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Synthesis and Evaluation of Poly(Ethylene Glycol)-Polylysine Block Copolymers as Carriers for Gene Delivery

Polymer Materials Research Group, Department of Organic Chemistry, University of Ghent, Krijgslaan 281 S-4bis, B-9000 Ghent, Belgium

T. Vanheede

Polymer Materials Research Group, Department of Organic Chemistry, University of Ghent, Krijgslaan 281 S-4bis, B-9000 Ghent, Belgium

V. Toncheva

Polymer Materials Research Group, Department of Organic Chemistry, University of Ghent, Krijgslaan 281 S-4bis, B-9000 Ghent, Belgium

E. Schacht

Polymer Materials Research Group, Department of Organic Chemistry, University of Ghent, Krijgslaan 281 S-4bis, B-9000 Ghent, Belgium

M. A. Wolfert

CRC Institute for Cancer Studies, University of Birmingham School of Medicine, Edgbaston, Birmingham B15 2TT, UK

L. Seymour

CRC Institute for Cancer Studies, University of Birmingham School of Medicine, Edgbaston, Birmingham B15 2TT, UK

A. Urtti

Department of Pharmaceutics, University of Kuopio, P.O. Box 1627, FIN-70211 Kuopio, Finland

Different types of poly(ethylene glycol)-poly(l-lysine) PEG-PLL block copolymers were examined for their ability to form polyelectrolyte complexes with DNA, their toxicity toward red blood cells and their in vitro transfection efficiency. The complexation of the polymers with DNA was studied using the ethidium bromide fluorescence technique. All polymers complexed DNA to form particles with sizes ranging from 80 nm to 150 nm. In most cases, smaller particles were also observed, and sometimes populations of even larger particles could be detected. In vitro toxicity toward red blood cells was low. Agglutination of red blood cells with some of the noncomplexed block copolymers was observed, but the aggregates were less dense than with polylysine. Transfection efficiency of 293 cells in vitro in the presence of chloroquine was dependent upon the charge ratio of polymer/DNA. Efficient transfection was achieved for the PEG-PLL block copolymers with linear PLL blocks. On the other hand, very low transfection efficiency was obtained from the PEG-PLL with a dendritic PLL block.

Journal of Bioactive and Compatible Polymers, Vol. 15, No. 2, 115-138 (2000)
DOI: 10.1177/088391150001500202


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