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. 2021 Nov 26;13(12):2014. doi: 10.3390/pharmaceutics13122014

Table 1.

Strategies that have enhanced therapeutic antibody delivery to the brain.

Delivery Strategy Therapeutic Antibody (Size) Antibody Target Disease Model Method of Transport Reference
Focused
ultrasound
(FUS; SUS;
SUS+MB)
Trastuzumab/Herceptin®
(148 kDa)
Human epidermal growth factor receptor (HER2) Breast cancer
with brain metastasis
N.D. [25]
Bevacizumab/Avastin®
(149 kDa)
Vascular endothelial growth factor (VEGF) Malignant glioma N.D. [26]
Aducanumab/Aduhelm®
(146 kDa)
Oligomeric Amyloid-β peptide (Aβ) Alzheimer’s disease N.D. [27]
Anti-Aβ polyclonal (Rabbit sera) (~150 kDa) Amyloid-β peptide (Aβ) Alzheimer’s disease N.D. [28]
Anti-Ab mAb,
(100–150 kDa)
Amyloid-β peptide (Aβ) Alzheimer’s disease N.D. [29,30]
Anti-Aβ mAb, A07/2a
(100 kDa)
pGlu3 Amyloid-β peptide (Aβ) Alzheimer’s disease N.D. [31]
Anti-2N tau antibody, RN2N
scFv (27 kDa)
Fab (56 kDa)
IgG (155 kDa)
Tau (isoforms with two N-terminal domains) Fronto-temporal lobar degeneration N.D. [32,33]
Anti-tau mAb (RNF5)
(150 kDa)
Tau (all isoforms) Fronto-temporal lobar degeneration N.D. [34]
Anti-α-synuclein mAb
(150 kDa)
α-synuclein Parkinson’s disease N.D. [35]
Bi-specific
antibody
Anti-Aβ mAb,
(150 kDa)
Amyloid-β peptide (Aβ) Alzheimer’s disease RMT (TfR) [36,37,38,39]
Anti-Aβ mAb, 13C3
(150 kDa)
Protofibrillar
Amyloid-β peptide (Aβ)
Alzheimer’s disease RMT (TfR) [40]
Anti-Aβ antibody, 3D6
scFv (~30 kDa)
IgG (~150 kDa)
Amyloid-β peptide (Aβ) Alzheimer’s disease RMT (TfR) [16]
Anti-BACE1 mAb (~150 kDa) BACE1 Alzheimer’s disease RMT (TfR) [41]
Nanoparticle
(liposome)
Cetuximab
(152 kDa)
Epidermal growth factor receptor (EGFR) In vitro BBB model
(brain malignancies)
RMT (TfR) [42]
Trastuzumab
(148 kDa)
HER2 receptor In vitro BBB model
(brain malignancies)
RMT (TfR) [42]
Anti-CD133 mAb (~150 kDa) Glioblastoma stem cells (GSCs) Glioblastoma RMT (LRP-1) [43]
Nanoparticle
(gold)
Anti-BACE1 mAb (~150 kDa) BACE1 Alzheimer’s disease RMT (TfR) [44]
Nanoparticle
(dendrimer)
Anti-NKG2a mAb
(~150 kDa)
NK cell receptor Glioblastoma RMT (caveolae-mediated endocytosis) [45]

Abbreviations: N.D., not determined; RMT, receptor-mediated transport; TfR, transferrin receptor; LRP-1, lipoprotein receptor-related protein-1.