TABLE 4.
Nonviral systems and vehicles for the delivery of RNAi therapeutics
| RNAi Delivery Means | System Composition | FDA-Approved RNAi Medications |
|---|---|---|
| Ribonucleoside modifications | Adenine 2'-F ribonucleoside | Yes – givosiran, lumasiran, inclisiran |
| Adenine 2'-OMe ribonucleoside | Yes – givosiran, lumasiran, inclisiran | |
| Cytosine 2'-F ribonucleoside | Yes – givosiran, lumasiran, inclisiran | |
| Cytosine 2'-OMe ribonucleoside | Yes – patisiran, givosiran, lumasiran, inclisiran | |
| Guanine 2'-F ribonucleoside | Yes – givosiran, inclisiran | |
| Guanine 2'-OMe ribonucleoside | Yes – givosiran, lumasiran, inclisiran | |
| Thymidine | Yes – patisiran, inclisiran | |
| Uracil 2'-F ribonucleoside | Yes – givosiran, lumasiran | |
| Uracil 2'-OMe ribonucleoside | Yes – patisiran, givosiran, lumasiran, inclisiran | |
| Phosphate linkage modifications | Phosphorothioate | Yes – givosiran, lumasiran, inclisiran |
| Charge-neutralizing phosphotriester | No | |
| Receptor ligand conjugates | Tri-GalNAc | Yes – givosiran, lumasiran, inclisiran |
| Antibody conjugates | Entire antibody | No |
| Antibody fragment | No | |
| LNP | DSPC | Yes – patisiran |
| PEG-lipids | Yes – patisiran | |
| Ionizable | Yes – patisiran | |
| Polymer-based NP | PEI | No |
| PEI-PEG | No | |
| Polyurethane | No | |
| PACE | No | |
| Micelle | No | |
| Inorganic material-based NP | Gold-mediated | No |
| Mesoporous silicon | No | |
| Graphene oxide mediated | No | |
| Fe3O4 mediated | No | |
| Liposome | Neutral | No |
| Cationic | No | |
| pH-sensitive cationic | No | |
| Ionizable | No | |
| Chemotherapeutic coated | No | |
| Exosome | Exosome | No |
| Exosome-GE11 peptide | No | |
| ELV | No |
DSPC, 1,2-distearoyl-sn-glycero-3-phosphocholine; ELV, exosome-like vesicle; Fe3O4, iron(III) oxide; PACE, poly(amine-co-ester); PEI, polyethylenimine.