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. 2023 Jul 7;5(15):3834–3856. doi: 10.1039/d3na00198a

Post-insertion of targeting ligands into LNPs.

Receptors Targeting ligands Targeting strategy Diseases Reference
α4β7 integrin (inflammatory gut-homing leukocytes) MAdCAM-1-Fc protein DSPE-PEG-maleimide (one-pot) Piroxicam-accelerated colitis (PAC) 80
Inflammatory gut-homing leukocyte targeting
Cd3 aCD3 mAb (in vitro) DSPE-PEG-maleimide (one-pot) CD3 phenotype T cell targeting in a tumor environment 58
aCD3 F(ab′)2 (in vivo)
Caveolae Plasmalemma vesicle-associated protein (PV1) DSPE-PEG maleimide (one-pot) X, lung targeting 81
Lung endothelial cells Anti PECAM-1 mAb DSPE-PEG-Mal (mal post insertion) Lung targeting 82
DEC205+ murine dendritic cells DEC205 scFv DSPE-PEG-Mal (one-pot) X, spleen isolation after 24h of retro orbital injection 83
Cd4 aCD4 mAb DSPE-PEG-Mal (mal post insertion) CD4 phenotype T cell targeting 84
Splenic T cells aCD5 DSPE-PEG-Mal (mal post insertion) Cardiac fibrosis 85
Antigen specific CD8+T cells pMHC1 DSPE- PEG2000-mal and conjugation with TCEP Pr8 influenza virus 59
Osteoblast CH6 Aptamer Ch6-S-S-(SH2)2-OH → CH6-SH with DTT, DSPE-PEG-Mal → DSPE-PEG-CH6 (post insertion mal) Metabolic skeletal disorders associated with impaired bone formation (e.g. osteoporosis) 86
Cerebrovascular of inflamed brain VCAM-1 (CD106) DSPE-PEG2000 azide Glioblastoma (pathological permeability of the BBB) 96
Neutrophils aCD177 Peptide H or peptide M-PEG2000-DSPE, m-PEG2000-DSPE X 102
Ly6C + inflammatory leukocytes Anti-Ly6C antibodies by ASSET (anchored secondary scFV enabling targeting) DSPE-PEG-Ome (one-pot) DSS colitis 60
Cd34 mAB for ASSET evaluation, Ly6C for DSS colitis Anti-Ly6C antibodies by ASSET (anchored secondary scFV enabling targeting) DSPE-PEG-carboxyl (carboxyl post insertion with EDC and NHS) DSS colitis 61
Ly6C + inflammatory leukocytes Anti-Ly6C antibodies by ASSET (anchored secondary scFV enabling targeting) DSPE-PEG and ASSET DSS colitis 62
EGFR aEGFR (ASSET) DSPE-PEG and ASSET Tumor 63