Availability of liposomes as drug carriers to the brain.
Phospholipid vesicles, also known as liposomes, were examined for their ability to act as a drug carrier to the brain. 9-Amino-1,2,3,4-tetrahydroacridine (THA), a centrally acting acetylcholinesterase inhibitor, was used as a model drug. THA was encapsulated in dehydration-rehydration vesicles (DRV) composed of egg yolk phosphatidylcholine, cholesterol and dipalmitoyl-phosphatidic acid (molar ratio, 10/10/1) and injected into the heart of mice. The toxicity and side effects of THA were reduced by encapsulation in liposomes. The THA concentration in the mouse brain after injection of THA-encapsulated DRV at a dose of 2 mg/kg remained higher than that of free THA at the same dose. Effective concentration of THA in the brain was also prolonged by the use of liposomes, although accumulation of THA in the spleen and kidney was observed. We, therefore, concluded that liposomes are useful as carriers of drugs to the brain.
Kobayashi
K
K
Department of Cell Chemistry, Okayama University Medical School, Japan.
Han
M
M
Watarai
S
S
Yasuda
T
T
D000818:Animals; D001812:Blood-Brain Barrier; D001921:Brain / Q000378:metabolism*; D004337:Drug Carriers / Q000737:chemistry*; D008081:Liposomes / Q000378:metabolism*; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D013619:Tacrine / Q000008:administration & dosage*; D014018:Tissue Distribution
D004337:Drug Carriers; D008081:Liposomes; D013619:Tacrine