Abstract
A strategy for conjugating an antitumor agent to superparamagnetic iron oxide nanoparticles (SPIONs) via a biocleavable ester binding is reported. Paclitaxel (PTX) was selected as a model drug. Both the in vitro and in vivo performance of the conjugates of SPION-PTX was investigated respectively. PTX can be released slowly through the hydrolysis of the ester bond in a pH-dependent manner and the SPION-PTX has near equal cytotoxity to the clinical PTX injection (Taxol) at the equivalent dose of PTX. Furthermore, the SPION-PTX can accumulate in tumor tissues as demonstrated by MRI and exhibit better tumor suppression effect than Taxol in vivo. The above good performance of the SPION-PTX together with the good biocompatibility of the SPIONs would promote greatly the application of the SPIONs in the biomedicine field.
This journal is © The Royal Society of Chemistry 2012
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 Line, Tumor
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Contrast Media / chemical synthesis
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Contrast Media / chemistry
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Contrast Media / pharmacokinetics
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Dextrans* / chemistry
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Dextrans* / pharmacokinetics
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Drug Carriers / chemical synthesis
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Drug Carriers / chemistry
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Drug Carriers / pharmacokinetics
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HeLa Cells
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Humans
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Magnetite Nanoparticles* / chemistry
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Mice
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Mice, Inbred ICR
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Models, Biological
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Nanoconjugates / administration & dosage
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Nanoconjugates / chemistry
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Neoplasms / diagnosis*
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Neoplasms / drug therapy*
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Neoplasms / metabolism
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Paclitaxel / administration & dosage*
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Paclitaxel / chemistry
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Paclitaxel / pharmacokinetics
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Xenograft Model Antitumor Assays
Substances
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Antineoplastic Agents
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Contrast Media
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Dextrans
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Drug Carriers
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Magnetite Nanoparticles
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Nanoconjugates
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ferumoxides
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Paclitaxel