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Synthesis of an inhibitor of carbonic anhydrase : formulation of an inhibitor of carbonic anhydrase : formulation of δ-aminolevulinic acid for melanoma imaging
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Carbonic anydrase (CA) is a zincmetalloenzyme with a role in several physiological reactions, the most important being the hydration of CO2 to generate bicarbonate ion and protons. Five CA families have been identified so far (α, β, δ, γ and ζ-CA) but only α-CA is expressed by vertebrades. This particular family has 16 presently known isoforms which differ in tissue distribution and associated physiological function. Therefore, specific CA modulators (activators and above all, inhibitors) can be used as antiglaucoma, diuretics, anticancer, antiobesity agents and for other therapeutical applications. For almost 60 years, sulfonamides and their esters have been developed as CA inhibitors. Due to their high inhibition rate, they represent the main compounds belonging to the class of CA inhibitors. A first goal of the present work was to synthetize a fluorescent labelled-sulfonamide with anticancer activity and to fully characterize the obtained product. In a second part of this research project, the complexation of a different sulfonamide, synthetized in the Dept. of Chemistry of the University of Florence, into selected cyclodextrins was studied. In this case the CA inhibitor was expected to have activity against glaucoma. Thus, the expected enhancement of the water solubility obtained by the use of cyclodextrins was aimed at the obtainment of an ophtalmic formulation. Finally, in the third part of this project, a formulation with δ-aminolevulinc acid, a hydrophilic amino acid that once it is absorved in the skin, is converted to protoporphyrin IX (a powerful photosensitizer that helps in photodynamic diagnose and therapy of skin neoplastic disorders like melanoma) were studied. Nine different niosome formulations (with and without edge activators such as DCP and SCH) were developed in order to evaluate the efficiency of encapsulation and the delivery of the drug through the skin.
Descrição
Trabalho Final de Mestrado Integrado, Ciências Farmacêuticas, Universidade de Lisboa, Faculdade de Farmácia, 2014
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Mestrado Integrado - 2014