Abstract
Efficient intracellular translocation is achieved using an easily prepared hyperbranched polysulfonamine that remains negatively charged at physiological pH. Investigations on the cellular uptake mechanism and the subcellular distribution of PSA are reported. The in vitro cytotoxicity of PSA is found to be low. Using doxorubicin as a model drug, a PSA/drug complex is prepared by electrostatic interaction with a high drug payload that exhibits a controlled release in response to pH. Efficient intracellular drug delivery, strong growth inhibition of tumor cells, and low cytotoxicity to normal cells are observed. The results suggest a possible way to utilize anionic polymers for intracellular delivery of therapeutic moieties or drugs.
Copyright © 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Amines / chemistry*
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Amines / metabolism
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Animals
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Anions / chemistry
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Biological Transport
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Cell Proliferation / drug effects
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Cell Survival / drug effects
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Delayed-Action Preparations / chemical synthesis*
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Delayed-Action Preparations / metabolism
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Doxorubicin / chemistry
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Doxorubicin / pharmacology*
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Drug Carriers / chemical synthesis*
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Drug Carriers / metabolism
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Endocytosis
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Fluorescein-5-isothiocyanate / analysis
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HEK293 Cells
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Humans
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Hydrogen-Ion Concentration
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Mice
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NIH 3T3 Cells
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Neoplasms / drug therapy
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Polymers / chemistry*
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Polymers / metabolism
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Static Electricity
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Sulfones / chemistry*
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Sulfones / metabolism
Substances
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Amines
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Anions
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Delayed-Action Preparations
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Drug Carriers
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Polymers
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Sulfones
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polysulfone P 1700
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Doxorubicin
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Fluorescein-5-isothiocyanate