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Title: pH-triggered release of gefitinib : a potent anticancer agent
Authors: Vella, Chelsey (2018)
Keywords: Antineoplastic agents
Hydrogen-ion concentration
Issue Date: 2018
Citation: Vella, C. (2018). pH-triggered release of gefitinib: a potent anticancer agent (Master's dissertation).
Abstract: Gefitinib (IUPAC: N-(3-chloro-4-fluorophenyl)-7-methoxy-6-[3-(morpholin-4-yl) propoxy]quinazolin-4-amine) is a new anti-cancer agent used in patients diagnosed with various advanced cancers. However, as with many other active pharmaceutical ingredients, its bioavailability –, and therefore its efficacy, is limited to a specific pH. This study involves a polymorph screen and complexation of gefitinib with a late lanthanide, with the aim of synthesizing a more pH labile, and hence potentially more bioavailable, complex of the drug. From the polymorph screen, three samples were observed to have different patterns that might be the result of formation of polymorphs or solvates. The lanthanide metals selected for this purpose were erbium, europium, galladinium and ytterbium. Their respective sodium EDTA complexes (Na[La(EDTA)(H2O)3. 5 H2O) were synthesized and subsequently used for complexation with gefitinib by substitution of the water ligands. The synthesis was repeated more than once to obtain different samples and check for replication of results. The synthesis was also attempted using liquid assisted grinding as a solid state approach. The samples were characterized by a number of characterization techniques including microscopy, infra-red spectroscopy, single crystal and powder x-ray diffraction. High Performance Liquid Chromatography was done in order to find the concentration of the drug released at three different pH: 1.5, 2.5 and 5. Different concentrations of drug release were observed that varied between one complex and another.
Description: M.SC
Appears in Collections:Dissertations - FacSci - 2018

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