Ectoenzymes as promising cell identification structures for the high avidity targeting of polymeric nanoparticles.

Pharmacotherapy is often limited by undesired side effects while insufficient drug reaches the site of action. Active-targeted nanotherapy should provide a solution for this problem, by using ligands in the nanoparticle corona for the identification of receptors on the target-cell surface. However, since receptor binding is directly associated with pharmacological responses, today's targeting concepts must be critically evaluated. We hypothesized that addressing ectoenzymes would help to overcome this problem, but it was not clear if particles would show sufficiently high avidity to provide us with a viable alternative to classical ligand-receptor concepts. We scrutinized this aspect by immobilizing the highly selective angiotensin-converting enzyme 2 (ACE2) inhibitor MLN-4760 in the corona of block-copolymer nanoparticles and investigated enzyme binding via microscale thermophoresis and flow cytometry. Excellent avidities with K

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Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.