Preparation and evaluation of a new class of gene transfer reagents: poly(-alkylaminosiloxanes)

J Control Release. 2003 Dec 12;93(3):403-14. doi: 10.1016/j.jconrel.2003.08.014.

Abstract

We report the evaluation of poly(-alkylaminosiloxane) as a novel class of polycationic DNA carriers. Controlled hydrolysis of mono- and di-aminoalkylmethyldimethoxysilane provided a wide range of defined oligomeric mixtures. Basic hydrolysis conditions yielded mixtures composed mainly of cyclic and long linear oligomers, while under acidic conditions mainly short-linear oligomers were derived. They all efficiently interacted with plasmid DNA as revealed by electron microscopy and DNA retardation assays. However, only diamine-based oligomers prepared under basic conditions were able to mediate substantial levels of DNA transfection in human HeLa cells. SiDA1b, prepared by basic hydrolysis of 3-(2-aminoethylamino)propyl-methyl-dimethoxysilane, was found to be at least as efficient as the frequently used cationic transfection agents DOTAP and polyethylenimine (PEI). The transfection activity was sensitive to bafilomycin A1, suggesting a mechanism that depends on proton capture during the acidification process associated with endocytosis.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Line
  • Cell Line, Transformed
  • Cell Line, Tumor
  • DNA / administration & dosage*
  • DNA / genetics
  • DNA / ultrastructure
  • Dose-Response Relationship, Drug
  • Drug Evaluation, Preclinical / methods
  • Gene Transfer Techniques*
  • HeLa Cells
  • Humans
  • Rabbits
  • Siloxanes / administration & dosage*
  • Siloxanes / chemical synthesis*

Substances

  • Siloxanes
  • DNA