Series of New β-Cyclodextrin-Cored Starlike Carriers for Gene Delivery

摘要

The development of safe and effective β-cyclodextrin (β- CD)-cored cationic star gene carriers has attracted considerable attention. In this work, a series of star-shaped hemocompatible CD-PGPP, CD- PGAEPP, and CD-PGAPP vectors composed of β-CD cores and piperazine (PP)-, N-(aminoethyl)piperazine (AEPP)-, or N-(3-amino- propyl)-2-pyrrolidinone (APP)-functionalized poly(glycidyl methacry- late) arms were successfully proposed and compared for highly efficient gene delivery. Such star carriers possess plentiful secondary amine, tertiary amine, and nonionic hydroxyl groups. CD-PGPP, CD-PGAEPP, and CD-PGAPP were effective in condensing plasmid DNA into nanoparticles, whose sizes were 100—200 nm and positive ζ potentials were 25—40 mV at nitrogen/phosphate (N/P) ratios of 10 and above. CD-PGPP, CD-PGAEPP, and CD-PGAPP showed significantly lower cytotoxicity than control poly(ethylenimine) (PEI;～25 kDa). At most N/P ratios, CD-PGAPP exhibited better gene transfection performance than CD-PGPP and CD-PGAEPP particularly in HepG2 cells. More importantly, in comparison with PEI, all of the CD-PGPP, CD-PGAEPP, and CD-PGAPP vectors did not cause undesirable hemolysis.