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pH and hydrogen peroxide dual responsive supramolecular prodrug system for controlled release of bioactive molecules

Yin Wang1, Haibo Wang1, Yangjun Chen1

  • 1MOE Key Laboratory of Macromolecular Synthesis and Functionalization, Department of Polymer Science and Engineering, Zhejiang University, Hangzhou 310027, Zhejiang, China.

Colloids and Surfaces. B, Biointerfaces
|July 2, 2014
PubMed

Insights

Researchers developed dual-responsive smart polymers for cancer therapy. These novel nanocarriers effectively release drugs in response to low pH and hydrogen peroxide, improving cancer treatment potential.

Area of Science:

  • Biomaterials Science
  • Polymer Chemistry
  • Nanotechnology

Background:

  • Cancer remains a major global health threat, necessitating advanced therapeutic strategies.
  • Current smart drug nanocarriers often lack robustness due to single-stimulus responsiveness.
  • Multi-responsive polymers offer enhanced therapeutic efficacy but are often complex to synthesize.

Purpose of the Study:

  • To develop a facile strategy for creating dual-responsive polymers for cancer therapy.
  • To investigate the self-assembly and drug release characteristics of these novel nanocarriers.
  • To evaluate the potential of these nanocarriers for targeted cancer treatment.

Main Methods:

  • Orthogonal assembly of beta-cyclodextrin-hydrazone-doxorubicin (β-CD-hydrazone-DOX) and polyethylene glycol-ferrocene (PEG-Fc) to create dual-responsive polymers.
  • Characterization of polymer self-assembly into micelles in aqueous solutions.
  • In vitro assessment of doxorubicin (DOX) release under varying pH and hydrogen peroxide (H2O2) conditions.
  • Cellular uptake studies using fluorescence microscopy and flow cytometry.

Main Results:

  • The synthesized polymers spontaneously assembled into micelles, suitable for drug nanocarrier applications.
  • Doxorubicin (DOX) release was significantly enhanced under acidic pH (5.0) and in the presence of H2O2.
  • In vitro studies confirmed the internalization of the supramolecular prodrug micelles into cancer cells.
  • The dual-responsive system demonstrated enhanced drug release capabilities compared to single-responsive systems.

Conclusions:

  • A facile method for preparing dual-responsive (pH and H2O2) smart polymers was successfully established.
  • The self-assembled micelles show significant potential as effective nanocarriers for cancer drug delivery.
  • The enhanced drug release in response to tumor microenvironment stimuli suggests promising applications in cancer therapy.
Keywords:
Dual responsiveHost–guest interactionsProdrug micellesβ-Cyclodextrin

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