Synthesis, characterization, and in vitro transfection activity of charge-reversal amphiphiles for DNA delivery.


Journal Article

A series of charge-reversal lipids were synthesized that possess varying chain lengths and end functionalities. These lipids were designed to bind and then release DNA based on a change in electrostatic interaction with DNA. Specifically, a cleavable ester linkage is located at the ends of the hydrocarbon chains. The DNA release from the amphiphile was tuned by altering the length and position of the ester linkage in the hydrophobic chains of the lipids through the preparation of five new amphiphiles. The amphiphiles and corresponding lipoplexes were characterized by DSC, TEM, and X-ray, as well as evaluated for DNA binding and DNA transfection. For one specific charge-reversal lipid, stable lipoplexes of approximately 550 nm were formed, and with this amphiphile, effective in vitro DNA transfection activities was observed.

Full Text

Duke Authors

Cited Authors

  • Zhang, X-X; Prata, CAH; Berlin, JA; McIntosh, TJ; Barthelemy, P; Grinstaff, MW

Published Date

  • April 20, 2011

Published In

Volume / Issue

  • 22 / 4

Start / End Page

  • 690 - 699

PubMed ID

  • 21456532

Pubmed Central ID

  • 21456532

Electronic International Standard Serial Number (EISSN)

  • 1520-4812

Digital Object Identifier (DOI)

  • 10.1021/bc1004526


  • eng

Conference Location

  • United States