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KMID : 0370219980420020196
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Yakhak Hoeji
1998 Volume.42 No. 2 p.196 ~ p.204
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Brain Delivery of 99mTc-Diethylene Triamine Pentaacetic Acid and Phenytoin by Transient Osmotic Opening Method in Rats
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황만용/Hwang MY
박경호/이민화/Park KH/Lee MH
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Abstract
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The blood-brain barrier (BBB) of rats was modificated opening reversibly by infusing a hyperosmotic solution of arabinose (1.6 molal) into the right external carotid artery. Pre vious studies demonstrated that permeability was increased maxmmally in the first 15 min and remained slightly elevated at 1 hr. As control reference, saline was used. In the present study, to evaluate the effects of osmotic BBB opening on the BBB trasport according to hydrophilic or hydrophobic characteristics of drugs. And the differences of the uptakes of these compounds to right (treated osmotic opening) and left (untreated) hemispheres in same rats were compared each other following injection of 8 mCi per rat of 99mTc-ethylene triamine pentaacetic acid (DTPA) as hydrophilic drug or 5mg/kg of phenytoin as hydrophobic drug mto the right external carotid artery of rats between two groups (1.6 molal arabinose vs saline). The uptakes of 99mTc-DTPA and phenytoin in the right cerebral hemispheres were increased to about thirty three times and twice rather than those in the left cerebral heimspheres, respectively. And PAs (permeability X capillary surface area) were also increased from a control mean of 2.11 X 10-4 (Untreated) to 6.98 X lO-3 sec-1 (treated osmotic opening for 99mTc-DTPA and 0.29 to 0.17 sec-1 for phenytoin, respectively. From the results of present study, it is noted that osmotic opening of BBB is more effective in the brain delivery of hydrophilic drugs rather than that of hydrophobic drugs.
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