title: Polyethylenimine-cyclodextrin-tegafur conjugate shows anti-cancer activity and a potential for gene delivery.
abstract: 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.
authors: Institute of Chemical Biology and Pharmaceutical Chemistry, Zhejiang University, Hangzhou, China.
authors: Qi-da
authors: QD
authors: Hu
authors: Hui
authors: H
authors: Fan
authors: Wei-jian
authors: WJ
authors: Lou
authors: Qing-qing
authors: QQ
authors: Wang
authors: Gu-ping
authors: GP
authors: Tang
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D019556:COS Cells; D045744:Cell Line, Tumor; D003505:Cyclodextrins / Q000008:administration & dosage* / Q000737:chemistry; D004247:DNA / Q000378:metabolism; D004338:Drug Combinations; D018014:Gene Transfer Techniques; D017930:Genes, Reporter; D015316:Genetic Therapy / Q000379:methods; D019073:HT29 Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D009682:Magnetic Resonance Spectroscopy / Q000379:methods; D008546:Melanoma, Experimental; D051379:Mice; D053758:Nanoparticles / Q000737:chemistry; D009369:Neoplasms / Q000188:drug therapy*; D010957:Plasmids / Q000378:metabolism; D011094:Polyethyleneimine / Q000008:administration & dosage* / Q000737:chemistry; D005641:Tegafur / Q000008:administration & dosage* / Q000737:chemistry
chemical_list: D000970:Antineoplastic Agents; D003505:Cyclodextrins; D004338:Drug Combinations; D005641:Tegafur; D011094:Polyethyleneimine; D004247:DNA