Table 1.
A summary of endothelial cell-targeting platforms reported in recent studies.
| Targeted cells | Platform | Targeting ligand | Route of administration | Delivered therapeutics? | Model of
evaluation/Application |
Effects on targeted cells |
|---|---|---|---|---|---|---|
|
Activated endothelial
cells |
Iron oxide microparticles [63] |
Vascular cell adhesion molecule-1 binding peptide |
Intravenous | No | Mouse model of cerebral
ischemia |
Imaging endothelial cell
activation |
|
| ||||||
|
Activated endothelial
cells |
Iron oxide microparticles [64] |
Vascular cell adhesion molecule-1 binding peptide |
Intravenous | No | Mouse model of acute brain inflammation, vascular dementia, Alzheimer's disease (AD) and multiple sclerosis |
Imaging endothelial cell
activation |
|
| ||||||
|
Activated endothelial
cells |
Iron oxide microparticles [65] |
Vascular cell adhesion molecule-1 binding peptide |
Intravenous | No | Mouse model of Stroke | Imaging endothelial cell
activation |
|
| ||||||
| Endothelial cells | Poly(butylcyanoacrylate)
nanoparticles (PBCN) [66] |
Polysorbate 80 | Intravenous | No | Healthy mouse, mouse model of AD |
Enhance BBB interaction |
|
| ||||||
| Endothelial cells | Poly(butylcyanoacrylate)
nanoparticles (PBCN) [67] |
Polysorbate 80 | Intravenous | Puerarin | Rat model of ischemia
reperfusion |
Enhance BBB interaction |
|
| ||||||
| Endothelial cells | Monovalent molecular shuttle (modified anti- TfR monoclonal antibody )[68-70] |
Anti-TfR monoclonal antibody |
Intravenous | Antibody | Mouse model of Alzheimer disease |
Enhance BBB penetration |
|
| ||||||
|
Endothelial cells
(BBTB) |
Liposome [71] | Cyclic Arg-Gly-Asp (RGD) peptide |
Intravenous | No | Mouse model of C6 glioma |
Enhance BBB penetration |
|
| ||||||
|
Endothelial cells
(BBTB) |
Liposome [72] | Folate and transferrin (Tf) |
Intravenous | Doxorubicin | Rat model of C6 glioma |
Enhance BBB penetration |
|
| ||||||
|
Endothelial cells
(BBTB) |
Liposome [73] | Cell penetration peptide TAT and transferrin (Tf) |
Intravenous | Doxorubicin | Mouse model of glioma | Enhance BBB penetration |
|
| ||||||
| Endothelial cells | Chitosan nanoparticle [74] |
Transferrin (Tf) | Intravenous | Peptide | Mouse model of stroke | Enhance BBB penetration |
|
| ||||||
| Endothelial cells | Angiopep2-neurotensin conjugates [75] |
Angiopep-2 | Intravenous | Neurotensin | Rat model of pain | Enhance BBB penetration |
|
| ||||||
|
Endothelial cells
(BBTB) |
Paclitaxel–Angiopep-2
peptide drug conjugate (GRN1005) [76] |
Angiopep-2 | Intravenous | Paclitaxel | Glioma patients (Phase I) | Enhance BBB penetration |
|
| ||||||
|
Endothelial cells
(BBTB) |
Paclitaxel–Angiopep-2
peptide drug conjugate (GRN1005) [77] |
Angiopep-2 | Intravenous | Paclitaxel | Mouse human glioma cell xerograph
model |
Enhance BBB penetration |
|
| ||||||
|
Endothelial cells
(BBTB) |
Paclitaxel–Angiopep-2
peptide drug conjugate (GRN1005) [78] |
Angiopep-2 | Intravenous | Paclitaxel | Mouse orthotopic glioma model |
Enhance BBB penetration |
|
| ||||||
|
Endothelial cells
(BBTB) |
Paclitaxel–Angiopep-2
peptide drug conjugate (GRN1005) [79] |
Angiopep-2 | Intravenous | Paclitaxel | Mouse model of brain metastases of breast cancer |
Enhance BBB penetration |
|
| ||||||
|
Endothelial cells
(BBTB) |
Doxorubicin–Angiopep-2
peptide drug conjugate (ANG1007 and ANG1009) [80] |
Angiopep-2 | Intravenous | Doxorubicin | Mouse model of glioma | Enhance BBB penetration |
|
| ||||||
| Endothelial cells | Fused protein [81] | Monoclonal antibody (mAb) against human insulin receptor (HIRMAb) |
Intravenous | Iduronate 2-sulfatase (IDS) |
Rhesus monkey | Enhance BBB penetration |
|
| ||||||
| Endothelial cells | Gold nanoparticles [82] | Insulin | Intravenous | No | Healthy mouse | Enhance BBB penetration |
|
| ||||||
|
Endothelial cells
(BBTB) |
Trail [83] | Choline derivate | Intravenous | Trail | Mouse model of glioma | Enhance BBB penetration |
|
| ||||||
| Endothelial cells (BBB) | PEG-dendrigraft poly-l- lysine (DGL)/DNA nanoparticles [83] |
Dermorphin | Intravenous | DNA | Cerebral ischemia reperfusion injury |
Enhance BBB penetration |
For each platform, targeting ligand; delivered therapeutics; model of evaluation/application and effects on targeted cells are described.