Lipid-Like Delivery Materials for Efficient siRNA Delivery - Nanotechnology for the Delivery of Therapeutic Nucleic Acids - page 157

day. Measuring target and control gene expression concurrently
with luminescence is efficient, permitting the rapid identification of
effective compounds and structure-function relationships. In this
case, lipidoids with at least two amines per backbone, two long lipid
tails, or many shorter lipid tails potently silenced the target gene
without influencing control gene expression.

Figure 7.2 Synthesis of lipidoids. (a) Alkyl-acrylate, alkyl-acrylamide,

and amino molecules were used to synthesize a combinatorial
library of lipidoids. (b) Synthesis occurs through the conjugate
addition of amines to an acrylate or acrylamide. Depending on
the number of addition sites in the amino monomer, lipidoids
can be formed with anywhere from 1 to 7 tails. Amino groups in
the lipidoid can be quaternized by treatment with methyl iodide.
For ease of nomenclature, lipidoids are named as follows: (amine
number)(acrylate or acrylamide name)-(number of tails)(“+” if
quaternized). Reproduced with permission from Ref. [13].