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Functionalization of Single-walled Carbon Nanotubes with Thermo-reversible Block Copolymers and Characterization by Small-angle Neutron Scattering
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SiRNA delivery with functionalized carbon nanotubes.

Amir Khashayar Varkouhi1, Stéphanie Foillard, Twan Lammers

  • 1Department of Pharmaceutics, Utrecht Institute for Pharmaceutical Sciences, Faculty of Science, Utrecht University, Sorbonnelaan 16, 3584 CA Utrecht, The Netherlands.

International Journal of Pharmaceutics
|February 16, 2011
PubMed
Summary

Functionalized carbon nanotubes (CNTs) showed moderate siRNA delivery efficiency and significant cytotoxicity. Biodegradable carriers mimicking CNTs are preferred for future drug delivery systems.

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Area of Science:

  • Biomaterials Science
  • Nanotechnology
  • Molecular Biology

Background:

  • Carbon nanotubes (CNTs) are explored for drug and nucleic acid delivery due to their unique nano-needle structure.
  • CNTs are hypothesized to enter cells directly, bypassing endocytosis and avoiding cell death.

Purpose of the Study:

  • To investigate the efficacy of two cationically functionalized CNTs (CNT-PEI and CNT-pyridinium) for siRNA delivery.
  • To assess the cytotoxicity of these functionalized CNTs.

Main Methods:

  • Complexation of siRNA with CNT-PEI and CNT-pyridinium.
  • In vitro evaluation of gene silencing activity.
  • Assessment of cellular toxicity.

Main Results:

  • Both CNT-PEI and CNT-pyridinium complexed siRNA, achieving 10-30% silencing activity.
  • Cytotoxicity ranged from 10-60% for the functionalized CNTs.
  • No significant advantage in toxicity reduction or silencing enhancement over standard transfection systems like PEI was observed.

Conclusions:

  • The functionalization strategy is critical for developing efficient and non-cytotoxic CNT-based delivery systems.
  • Given current results and the non-degradable nature of CNTs, biodegradable carriers are recommended for future development.
  • Biodegradable carriers mimicking the CNT needle structure may offer a safer alternative for nucleic acid delivery.