S. Vanderkerken et al., Synthesis and evaluation of poly(ethylene glycol)-polylysine block copolymers as carriers for gene delivery, J BIOACT C, 15(2), 2000, pp. 115-138
Different types of poly(ethylene glycol)-poly(L-lysine) PEG-PLL block copol
ymers were examined for their ability to form polyelectrolyte complexes wit
h DNA, their toxicity toward red blood cells and their in vitro transfectio
n efficiency. The complexation of the polymers with DNA was studied using t
he ethidium bromide fluorescence technique. All polymers complexed DNA to f
orm particles with sizes ranging from 80 nm to 150 nm. In most cases, small
er particles were also observed, and sometimes populations of even larger p
articles could be detected. In vitro toxicity toward red blood cells Mi as
low. Agglutination of red blood cells with some of the noncomplexed block c
opolymers was observed, but the aggregates were less dense than with polyly
sine. Transfection efficiency of 293 cells in vitro in the presence of chlo
roquine was dependent upon the charge ratio of polymer/DNA. Efficient trans
fection was achieved for the PEG-PLL block copolymers with linear PLL block
s. On the other hand, very low transfection efficiency was obtained from th
e PEG-PLL with a dendritic PLL block.