DQAsomes: a novel potential drug and gene delivery system made from Dequalinium.
OBJECTIVE
Dequalinium, a drug known for over 30 years, is a dicationic amphiphile compound resembling bolaform electrolytes. The purpose of our work was to determine the state of aggregation of dequalinium in aqueous 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 Green I stain. For in vitro cell transfection experiments plasmid DNA encoding for firefly luciferase was used.


RESULTS
Dequalinium forms in aqueous medium liposome-like aggregates, which we term DQAsomes. These dequalinium vesicles bind DNA and they are able to transfect cells in vitro with an efficiency comparable to Lipofectin.


CONCLUSIONS
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.
Weissig
V
V
Center for Imaging and Pharmaceutical Research, Massachusetts General Hospital, Charlestown, MA, USA. vweissig@cipr.mgh.harvard.edu
Lasch
J
J
Erdos
G
G
Meyer
H W
HW
Rowe
T C
TC
Hughes
J
J
D000818:Animals; D000891:Anti-Infective Agents, Local / Q000008:administration & dosage*; D002460:Cell Line; D003868:Dequalinium / Q000008:administration & dosage*; D004337:Drug Carriers; D016503:Drug Delivery Systems; D005614:Freeze Fracturing; D008081:Liposomes; D008854:Microscopy, Electron; D010316:Particle Size; D014162:Transfection / Q000379:methods*
D000891:Anti-Infective Agents, Local; D004337:Drug Carriers; D008081:Liposomes; D003868:Dequalinium