4.6 Article

Effect of polycation nanostructures on cell membrane permeability and toxicity

Journal

ENVIRONMENTAL SCIENCE-NANO
Volume 9, Issue 2, Pages 702-713

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/d1en01156a

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Funding

  1. National Science Centre Poland [2019/35/B/ST5/02147]

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This study investigates the interaction between polycation nanostructures and cell membranes and their impact on cytotoxicity. The results show that polycations with short alkyl groups have the highest cytotoxicity and the ability to form pores in biomembranes.
The interaction of nanometric synthetic materials with cell membranes is one of the key factors determining their possible cytotoxicity. This work investigated the interaction of polycation nanostructures with lipid and cellular membranes. The nanostructures (polymer micelles) were formed in aqueous media as a result of the self-assembly of strong amphiphilic polycations containing hydrophobic alkyl groups of various lengths. The effect of alkyl length on micellization and its influence on the physicochemical properties and biological activity of the polycations were analyzed. Next, the cytotoxicity of the polycations was assessed using human skin fibroblasts (HSFs). The results show that the ability of the polycations to form pores in biomembranes decreases with the length of the attached alkyl groups. The polycations substituted with short alkyl groups were the most cytotoxic, which correlates well with their high capacity to open pores in biomembranes. However, they can perforate the fibroblast plasma membrane at non-toxic concentrations. Overall, our results show that the observed trends in cytotoxicity cannot be fully explained within simple interactions between polycationic micelles and cell membranes. A relationship does, however, seem to exist between polycation membrane activity (pore formation) and its cytotoxicity.

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