Quantitative Cellomics high-content analysis (HCA) of cellular
uptake and endosomal escape by particles with different sizes. (a)
The image analysis modality to analyze fixed cells directly in the
tissue culture plates. Representative images are shown in (b) at 2
h and (c) at 4 h after incubation with particles of different sizes.
Quantitative results are presented in terms of (d) particle spot characteristics
(area and intensity), directly suggesting successful size control
during particle–cell interactions. (e) Gal8 spot characteristics
(area and intensity) indicating the formation of larger endosomal
vesicles by larger particles. (f) Frequency of detected particles
and Gal8 spots in cells at 2 h. (g) Average total particle intensity
per cell at all time points as a representative measure of total particle
uptake quantity. (h) Average number of Gal8 spots per cell at all
time points as an indication of endosomal escape level, serving as
a predictive index for transfection efficiency according to previous
reports using this assay. (i) Quantitative measure of overall endosomal
escape degree, i.e., average total Gal8 spot intensity per cell, due
to different Gal8 spot characteristics observed for different particle
sizes. (j) Transfection efficiencies (luciferase reporter expression
level) as a result of incubation with particles at different sizes
for different periods of time, which correlated well with the trends
of total cellular uptake and endosomal escape levels. (k) Regardless
of the particle size, fitting the overall endosomal escape level (Y axis) of all plate well-averaged data points against the
overall cellular uptake level (X axis) shows a strong
positive correlation at 2–4 h postdosage. In the figure, n = 21 wells for the fitted line of 1 h and n = 42 wells for the fitted line of 2 and 4 h. (l) Fitting the endosomal
escape level in a single cell (Y axis) of all cells
assessed in the same well of the group of 200 nm (n = 5400 cells), 400 nm (n = 4693 cells), and 900
nm (n = 4336 cells), against the cellular uptake
level in the same single cell (X axis), shows a strong
positive correlation. The figure was generated by overlapping the
FlowJo-generated pseudocolor heat maps showing the cell distribution
density with an arbitrary correlation curve plotted. In (a–c),
all figures share the same scale bar of 50 μm.