| Abstract: |
The present thesis involves the design, synthesis and investigation of a new carrier system for site-specific delivery and sustained release of drugs to the brain.The carrier suggested is 3, 5-dicarbonyl derivative of 1, 4-dihyDROPyridine that has an alkoxycarbonylmethyl substituent on the nitrogen atom. The drug moiety will be connected to the 3, 5-dicarbonyl groups in the form of esters or amides. One carrier moiety will carry two molecules of the drug and accordingly doubling the brain-specific delivery of the drug for each carrier moiety.The dissertation is divided into four main sections; introduction, scope of investigation, results & discussion and experimental section.The introduction is first concerned with the idea of brain specific CDS, using the DihyDROPyridine __ Pyridinium salt Redox CDS to deliver certain drugs to the brain, and the problems associated with the application of this system in pharmaceutical formulations. A survey of the most important and documented modifications to overcome pyridine CDS problems and an idea about the choice of model drugs to study new carriers for brain-specific delivery are also included.The scope of investigation states the main objectives of design, synthesis and investigation of 3, 5-dicarbonyl derivative of 1, 4-dihyDROPyridine that has an alkoxycarbonylmethyl substituent on the nitrogen atom as a novel shelf-stable carrier system to deliver biologically active compounds to the brain. percentages of 54.5%, 47.8%, 26.6%, 19.3%, 8.5%, 7.8% and 7.2%respectively; while imipenem showed the highest antibacterial effect withresistance percentage of 6.6%. Four isolates were found to be susceptible to all tested antibiotics and only one isolate was resistant to all testedantibiotics. The remaining isolates showed resistance to one or moreantibiotics, thus 57, 44, 29, 4, 15, 5, 5, and one isolate, were resistant toone, two, three, four, five, six, seven, and eight antibiotics, respectively.
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