Abstract
We developed camptothecin (CPT)-conjugated, core-cross-linked (CCL) micelles that are subject to redox-responsive cleavage of the built-in disulfide bonds, resulting in disruption of the micellar structure and rapid release of CPT. CCL micelles were prepared via coprecipitation of disulfide-containing CPT-poly(tyrosine(alkynyl)-OCA) conjugate and monomethoxy poly(ethylene glycol)-b-poly(tyrosine(alkynyl)-OCA), followed by cross-linking of the micellar core via azide-alkyne click chemistry. CCL micelles exhibited excellent stability under physiological conditions, while they underwent rapid dissociation in reduction circumstance, resulting in burst release of CPT. These redox-responsive CCL micelles showed enhanced cytotoxicity against human breast cancer cells in vitro.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, U.S. Gov't, Non-P.H.S.
MeSH terms
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology*
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Camptothecin / chemical synthesis
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Camptothecin / chemistry
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Camptothecin / pharmacology*
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Cell Proliferation / drug effects
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Cell Survival / drug effects
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Click Chemistry
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Cross-Linking Reagents / chemical synthesis
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Cross-Linking Reagents / chemistry
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Cross-Linking Reagents / pharmacology*
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Disulfides / chemistry
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Dose-Response Relationship, Drug
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Drug Screening Assays, Antitumor
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Humans
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MCF-7 Cells
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Micelles
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Models, Molecular
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Molecular Structure
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Oxidation-Reduction
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Particle Size
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Structure-Activity Relationship
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Surface Properties
Substances
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Antineoplastic Agents
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Cross-Linking Reagents
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Disulfides
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Micelles
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Camptothecin