V. Weissig et al., DQASOMES - A NOVEL POTENTIAL-DRUG AND GENE DELIVERY SYSTEM MADE FROM DEQUALINIUM(TM), Pharmaceutical research, 15(2), 1998, pp. 334-337
Purpose. Dequalinium, a drug known for over 30 years, is a dicationic
amphiphile compound resembling bolaform electrolytes. The purpose of o
ur work was to determine the state of aggregation of dequalinium in aq
ueous medium and to investigate both, its ability to bind DNA and its
potential to serve as a novel non-viral transfection vector. Methods.
The form of aggregation was determined employing electron microscopic
techniques. The DNA binding capacity of dequalinium was assayed using
SYBR(TM) Green I stain. For in vitro cell transfection experiments pla
smid DNA encoding for firefly luciferase was used. Results, Dequaliniu
m forms in aqueous medium liposome-like aggregates, which we term DQAs
omes. These dequalinium vesicles bind DNA and they are able to transfe
ct cells in vitro with an efficiency comparable to Lipofectin(TM). Con
clusions. Based on the intrinsic properties of dequalinium such as the
in vivo selectivity for carcinoma cells and selective accumulation in
mitochondria we propose DQAsomes as a novel and unique drug and gene
delivery system.