Polymeric carriers in medicine

dc.contributor.authorMukaya, Hembe Elie
dc.date.accessioned2009-03-31T09:45:51Z
dc.date.available2009-03-31T09:45:51Z
dc.date.issued2009-03-31T09:45:51Z
dc.description.abstractThe application of inorganic chemistry to medicine is a rapidly developing field, and novel therapeutic and diagnostic metal complexes are now having an impact on medical practice. The family of platinum-containing medicinal agents used for the chemotherapy of malignancies ranks among the most potent types of anticancer drug in present use. While highly potent against many cancers, cisplatin like other anticancer drugs suffers from virtually all of the clinical limitations observed with metal-free antitumor agents in current clinical use, most notably toxic side effects and a propensity for eliciting drug resistance in the cancerous cell. In an effort to increase the effectiveness of chemotherapy, one of the techniques in, use involves the binding of, the monomeric anticancer drug systems to water-soluble, biocompatible and biodegradable polymeric carriers. The interest in, and use of, polymers as drug delivery systems has received considerable attention worldwide; and this technique was utilized in this project. In the present project monomers bearing suitable side groups (aspartic and glycolic acid) for platinum drug anchoring in a chelating form were synthesized. These monomers were incorporated into the polymer backbone as side chain units. Functionalized polyaspartamides and polyamidoamines were water-soluble carriers used in this project, and they were obtained by condensation and Michael addition polymerization. Leaving group ligands (dicarboxylato, carboxylatohydroxylato, and dihydroxylato) were used to anchor the platinum drug to the polymer backbone. The platinum content of conjugates was in the range of 0.92 % - 18.15 %. A certain number of the resulting conjugates were bio-evaluated in vitro for their antiproliferative activities against the HeLa, Colo 320 DM and MCF 7 human cancer cell lines, while the corresponding carriers were in vitro tested for toxicity against resting and stimulated human lymphocyte cell lines. For 50 % cell growth inhibition, concentrations varying from 0.000044 to 9 μg/mL Pt for conjugates and 4 to >50 μg/mL for carriers were reported.en
dc.identifier.urihttp://hdl.handle.net/10539/6852
dc.language.isoenen
dc.titlePolymeric carriers in medicineen
dc.typeThesisen
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