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

Qi-da HU 1,4,Hui FAN 2,Wei-jian LOU 2,Qing-qing WANG 3,Gu-ping TANG 1(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)  
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.
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