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Phase II Reactions: Methylation Reactions01:17

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Methylation is a phase II biotransformation process involving the attachment of a methyl group to a substrate. Enzymes known as methyltransferases orchestrate this reaction.
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Related Experiment Video

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Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
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Au@SiO2 core-shell structure involved with methotrexate: Fabrication, biodegradation process and bioassay explore.

Xiaolei Huo1, Chaofan Dai1, Deying Tian1

  • 1Jiangsu Key Laboratory of Biofunctional Material, College of Chemistry and Material Science, Nanjing Normal University, Nanjing 210023, China.

International Journal of Pharmaceutics
|October 31, 2015
PubMed
Summary

A novel Au@SiO2 core-shell nanoparticle effectively loads methotrexate (MTX) for enhanced cancer therapy. This drug delivery system shows significant tumor inhibition, amplified by photothermal therapy.

Keywords:
AuCore–shell structureDrug deliveryMethotrexateSiO(2)

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Area of Science:

  • Materials Science
  • Nanotechnology
  • Drug Delivery

Background:

  • Methotrexate (MTX) is a chemotherapy drug.
  • Gold nanoparticles (Au NPs) offer unique optical properties.
  • SiO2 shells provide a protective and controllable environment.

Purpose of the Study:

  • To develop a core-shell Au@SiO2 nanoparticle for MTX drug delivery.
  • To investigate the drug-loading capacity and release profile.
  • To evaluate the in vitro anticancer efficacy and potential for photothermal therapy.

Main Methods:

  • Synthesis of Au@SiO2 core-shell nanoparticles with MTX loading.
  • Characterization of drug-loading efficiency based on Au and MTX content.
  • Biodegradation studies in phosphate buffer solution (PBS) at 37°C.
  • In vitro bioassays to assess tumor inhibition and photothermal enhancement.

Main Results:

  • A stable Au@SiO2 core-shell structure was successfully synthesized, encapsulating MTX.
  • Drug-loading capacity was significantly influenced by the core-shell architecture.
  • Biodegradation occurred in two stages: drug release/fragmentation and SiO2 dissolution.
  • Significant in vitro tumor inhibition was observed, enhanced by photothermal therapy.

Conclusions:

  • The Au@SiO2 core-shell structure is a promising platform for MTX delivery.
  • The nanoparticles demonstrate effective tumor inhibition, with potential for synergistic photothermal therapy.
  • This approach offers a new strategy for targeted cancer treatment.