Targeting of post-ischemic cerebral endothelium in rat by liposomes bearing polyethylene glycol-coupled transferrin.
To achieve an efficient delivery targeting to post-ischemic cerebral vascular endothelium, PEG-liposome conjugated with transferrin (Tf) (Tf-PEG-liposome) was intravenously administered to the rats after 90 min of transient middle cerebral occlusion. The expression of Tf receptor (TfR) in the cerebral endothelium increased with a peak at 1 day after the reperfusion and returned to the control level by 6 days. The Tf-PEG fluorescence was marginally detectable in sham control brain, but remarkably increased with a peak at 2 days, showing about 70% of TfR positive vascular endothelium double-labeled with Tf-PEG. These results indicate that the Tf-PEG-liposome could be utilized as an efficient drug delivery tool to the brain after stroke.
Department of Neurology, Graduate School of Medicine and Dentistry, Okayama University, 2-5-1 Shikata-cho, Okayama 700-8558, Japan. nomori@cc.okayama-u.ac.jp
N
N
Omori
K
K
Maruyama
G
G
Jin
F
F
Li
S J
SJ
Wang
Y
Y
Hamakawa
K
K
Sato
I
I
Nagano
M
M
Shoji
K
K
Abe
D000818:Animals; D001812:Blood-Brain Barrier; D002545:Brain Ischemia / Q000188:drug therapy / Q000378:metabolism; D004730:Endothelium, Vascular / Q000378:metabolism*; D020244:Infarction, Middle Cerebral Artery / Q000378:metabolism; D008081:Liposomes; D008297:Male; D011092:Polyethylene Glycols / Q000008:administration & dosage; D051381:Rats; D017208:Rats, Wistar; D011990:Receptors, Transferrin / Q000096:biosynthesis; D013687:Telencephalon / Q000098:blood supply; D014168:Transferrin / Q000008:administration & dosage* / Q000378:metabolism / Q000493:pharmacokinetics
D008081:Liposomes; D011990:Receptors, Transferrin; D014168:Transferrin; D011092:Polyethylene Glycols