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Biocompatible polymer nanomaterials with non-steroid drugs tailored for anti-inflammation therapy
Běhalová, Kateřina ; Etrych, Tomáš (advisor) ; Kovář, Marek (referee)
The main aim of this bachelor thesis was synthesis and physico-chemical and preliminary biological characterization of water-soluble biocompatible polymeric system for targeted delivery of acetylsalicylic acid to inflamed tissue. Such polymer conjugates should be employed in the future for the therapeutic use within the treatment of chronic inflammatory diseases. The project included the preparation of a series of suitable acetylsalicylic acid derivatives and the synthesis of a polymeric carrier based on N-(2-hydroxypropyl) methacrylamide copolymer. Finally, the acetylsalicylic acid derivative was attached to the polymer forming a polymeric conjugate with pH-sensitive bond between the drug derivative and polymer chain, thus allowing controlled release of the drug in the target site. The work includes SEC, NMR and HPLC characterization of all synthesized compounds, verification of their stability in solutions with different pH and results of the release of drug derivatives from the polymeric carrier at physiological pH, or mildly acidic pH modeling inflamed environment. Moreover, the cytotoxicity bioassay of acetylsalicylic acid derivatives using LDH assay did not prove any cytoxicity at the level of necrotic activity. Also, their cyclooxygenase 1 inhibitory activity was observed and discussed. The polymeric...
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Biocompatible polymer nanomaterials with dexamethasone tailored for anti-inflammation therapy
Starenko, Daniil ; Etrych, Tomáš (advisor) ; Indra, Radek (referee)
Chronic inflammatory diseases are very common and affect lives of many people around the world. Moreover, in long-term effect chronic inflammation can lead to the development of such complications as diabetes, atherosclerosis and oncological diseases. Temporary therapy does not lead to complete recovery of a patient, but can provide a relief of symptoms by means of immunosuppression, which causes many adverse effects, because of long-term and nonselective drug activity. Application of the polymeric drug delivery systems is one of the actively researched ways for the improvement of inflammatory diseases treatment quality, which enables longer circulation, better distribution and controlled release of the drug. Dexamethasone is one of the commonly used glucocorticoid drugs used for treatment of chronic inflammatory diseases. Properties of this drug can be enhanced via polymeric drug delivery systems. Recently, so-called biological treatment, particularly employing monoclonal antibodies, against inflammation was introduced into the clinical use. One of such is infliximab - chimeric monoclonal antibody, which acts like the inhibitor of tumor necrotizing factor α (TNF-α). Presented bachelor thesis focuses on the synthesis and characterization of a polymer conjugates based on...
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