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Hsiao, I.L.* ; Fritsch-Decker, S.* ; Leidner, A.* ; Al-Rawi, M.* ; Hug, V.* ; Diabaté, S.* ; Grage, S.L.* ; Meffert, M.* ; Stöger, T. ; Gerthsen, D.* ; Ulrich, A.S.* ; Niemeyer, C.M.* ; Weiss, C.*

Biocompatibility of amine-functionalized silica nanoparticles: The role of surface coverage.

Small 15:1805400 (2019)
Postprint DOI
Open Access Green
Here, amorphous silica nanoparticles (NPs), one of the most abundant nanomaterials, are used as an example to illustrate the utmost importance of surface coverage by functional groups which critically determines biocompatibility. Silica NPs are functionalized with increasing amounts of amino groups, and the number of surface exposed groups is quantified and characterized by detailed NMR and fluorescamine binding studies. Subsequent biocompatibility studies in the absence of serum demonstrate that, irrespective of surface modification, both plain and amine-modified silica NPs trigger cell death in RAW 264.7 macrophages. The in vitro results can be confirmed in vivo and are predictive for the inflammatory potential in murine lungs. In the presence of serum proteins, on the other hand, a replacement of only 10% of surface-active silanol groups by amines is sufficient to suppress cytotoxicity, emphasizing the relevance of exposure conditions. Mechanistic investigations identify a key role of lysosomal injury for cytotoxicity only in the presence, but not in the absence, of serum proteins. In conclusion, this work shows the critical need to rigorously characterize the surface coverage of NPs by their constituent functional groups, as well as the impact of serum, to reliably establish quantitative nanostructure activity relationships and develop safe nanomaterials.
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Publication type Article: Journal article
Document type Scientific Article
Corresponding Author
Keywords Cytotoxicity ; Macrophages ; Silica Nanoparticles ; Surface-characterization ; Surface-functionalization; In-vivo; Toxicity; Nanomaterials; Particles; Cells; Categorization; Instillation; Exposure; Stress; Design
ISSN (print) / ISBN 1613-6810
e-ISSN 1613-6829
Journal Small
Quellenangaben Volume: 15, Issue: 10, Pages: , Article Number: 1805400 Supplement: ,
Publisher Wiley
Publishing Place Postfach 101161, 69451 Weinheim, Germany
Non-patent literature Publications
Reviewing status Peer reviewed
Institute(s) Lung Health and Immunity (LHI)