Medicinal Chemistry and Drug Design

Polymer vesicles, are attracting much attention as alternative nanodelivery system to implement drug targeting strategies. Polymersomes have several interesting features. For instance, ease of chemical modification of the polymer chains can be used to modulate their tissue specificity and organ distribution. A wide variety of polymers is available, however a good candidate for pharmaceutical formulations is the di-block copolymer poly(dimethylsiloxane)-b-poly(2-methyloxazoline) (PDMS-PMOXA). This polymer is formed by two subunits which are FDA approved for the development of novel nanomaterials with a potential human use. In our work we are developing a responsive nanomaterial for the treatment of breast cancer. In order to develop a targeted delivery system a very good understanding of the cancer biology is necessary. In particular cancer biomarker are of particular interest due to their specificity for cancer cells. The enzyme family of cathepsins are highly expressed in certain type of cancers as breast tumor. Moreover, they are responsible for the degradation of proteins in the lysosomes. The elevate expression of these enzymes in tumors is an evidence of the increased metabolism of cancer cells. For this reason, these enzymes are a very interesting target for the development of a novel nanomaterial. In this work we are presenting a peptide cross linked polymeric nanoparticle with the main goal to encapsulate anticancer compounds and to release them only upon activation of the system by cathpesin B.

Recent Publications

1. F. Porta and Alexander Kros, Colloidosomes as single implantable beads for the in vivo delivery of hydrophobic drugs, Particles & Particles Systems Characterization, 2013, 30, 606-613
2. P. Nadrah, F. Porta, O. Planinšek, A. Kros, M. GaberšÄek , Poly(propylene imine) dendrimer caps on mesoporous silica nanoparticles for redox-responsive release: smaller is better, PCCP, 2013, 15, 10740-10748
3. D. Witzigmann, S. Sieber, F. Porta, P. Grossen, A. Bieri, N. Strelnikova, T. Pfohl, C. Prescianotto-Baschong and J. Huwyler, Formation of lipid and polymer based gold nanohybrids using a nanoreactor approach, RCS Adv., 2015, 5, 74320
4. D. Gliesche, J. Hussner, D. Witzigmann, F. Porta, T. Glatter, A. Schmidt, J. Huwyler, H. Meyer zu Schwabedissen, Secreted Matrix Metalloproteinase-9 of proliferating smooth muscle cells as a trigger for drug release from stent surface polymers in coronary arteries, Mol. Pharm., 2016, 13 (7), 2290-2300,
5. D. Witzigmann, P. Detampel, F. Porta, J. Huwyler, Isolation of multiantennary N-glycans from glycoproteins for hepatocyte specific targeting via the asialoglycoprotein receptor, RCS Adv., 2016, 6, 97636-97640,