Small interfering ribonucleic acids (siRNAs) have the potential to silence genetic sequences without altering the host genome, making them a promising candidate for anti-cancer therapy. However, their large size, anionic nature, and sensitivity to degradation prevent direct use. To address this issue, numerous siRNA delivery systems, including polymeric micelles, have been investigated. This thesis reviewed different micellar polymer systems and focused on the active targeting of these compounds. The main polymeric building blocks were identified, and the safety aspect was examined.

The aim of this project was to apply computational design methods and to synthesize a tailor-made micelle for siRNA transport to minimize the risk of toxicity. The micellar model was used for predictive optimization of binding efficiency by in silico methods and applied in vitro to treat human non-small cell lung cancer cells. These cells were resected from a tumor of a patient of the University Hospitals of Geneva (HUG).

In addition, the preparation of a model antibody antigen-binding fragment that could be precisely added to the delivery system was studied. The preparation process was monitored by UPLC-HRMS.