron Microscopy(SEM) and Raman spectroscopy(Raman). RESULTS GO-β-CD were prepared and characterized successfully. GO-β-CD had a high drug loading capacity for 5-Fu, with a loading rate of 105%. The results of HPLC analysis showed the burst release effect of GO-β-CD-5-Fu was weakened in a gradient-release pattern,and the elimination half-life (T1/2) was (4.5±0.08)d. CONCLUSION GO-β-CD was successfully loaded with 5-Fu and resulted in increase of the release time. Furthermore, GO-β-CD-5-Fu had a 324-fold longer T1/2 than 5-Fu.
Key words:  functionalized graphene  fluorouracil  nanoparticles  in vitro release
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