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|Title: ||Synthesis and investigation of novel shelf-stable, brain-specific chemical delivery system|
|Authors: ||Al-Obaid, Abdulrahman M.|
Farag, Hassan A.
Khalil, Ashraf A.
Al-Shabanah, Othman A.
Abdel Hamide, Sami G.
El-Kashef, Hassan A.
Ahmed, Hassan S.
Al-Affifi, Ahmed M.
Gadkariem, Elrasheed A.
El-Subbagh, Hussein I.
Chemical delivery systems
|Issue Date: ||2006 |
|Publisher: ||Saudi Pharmaceutical Society|
|Citation: ||Saudi Pharmaceutical Journal: 14(1); 1 - 15|
|Abstract: ||A 1,4-dihydropyridine pyridinium salt type redox system is described as a general and
flexible method for site-specific and sustained delivery of drugs into the brain. Monoamine
oxidase inhibitors (MAOIs) were used as a model example to be delivered into the brain.
Chemical and biological oxidations of these compounds were investigated. The prepared
1,4-dihydropyridines were subjected to various chemical and biological oxidation to evaluate
their ability to cross blood brain barrier (BBB), and to be oxidized biologically into their
corresponding quaternary compounds. 1-(Ethoxy-carbonylmethyl)-3,5-bis[N-(2-fluorobenzylideneamino)
carbamoyl]-1,4-dihydropyridine (31) proved to cross BBB in adequate rate
and converted by the oxidizing enzymes into the corresponding quaternary salt
(20). Stability studies of the synthesized chemical delivery systems (CDSs) at various pH values
and temperatures showed that the shelf life time of a solution containing compound 31 is 20.53
days at 5°C, which recommend a lower storage temperature for such solutions. The prepared
CDSs proved to be fairly stable for powder form storage. The stability of the prepared compounds
is attributed to the conjugation of the two carboxylic functions at C3 and C5 of the pyridine ring
with their adjacent double bonds. These results are in consistency with the original rationale
|Description: ||1Department of Pharmaceutical Chemistry. 2Department of
Pharmacology, College of Pharmacy, King Saud University, P.O.
Box 2457, Riyadh-11451, Saudi Arabia.
*To whom correspondence should be addressed.
|Appears in Collections:||College of Pharmacy|
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