A1 Refereed original research article in a scientific journal
In vitro Targetability Validation of Peptide-Functionalized Mesoporous Silica Nanoparticles in the Presence of Serum Proteins
Authors: Paramonov Valeriy M, Gerstenberg Melanie, Sahlgren Cecilia, Lindén Mika, Rivero-Müller Adolfo
Publisher: FRONTIERS MEDIA SA
Publication year: 2020
Journal: Frontiers in Chemistry
Journal name in source: FRONTIERS IN CHEMISTRY
Journal acronym: FRONT CHEM
Article number: ARTN 603616
Volume: 8
Number of pages: 15
ISSN: 2296-2646
eISSN: 2296-2646
DOI: https://doi.org/10.3389/fchem.2020.603616
Web address : https://www.frontiersin.org/articles/10.3389/fchem.2020.603616/full
Self-archived copy’s web address: https://research.utu.fi/converis/portal/detail/Publication/51285409
Demonstration of receptor-mediated targeting of nanoparticles to specific organs and/or cell types is an integral aim in many bionanomedicine development projects. However, engagement of targeted receptors with ligands on nanocarriers, which is the cornerstone of the active targeting concept, is challenging to study under biologically relevant conditions and thus often stays overlooked. In this work, we utilize an in-house established bioassay for in vitro targetability validation of mesoporous silica nanoparticles (MSNs), functionalized with high-affinity peptide ligands to somatostatin receptors via protective group chemistry, ensuring the correct orientation of the peptide's pharmacophore. We demonstrate that targeted nanoparticles, but not scrambled peptide-decorated counterparts, specifically engage the targeted receptors in living cells in culture media containing serum protein. The importance of being able to exclude false positives originating from the premature detachment of targeting peptides from the MSNs is highlighted.
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