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Pharmacology and pharmacy
One of the most important goals of pharmaceutical science is local izing the pharmacological activity of the drug at the site of action. Drug delivery systems - are. molecular tools which without undesired interaction at other sites target a specific drug receptor. In this work a· novel folate-cyclodextrin conjugate was synthesised for potential use as a drug delivery system in cancer therapy. Folate was directly covalently bound to an amino derivative of p-Cyclodextrin with a view to decreasing the polydispersity of the carrier system. Ultimately the cyclodextrin cavity will be used to transport drugs to the site of action. This study also describes the structural characterisation of the novel folatecyclodextrin conjugate using a range of techniques including electronic, vibrational, NMR, MALDI-MS and ESI-MS spectroscopies, all of which provided evidence that the folate moiety was bound to the cyclodextrin through an amide linkage. HPLC analysis was employed to study the purity of the conjugate prepared and provided evidence of the formation of a and y structural isomers. The photostability of the conjugate was assessed using electronic spectroscopy and the formation of particles was detected by light scattering. Preliminary biological evaluation of the tumour targeting device was carried out using HeLa cells and no evidences of cytotoxicity are recorded.
Clementi, Antonio (Thesis), "Synthesis of Novel Targeted Drug Delivery Systems for Cancer Therapy" (2008). Masters. Paper 58.