Antisense Oligonucleotides and RNA Interference - Challenges in Delivery of Therapeutic Genomics and Proteomics - page 353

S. No. Delivery System Composition Route of Administration Characteristics References

1. Cationic lipid-

based vectors:
liposomes/
lipoplexes

Lipids such as lipofectin, RNAifect, oligofectamine,
lipofectamine, cardiolipin, and transIT TKO are
commonly used transfection reagents composed of
cationic lipids and colipids like ceramide carbomoyl
spermine (CCS) and dioleoyl phosphatidylethanolamine
(DOPE), dioleoyl phosphatidylcholine (DOPC), N -(1-
(2,3-dioleoyloxy)propyl)- N , N , N -trimethylammonium
chloride (DOTAP), 3ss[ N -( N ,N dimethylaminoethane)
carbamoyl]-cholesterol (DC-CHOL), 1,2-dioleoyl-
sn-glycero-3-phosphocholine (DOPC), N -[1-(2,3-
dioleyloyx) propyl]- N - N - N -trimethyl ammonium
chloride (DOTMA), dioctadecyldimethylammonium
bromide (DODAB)cholesterol, etc.

Intravenous,
intracerebroventricular,
intravaginal

Have improved pharmacokinetic
properties with reduced systemic
toxicity, but may precipitate acute
immune responses
Protect oligonucleotides
from degradation and provide
controlled drug delivery

[12,155-161]

2. Polymeric

micelles

Polymers like poly(aspartate hydrazone adriamycin),
poly(ethylene oxide)-block-poly(aspartic acid),
pluronics, poly( N -isopropylacrylamide), poly(ethylene
glycol)-block-poly(ethylenimine), N -(2-hydroxypropyl)
methacrylamide (HPMA) copolymers, etc.

Intravenous,
intraperitoneal

Protect oligonucleotides
from degradation and provide
controlled drug delivery

[160,162-165]

3. Polymeric

nanoparticles

Polymers like gelatin, chitosan, albumin, sodium
alginate, poly(lactide- co -glycolide), polyanhydrides,
hyaluronic acid, cyclodextrin, gold nanoparticles, silica
nanoparticles, etc.

Intravenous Have improved pharmacokinetic

properties with reduced systemic
toxicity but may cause acute
immune responses, protect
oligonucleotides from degradation,
and provide controlled drug
delivery

[12,155,160,166-170]

4. Lipid-polymer

hybrid systems

Consists of hybrid systems like liposome-entrapped
polylysine-condensed DNA, lipid-coated precondensed
polylysine-DNA, poly(propylacrylic acid)-coated
cationic lipid-DNA conjugate, etc.

Intravenous Provide better protection

against nucleases and more
efficient transfection than
uncoated lipoplexes or polyplexes

[160,171-174]