基于环糊精和阳离子聚合物构建超分子基因载体.docVIP

 Supramolecular gene carrier base on cyclodextrin and polycation# 5 ** Abstract: A series of novel supramolecular pseudo-comb polycations (l-PGEA-Ad/ CD-PGEAs) were synthesized by tying multiple low-molecular-weight β- cyclodextrin-cored star 10 15 20 25 30 35 40 45 ethanolamine-functionalized poly(glycidyl methacrylate) (PGEA) polymers (CD-PGEAs) with an adamantine-modified linear PGEA (l-PGEA-Ad) backbone via the host–guest interaction. The pseudo-comb carriers were studied in terms of their DNA binding capability, cytotoxicity, and gene transfection in HepG2 cell line. The pseudo-comb l-PGEA-Ad/CD-PGEAs exhibited better pDNA-condensing abilities than their counterparts, CD-PGEA and l-PGEA. Meanwhile, the pseudo-comb carriers displayed low cytotoxicity, similar to CD-PGEA and l-PGEA. Moreover, the gene transfection efficiencies of the pseudo-comb carriers were much higher than those of CD-PGEA and l-PGEA at various N/P ratios. Such supramolecular preparation of pseudo-comb gene carriers could provide a flexible approach to adjusting the structure and functionality of supramolecular polymers via properly using noncovalent interactions. Key words: Polymer science; Gene delivery; Supramolecular polymer; cyclodextrin 0 Introduction The development of safe and effective polycationic vectors is of crucial importance to the gene therapy.[1] In comparison with viral vectors and cationic lipids, polycations as the major type of nonviral gene delivery vectors show low host immunogenicity and can be produced on a large scale. A large number of polycations, including polyethylenimine (PEI), [2] polyamidoamine, [3] chitosan, [4] and cyclodextrin (CD)-based cationic vectors, [5] have been reported to deliver nucleic acids. We found that ethanolamine (EA)-functionalized poly(glycidyl methacrylate) (PGMA) (or PGEA) with plentiful flanking secondary amine and hydroxyl groups can produce good transfection efficiency in some cell lines, while exhibiting low toxicity.