The Role of Hydrophobicity in the Cellular Uptake of Negatively Charged Macromolecules.
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.
['Abou Matar|Tamara|T|', 'Karam|Pierre|P|0000-0003-4550-7641']
D002470:Cell Survival D004705:Endocytosis D005453:Fluorescence D006367:HeLa Cells D006801:Humans D057927:Hydrophobic and Hydrophilic Interactions D046911:Macromolecular Substances D057054:Molecular Imaging D053758:Nanoparticles D011108:Polymers
hydrophobic cellular uptake negatively charged macromolecules conjugated polyelectrolytes