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(RAFT) is particularly well suited to syn-
thesize sulfur-end-functionalized polymers
due to the use of thiocarbonate RAFT
chain transfer agents (CTAs).
[4]
It is known that size, shape, and surface
chemistry of goldNP affect their uptake
by living cells.
[5]
However, few have been
reported on whether altering the hydro-
philic-to-hydrophobic ratio of a polymer
coating can affect cellular interaction. In this paper we report
on goldNP decorated with a series of polymers that differ in
their hydrophilic-to-hydrophobic comonomer ratio and investi-
gate how the latter affects cellular uptake. In addition, we devel-
oped a novel flow cytometry method for label-free investigation
of goldNP-cell interaction. This methodology is then used to
investigate the different parameters that affect the interaction
of the goldNP and in vitro cultured cells.
2. Results and Discussion
Copolymers composed of the hydrophilic 2-hydroxyethylacrylate
(HEA) and the hydrophobic methoxyethylacrylate (MEA) were
obtained by RAFT in an automated parallel synthesis robot
to minimize batch-to-batch variation.
[6]
Polymers with a theo-
retical degree of polymerization (DP; monomer to CTA ratio)
of 100 and HEA:MEA ratios of 100:0, 80:20, 60:40, 50:50,
40:60, and 20:80, respectively, were synthesized according to
Scheme 1. For clarity of presentation these polymers will fur-
ther on be denoted as HEA
x
MEA
y
( x and y represent HEA and
MEA to CTA ratio, respectively). Polymerization was stopped at
a conversion of approximately 65% to ensure good chain end-
fidelity of the polymers and Table S1, Supporting Information,
summarizes their properties. In all cases linear first order poly-
merization kinetics (Figure S1, Supporting Information) were
observed and good control over the polymerizations was fur-
ther evidenced by dispersities below 1.3. As reported earlier by
Hoogenboom et al., copolymers of HEA and MEA have an ideal
random monomer distribution
[7]
which was confirmed in our
present study. The polymers HEA
40
MEA
60
and HEA
20
MEA
80
appeared to by insoluble in water at room temperature or above
and were not included in further experiments.
13 nm (size measured by transmission electron micro-
scopy (TEM)) citrate-stabilized goldNP were synthesized by the
Tailoring Cellular Uptake of Gold Nanoparticles Via the
Hydrophilic-to-Hydrophobic Ratio of their (Co)polymer
Coating
Zhiyue Zhang, Katleen Van Steendam, Samarendra Maji, Lieve Balcaen,
Yulia Anoshkina, Qilu Zhang, Glenn Vanluchene, Riet De Rycke, Frank Van Haecke,
Dieter Deforce, Richard Hoogenboom,* and Bruno G. De Geest*
It is demonstrated how cellular uptake and protein corona of (co)polymer-
coated gold nanoparticles can be altered by the hydrophilic-to-hydrophobic
comonomer ratio. A novel, label-free flow cytometry strategy is developed
to investigate particle uptake. These findings offer insight in the design and
analysis of hybrid nanomaterials for interfacing with biological systems.
DOI: 10.1002/adfm.201500904
Z. Zhang, Dr. K. Van Steendam, Prof. D. Deforce,
Prof. B. De Geest
Department of Pharmaceutics
Ghent University
9000 Ghent, Belgium
E-mail: br.degeest@ugent.be
Dr. S. Maji, Dr. Q. Zhang, G. Vanluchene,
Prof. R. Hoogenboom
Supramolecular Chemistry Group
Department of Organic and Macromolecular Chemistry
Ghent University
9000 Ghent, Belgium
E-mail: richard.hoogenboom@ugent.be
Dr. L. Balcaen, Y. Anoshkina, Prof. F. Van Haecke
Department of Analytical Chemistry
Ghent University
9000 Ghent, Belgium
R. De Rijcke
Department of Biomedical Molecular Biology
Ghent University
9000 Ghent, and Inflammation Research Center
VIB, 9052 Zwijnaarde, Belgium
1. Introduction
The design of engineered nanoparticles that can interact with
living cells and tissues is important for many biomedical appli-
cations, including imaging, diagnostics, and drug delivery.
[1]
Gold nanoparticles (goldNP) have attracted major interest due
to their chemical stability, cytocompatibility, and their tunable
optical and electronic properties.
[2]
Furthermore, (quasi) cova-
lent surface functionalization of metallic gold is straightforward
using sulfur-containing compounds that form self-assembled
monolayers.
[3]
Polymer-decoration of goldNP is attractive to
modulate the goldNP properties and to render them colloidally
stable in complex media. To produce polymer-decorated goldNP,
reversible addition fragment chain-transfer polymerization
Adv. Funct. Mater. 2015, 25, 3433–3439
www.afm-journal.de
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