Polyethylenimine-cyclodextrin-tegafur conjugate shows anti-cancer activity and a potential for gene delivery  

作　　者：Qi-da HU Hui FAN Wei-jian LOU Qing-qing WANG Gu-ping TANG 

机构地区：[1]Institute of Chemical Biology and Pharmaceutical Chemistry,Zhejiang University,Hangzhou 310028,China [2]Department of Pharmacy,Sir Run Run Shaw Hospital,School of Medicine,Zhejiang University,Hangzhou 310016,China [3]Institute of Immunology,Zhejiang University,Hangzhou 310058,China [4]The First Affiliated Hospital,School of Medicine,Zhejiang University,Hangzhou 310003,China

出　　处：《Journal of Zhejiang University-Science B(Biomedicine & Biotechnology)》2011年第9期720-729,共10页浙江大学学报（英文版）B辑（生物医学与生物技术）

基　　金：Project supported by the National High-Tech R & D Program (863) of China (No. 2007AA03Z355);the Zhejiang Provincial Natural Science Foundation of China (No. Z207572)

摘　　要：Polyethylenimine-cyclodextrin-tegafur(PEI-CyD-tegafur) conjugate was synthesized as a novel multifunctional prodrug of tegafur for co-delivery of chemotherapeutic agent tegafur and enhanced green fluorescent protein(EGFP) reporter plasmid DNA.Conjugation of tegafur to PEI-CyD via chemical linkage was characterized by 1 H NMR spectrometry and ultraviolet(UV) spectrometry.PEI-CyD-tegafur was able to condense plasmid DNA into complexes of around 150 nm with positive charge at the N/P ratio of 25,in accordance with electron microscopy observation of compact and monodisperse nanoparticles.The results of in vitro experiments showed enhanced cytotoxicity and considerable transfection efficiency in B16F10 cell line.Therefore,PEI-CyD-tegafur may have great potential as a co-delivery system with anti-cancer activity and potential for gene delivery.Polyethylenimine-cyclodextrin-tegafur（PEI-CyD-tegafur） conjugate was synthesized as a novel multifunctional prodrug of tegafur for co-delivery of chemotherapeutic agent tegafur and enhanced green fluorescent protein（EGFP） reporter plasmid DNA.Conjugation of tegafur to PEI-CyD via chemical linkage was characterized by 1 H NMR spectrometry and ultraviolet（UV） spectrometry.PEI-CyD-tegafur was able to condense plasmid DNA into complexes of around 150 nm with positive charge at the N/P ratio of 25,in accordance with electron microscopy observation of compact and monodisperse nanoparticles.The results of in vitro experiments showed enhanced cytotoxicity and considerable transfection efficiency in B16F10 cell line.Therefore,PEI-CyD-tegafur may have great potential as a co-delivery system with anti-cancer activity and potential for gene delivery.

关 键 词：POLYETHYLENIMINE Β-CYCLODEXTRIN TEGAFUR CO-DELIVERY Gene therapy 

分 类 号：R979.1[医药卫生—药品] R945[医药卫生—药学]