Table 2.
Representative examples of anticancer siRNA delivery systems
| Category | Delivery system | Core components | Size (nm) Zeta (mV) |
Target gene |
Animal model | Reference |
|---|---|---|---|---|---|---|
| Lipid-based particles |
Cationic liposome | DOTAP | 50 | Luciferase | Human H460 lung cancer | [45] |
| Cholesterol | +15 | |||||
| Hyaluronic acid | ||||||
| Recombinant tetra-H2A | ||||||
| DSPE-PEG | ||||||
| DSPE-PEG-AA | ||||||
| Cationic liposome | DOTAP | 20 | c-Myc | Human H460 lung cancer | [46] | |
| DOPA | +33 | |||||
| Cholesterol | ||||||
| Calcium phosphate | ||||||
| DSPE-PEG | ||||||
| DSPE-PEG-AA | ||||||
| Cationic liposome | AtuFECT01 | 118 | PKN3 | Human prostate and pancreatic cancer | [49, 48] | |
| DPhyPE | +46 | Clinical trial | ||||
| DSPE-PEG | ||||||
| Neutral liposome | DOPC | NA | EphA2 | Human ovarian cancer | [67] | |
| Tween 20 | −2.9 | Clinical trial | ||||
| SLN | DOPE | 117 | c-Met | Human glioblastoma | [79] | |
| DC-Cholesterol | +37 | |||||
| Cholesterol | ||||||
| Cholesterol oleate | ||||||
| Glyceryl trioleate | ||||||
| PEG-siRNA | ||||||
| rHDL | Apolipoprotein A-I | 10 | STAT3 | Human ovarian and colorectal cancer | [80] | |
| Cholesterol | −3.2 | FAK | ||||
| Cholesterol oleate | ||||||
| PC | ||||||
| Oligolysine | ||||||
| Polymeric particles |
CDP | CDP | 70 | RRM2 | Human melanoma | [84, 85] |
| AD-PEG | +10 | Clinical trial | ||||
| AD-PEG-Tf | ||||||
| PEI | F25 LMW branched PEI | 60–130 +35 to +40 |
VEGF | Human prostate carcinoma | [99] | |
| PEI | PEI-g-PEG-RGD | 161 +4.2 | VEGFR1 | Murine colon adenocarcinoma | [115] | |
| PA MAM | G5 PAMAM | 100 +40 | Hsp 27 | Human prostate cancer | [126] | |
| Chitosan | Chitosan-RGD | 200 +40 | PLXDC1 | Murine ovarian cancer | [134] | |
| Atellocollagen | Atellocollagen | NA NA | PLK1 | Human non-small cell lung cancer | [140] | |
| Protein | Thiolated human serum albumin | 170 NA | VEGF | Human prostate carcinoma | [138] | |
| Inorganic particles |
AuNP | Hollow AuNP | 40 | p65 | Human HeLa cervical cancer | [152] |
| Thiolated siRNA | NA | |||||
| F-PEG-TA | ||||||
| CNT | CNT-NH3+ | NA NA |
NA | Human epithelial lung cancer | [154] | |
| Calcium phosphate | Calcium phosphate | 38 | Luciferase | Human pancreatic cancer | [156] | |
| PEG-CPP | −2.2 |
Cationic components are in bold
SLN solid lipid nanoparticles; rHDL recombinant high-density lipoproteins; CDP cyclodextrin-containing polymer; PEI polyethyleneimine; PAMAM polyamidoamine; AuNP gold nanoparticles; CNT carbon nanotubes; DOTAP 1,2-dioleoyloxy-3-trimethylammonium propane; DSPE 1,2-distearoyl-sn-glycero-3-phosphoethanolamine; PEG polyethylene glycol; AA anisamide; DOPA dioleoylphosphatidic acid; DPhyPE 1,2-diphytanoyl-sn-glycero-3-phosphoethanolamine; DOPC 1,2-dioleoyl-sn-glycero-3-phosphatidylcholine; DOPE 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine; DC-Cholesterol 3β-[N-(N′,N′-dimethylaminoethane)-carbamoyl]-cholesterol; PC phosphatidylcholine; AD adamantane; Tf transferrin; RGD tri-peptide Arg-Gly-Asp; G5 PAMAM fifth-generation polyamidoamine; F-PEG-TA folic acid-polyethylene glycol-thiol; PEG-CPP PEG-block-charge-conversional polymer; NA not available; PKN3 protein kinase N3; EphA2 ephrin type-A receptor 2; STAT3 signal transducer and activator of transcription 3; FAK focal adhesion kinase; RRM2 ribonucleoside-diphosphate reductase subunit M2; VEGF vascular endothelial growth factor; VEGFR1 vascular endothelial growth factor receptor 1; Hsp27 heat shock protein 27; PLXDC1 Plexin domain-containing protein 1; PLK1 polo-like kinase 1