Effect of edge activators on the formation and transfection efficiency of ultradeformable liposomes

Highly deformable hydrophilic lipid vesicles have been studied for transdermal delivery of therapeutically active small molecules and proteins. Here, we report the effects of edge activators on the formation of ultradeformable liposomes (UL) and transdermal gene delivery. Sodium cholate, sodium deox...

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Bibliographic Details
Published in:Biomaterials 2005, Vol.26 (2), p.205-210
Main Authors: Lee, Eun Hye, Kim, Adele, Oh, Yu-Kyoung, Kim, Chong-Kook
Format: Article
Language:English
Subjects:
Administration, Topical
Animals
Carcinoma, Hepatocellular - pathology
Cell Line, Tumor
Coated Materials, Biocompatible - adverse effects
Coated Materials, Biocompatible - chemistry
DNA - administration & dosage
DNA - adverse effects
DNA - chemistry
DNA - pharmacokinetics
Drug Delivery Systems - methods
Edge activators
Elasticity
Excipients - adverse effects
Excipients - chemistry
Humans
Liposomes - adverse effects
Liposomes - chemistry
Liver Neoplasms - pathology
Membrane Fluidity
Mice
Mice, Inbred C57BL
Particle Size
Phosphatidylcholines - chemistry
Plasmid DNA
Transdermal gene delivery
Transfection - methods
Ultradeformable liposomes
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Summary:Highly deformable hydrophilic lipid vesicles have been studied for transdermal delivery of therapeutically active small molecules and proteins. Here, we report the effects of edge activators on the formation of ultradeformable liposomes (UL) and transdermal gene delivery. Sodium cholate, sodium deoxycholate, and Tween 80 were tested as edge activators. Of the edge activators, sodium cholate and sodium deoxycholate resulted in the smaller sizes of UL and more positive zeta potentials than did Tween 80. Moreover, sodium deoxycholate-based UL showed the highest positive zeta potentials, which might lead to the firmer binding with negatively charged DNA. Following topical application onto mice, DNA complexed with UL containing either sodium cholate or sodium deoxycholate showed substantial transdermal absorption. In contrast, DNA complexed with Tween 80-based UL did not show in vivo transdermal absorption. These data suggest that UL might be of use as a transdermal delivery system of plasmid DNA, and that the choice of edge activators may play an important role in the transdermal delivery of plasmid DNA via UL.
ISSN:0142-9612
1878-5905
DOI:10.1016/j.biomaterials.2004.02.020