Targeting Somatostatin Receptors By Functionalized Mesoporous Silica Nanoparticles - Are We Striking Home?

A1 Journal article (refereed)


Internal Authors/Editors


Publication Details

List of Authors: Paramonov V, Desai D, Kettiger H, Mamaeva V, Rosenholm J, Sahlgren C, Rivero-Müller A
Publisher: Ivyspring International Publisher Pty Ltd
Publication year: 2018
Journal: Nanotheranostics
Volume number: 2
Issue number: 4
Start page: 320
End page: 346


Abstract

The concept of delivering nanoformulations to desired tissues by means
of targeting membrane receptors of high local abundance by ligands
anchored to the nanocarrier has gained a lot of attention over the last
decade. Currently, there is no unanimous opinion on whether surface
functionalization of nanocarriers by targeting ligands translates into
any real benefit in terms of pharmacokinetics or treatment outcomes.
Having examined the published nanocarriers designed to engage with
somatostatin receptors, we realized that in the majority of cases
targetability claims were not supported by solid evidence of targeting
ligand-targeted receptor coupling, which is the very crux of a
targetability concept. Here, we present an approach to characterize
targetability of mesoporous silica-based nanocarriers functionalized
with ligands of somatostatin receptors. The targetability proof in our
case comes from a functional assay based on a genetically-encoded cAMP
probe, which allows for real-time capture of receptor activation in
living cells, triggered by targeting ligands on nanoparticles. We
elaborate on the development and validation of the assay, highlighting
the power of proper functional tests in the characterization pipeline of
targeted nanoformulations.


Keywords

cAMP, cancer therapy, mesoporous silica nanoparticles, Nanomedicine, receptors, Targeting


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