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Table 2 Summary of the common lipid-based delivery system

From: Nonviral delivery systems for antisense oligonucleotide therapeutics

Delivery systems

Administration routs

Targeted diseases

Nanocarriers components

Particle size

Key observations

Ref

Biodegradable lipid nanoparticles

Intravenous injection

PCSK9 in liver

306-O12B-3, DOPE, PEG, cholesterol, ASO

150–500 nm

ASO/LNP complexes reduce the total PCSK9 protein and serum cholesterol level with no hepatotoxicity or nephrotoxicity

[47]

Lipid nanoparticles

Intravenous injection

Metastatic renal cancer

DOTAP, soyPC, TPGS, folate-PEG-DSPE, ASO

108.6 ± 5.8 nm

Folate receptor-targeted lipid-albumin nanoparticles augment cell uptake rate and prolong the half-life of ASO

[48]

Lipid nanoparticles

Intravenous injection

Lung cancer

DODMA, egg PC, cholesterol, T7-PEG-DSPE, PEG-DMG, ASO

139.4 ± 7.6 nm

T7-conjugated CO-ASOs-LNPs exhibit excellent colloidal stability and produce superior antitumor activity

[49]

Lipid nanoparticles

Intravenous injection

Acute myelogenous leukemia

Cholesterol, DDAB, PEI, TPGS, Tf, DOTAP, DSPE-PEG2000-Mal, ASO

133.4 ± 7.6 nm

Transferrin-conjugated lipid nanoparticles augment cell uptake rate significantly

[50]

Lipid nanoparticles

Intravenous injection

Hepatocellular carcinoma

Neutral cytidinyl lipid, cystine skeleton cationic lipid, DSPE-PEG, ASO

139.0 ± 9.2 nm

Mix/CT102 nanoparticles exhibit a predominant accumulation capacity in liver tissue

[51]

Cationic liposomes

NA

Prostate cancer

DSPE-PEG2000-Mal, Cholesterol, DOTAP, Phosphatidylcholine, Trastuzumab, ASO

127 – 154 nm

ASO liposomes are more effective than free ASO to penetrate 2D and 3D spheroid models

[55]

Cationic elastic liposomes

Cutaneous administration

Atopic dermatitis

DOTAP, Sodium cholate, ASO

Over 200 nm

IL-13 ASO/cationic elastic liposomes dramatically suppress IL-13 production (by up to 70% of free ASO)

[56]

Cationic liposomes

Injection

Candida albicans infection

DOTAP, DOPC; DOPE, MO, ASO

40 – 80 nm

DOTAP-based lipoplexes inhibit Candida albicans filamentation up to 60% after 72 h

[57]

Hydrogel liposomes

Subcutaneous administration

NA

Lipid-oligonucleotides, hydrogels, ASO

14 nm

Hydrogel-based liposomes prolong ASO release and enhance its stability

[58]

Lipid nanoparticles

Peritumoural injection

Subcutaneous tumor

Cytidinyl lipid, cationic lipid, ASO

236 ± 7.9 nm

Cytidinyl-lipid combined with a cationic lipid exhibits high encapsulation efficiency for ASO

[59]

Lipid nanoparticles

Intravenous injection

Acute myelogenous leukemia

DOTAP, DOPE, TPGS, Cholesterol, DOC, PEI, ASO

93 ± 18 nm

CD33-targeted lipid nanoparticles show a 15-fold reduction in the IC50 of an antileukemic drug

[60]

  1. DOTAP, cationic 1,2-dioleoyl-3-trimethylammonium-propane; DOPC, 1,2-dioleoyl-sn-glycero-3-phosphocholine; DOPE, 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine; MO, monoolein; SoyPC, L-α-phosphatidylcholine; TPGS, DL-α-Tocopherol methoxy-polyethylene glycol succinate; DODMA, 1,2-Dioleyloxy-3-dimethylaminopropane; egg PC, egg l-α-phosphatidylcholine; PEG-DMG, 1,2-Dimyristoyl-rac-glycero-3-methylpolyoxyethylene; DOC, deoxycholate; AML, acute myeloid leukemia; DDAB, didecyldimethylammonium bromide; Tf, human holo-transferrin; DSPE-PEG2000-Mal, 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[maleimide (polyethylene glycol)-2000]; PEI, polyethylenimine