Chemistry Reference
In-Depth Information
NH
2
X
HN
NH
2
X
NH
O
HN
N
NH
2
NH
N
HN
N
O
X
O
O
NH
N
O
O
N
HO
OH
HO
OH
N
N
O
N
N
O
HO
O
HO
OH
O
O
O
HO
N
N
N
N
N
N
OH
H
NH
2
O
N
HN
X
HO
O
OH
O
OH
O
OH
NH
X
O
HO
O
H
2
N
N
O
N
N
N
O
N
N
HN
HN
O
NH
X
NH
NH
2
H
2
N
SCHEME 11.11
The structure of “click” CD-based dendrimer for gene delivery. (Adapted
from ref. 36.)
gene delivery [37]. They found that the novel polymer design could effectively
complex, condense, and deliver plasmid DNA (pDNA) with exceptional biocompat-
ibility and efficacy. The dendrimers were synthesized by direct “click” coupling of
acetylated-per-azido-
-CD and a series of alkyne-functionalized cationic dendrons
(Scheme 11.11). Different analyses revealed that the cluster bound and complexed
with pDNA into the spherical nanoparticles in the size range of 80-130 nm. The stable
polycationic nanoparticles deliver pDNA into HeLa and H9c2(2-1) cells effectively
and protect pDNA degradation from nuclease.
To develop linear CD-containing cationic polymers for efficient gene delivery,
the same research group copolymerized acetylated-diazido-
-CD and dialkyne-
oligoethyleneamines via “click” HDC reaction with very high efficiency (Scheme
11.12) [36]. By changing the repeating amine number and polymerization degree,
two series of polymers with different amine density or different molecular weight
were successfully synthesized. The influence of the oligoethylene amine density and
the polymer length were also evaluated. Their results showed that the polymer com-
plex could effectively deliver pDNA into HeLa cells and the complex also protects
the payload from nuclease degradation.
Search WWH ::
Custom Search