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In this thesis, novel peptide-drug conjugates with antitumor activity were synthesized by linking daunomycin to targeting peptides—selected from a phage-display library—via enzyme-labile spacers. These conjugates were optimized and evaluated both in vitro and in vivo, offering potential as future therapeutic agents. A custom peptide synthesizer was developed to support peptide sequence optimization, and its functionality, cost-efficiency, and suitability for high-throughput applications were validated. The synthesizer’s compatibility with green solvents was demonstrated, with γ-valerolactone successfully replacing N,N-dimethylformamide, reducing reagent and solvent consumption. Additionally, the feasibility of electrospinning and high-speed electrospinning (HSES) was proven for formulating poorly soluble antitumor compounds such as doxycycline and curcuminoids, with the scalability of these processes confirmed. A novel injectable formulation for curcuminoids was also developed using FDA-approved 2-hydroxypropyl-β-cyclodextrin, resulting in a three orders of magnitude improvement in solubility while preserving antitumor activity in vitro.
- Kiss, K
- Budapest University of Technology and Economics Faculty of Chemical Technology and Biotechnology Department of Organic Chemistry and Technology George A Olah Doctoral School
