Table 3 Examples of engineering EV targeting by the addition of peptides
From: Extracellular vesicle-based therapeutics: natural versus engineered targeting and trafficking
Targeting peptide | Linkage method | Result | Reference |
|---|---|---|---|
RGERPPR— a specific peptide for the neuropilin-1 receptor expressed specifically on glioma and tumor vascular endothelial cells. | Click Chemistry (cyclo-addition reaction of sulfonyl azide). | EVs could cross the BBB and target glioma cells to deliver therapeutic payload, resulting in increased survival in a murine model of glioma. | |
M12—a muscle targeting peptide | Using phage display, the CP05 peptide, which binds to the extracellular loop of CD63 with high affinity, was identified. Fusion of targeting peptides to CP05 allowed coating of the EV surface via CP05-CD63 interaction. | Targeted EVs successfully delivered splice-correcting oligomers to muscle in a dystrophin-deficient mouse model of muscular dystrophy. | |
RGD—specifically binds to integrin αvβ3 expressed on the surface of angiogenic blood vessels. | RGD anchored to EV surface via linkage to PEG-lipid which self-assembles into EV membrane. | EVs were targeted to αvβ3 cells in zebrafish and promoted angiogenesis. | |
CTP—cardiac targeting peptide | Recombinant CTP-Lamp2b expressed in donor cells. | 15% increase in delivery to mouse hearts after intravenous injection. |