Drug delivery systems can increase the pharmacokinetic and pharmacodynamic properties of
various therapeutic agents. These systems can ensure a controlled release improve the
specificity of drugs to the target tissue and therefore decrease side effects to the healthy
surrounding tissue. In this work cell penetrating peptoids which mimic the structure of
peptides but exhibit increased stability were investigated as organelle- and organ-specific
carrier molecules. Several fluorescently labelled peptoid libraries differing for example in
length and side-chain composition were synthesized and investigated with high-throughput
screenings in different cell lines. The focus was on the elucidation of structure-function
relationships for cellular uptake intracellular localization and cytotoxicity. Furthermore
the organ targeting of the peptoids was analysed in in vivo studies by using zebrafish as model
organism. In addition the influence of the fluorescent dye on the localization and uptake of
the peptoids was investigated.
