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. Author manuscript; available in PMC: 2015 Jun 15.
Published in final edited form as: Adv Drug Deliv Rev. 2014 Jan 22;0:94–109. doi: 10.1016/j.addr.2014.01.008

Table 4.

Example therapeutic agents that have been delivered across the BBB or BTB

Therapeutic Agent Size Use Delivered to
Temozolomide 194 Da Chemotherapy Glioma model (9L)1 [141]
1,3-bis(2-choroethyl-1-nitrosourea (BCNU)2 214 Da Chemotherapy Glioma model (C6)1 [138,152]
Cytarabine 243 Da Chemotherapy Normal brain [140]
Boronophenylalanine 330 Da Agent for boron neutron capture therapy Glioma models (GBM 8401 [149]; 9L [150])
Doxorubicin 540 Da Chemotherapy Normal brain [96]
Methotrexate 545 Da Chemotherapy Normal brain [139]
siRNA ~13 kDa Huntington's disease therapy Normal brain [135]
Glial cell line-derived neurotropic factor (GDNF)2 24kDa Neuroprotective agent Normal brain [153]
Brain-derived neurotropic factor (BDNF) 27 kDa Neuroprotective agent Normal brain3 [156]
Herceptin (Trastuzumab) 148 kDa Anti-cancer antibody Normal brain [147]; Breast cancer brain met. model (BT474)1 [148]
BAM-10 Aβ targeted antibodies ~150 kDa Therapeutic antibody for Alzheimer's Disease TgCcrND8 Alzheimer's model mice1 [158]
BCNU-VEGF2 ~150 kDa Antiangiogenic-targeted chemotherapy Glioma model (C6)1 [155]
Plasmid DNA (pBDNF-EGFP)2 ~3600 kDa4 Gene therapy Normal brain [154]
Epirubicin in Magnetic nanoparticles ~12 nm Magnetic targeted chemotherapy Glioma model (C6)1 [144]
Doxorubicin in magnetic nanoparticles2 ~6–10 nm Magnetic targeted chemotherapy Glioma model (C6) [146]
BCNU in magnetic nanoparticles ~10–20 nm Magnetic targeted chemotherapy Glioma model (C6)1 [145]
Adeno-associated Virus (AAV) ~25 nm Gene therapy vector Normal brain [160–162]
Liposomal doxorubicin (Lipo-DOX) 90 nm Chemotherapy Normal brain [83]; Glioma model (9L)1 [142,163]
Interleukin-4 receptor targeted Lipo-DOX 100–120 nn l Chemotherapy Glioma model (8401) [143]
Neural progenitor cells 7–10 μm Stem cell Normal brain [159]
Natural killer cells (NK-92) ~10 μm Cell therapy for brain tumor Breast cancer brain met. model (MDA-MB-231-HER2) [151]
1

Also showed improved outcomes with FUS-induced BBB disruption

2

Used drug-loaded microbubbles

3

Also showed drug activity after delivery

4

Assumed 660 Da per base pair (bp), 760 bp for BDNF, and 4700 bp for pEGFP-N1