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The Role of Hydrophobicity in the Cellular Uptake of Negatively Charged Macromolecules
Author(s) -
Abou Matar Tamara,
Karam Pierre
Publication year - 2018
Publication title -
macromolecular bioscience
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.924
H-Index - 105
eISSN - 1616-5195
pISSN - 1616-5187
DOI - 10.1002/mabi.201700309
Subject(s) - macromolecule , chemistry , amphiphile , polyelectrolyte , nanocarriers , biophysics , polymer , side chain , polyvinylpyrrolidone , sulfonate , membrane , intracellular , polymer chemistry , copolymer , organic chemistry , drug delivery , biochemistry , sodium , biology
It is generally accepted that positively charged molecules are the gold standard to by‐pass the negatively charged cell membrane. Here, it is shown that cellular uptake is also possible for polymers with negatively charged side chains and hydrophobic backbones. Specifically, poly[5‐methoxy‐2‐(3‐sulfopropoxy)‐1,4‐phenylenevinylene], a conjugated polyelectrolyte with sulfonate, as water‐soluble functional groups, is shown to accumulate in the intracellular region. When the polymer hydrophobic backbone is dissolved using polyvinylpyrrolidone, an amphiphilic macromolecule, the cellular uptake is dramatically reduced. The report sheds light on the fine balance between negatively charged side groups and the hydrophobicity of polymers to either enhance or reduce cellular uptake. As a result, these findings will have important ramifications on the future design of targeted cellular delivery nanocarriers for imaging and therapeutic applications.