Shape and surface chemistry are important factors to regulate nanoparticle's cellular entry pathways. In this lecture, we report our recent effort of using nanobeacons to probe the shape and surface chemistry effect on the internalization efficiency of nanoparticles by cancer cells. We designed a series of self-assembling molecular beacons that can form either spherical or filamentous nanostructures depending on their self-assembly conditions. The surface chemistry of these supramolecular nanobeacons can be readily tuned through the incorporation of different C-terminal amino acids (for example, lysine gives a positively charged surface while glutamic acid gives a negatively charged surface). The beacons reported herein were designed to be specifically responsive to an enzyme located within the lysosomes. Only after specific cleavage by the targeted enzyme within the cells, the beacon molecule will start to fluoresce, giving a detectable optical signal. Our results show that spherical nanobeacons with a positively charged surface has the highest efficiency for cellular uptake, while filamentous nanostructures regardless of their charge status can hardly get into cells.

Using supramolecular nanobeacons to probe cellular uptake efficiency and enzymatic activities

247th National Meeting (2014)

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