Abstract
A new acidly sensitive PEGylated polyethylenimine linked by Schiff base (PEG-s-PEI) was designed to render pH-sensitive PEGylation nanoassemblies through multiple interactions with indomethacin and docetaxel (DTX). DTX nanoassemblies driven by PEG-s-PEI thus formulated exhibited an excellent pH-sensitivity PEGylation cleavage performance at extracellular pH of tumor microenvironment, compared to normal tissues, thereby long circulated in blood but were highly phagocytosed by tumor cells. Consequently, this smart pH-sensitive PEGylation cleavage provided an efficient strategy to target tumor microenvironment, in turn afforded superior therapeutic outcome in anti-tumor activity.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antineoplastic Agents / administration & dosage
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacokinetics
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Cell Proliferation / drug effects*
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Docetaxel / administration & dosage*
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Docetaxel / chemistry
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Docetaxel / pharmacokinetics
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Drug Carriers / administration & dosage*
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Drug Carriers / chemistry
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Drug Delivery Systems*
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Humans
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Hydrogen-Ion Concentration
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Indomethacin / administration & dosage
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Indomethacin / chemistry
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Indomethacin / pharmacokinetics
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Male
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Nanostructures / administration & dosage
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Nanostructures / chemistry
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Neoplasms, Experimental / drug therapy*
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Neoplasms, Experimental / pathology
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Polyethylene Glycols / chemistry*
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Polyethyleneimine / chemistry*
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Rats
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Rats, Sprague-Dawley
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Tissue Distribution
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Tumor Cells, Cultured
Substances
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Antineoplastic Agents
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Drug Carriers
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Docetaxel
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Polyethylene Glycols
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Polyethyleneimine
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Indomethacin