Surface functionalized gold nanoparticles for drug delivery

J Biomed Nanotechnol. 2013 Aug;9(8):1362-9. doi: 10.1166/jbn.2013.1536.

Abstract

Gold nanoparticles have been widely explored as cancer therapeutics and diagnostic agents in recent years. With their unique subcellular size and good biocompatibility, gold nanoparticles are a promising drug delivery vehicle. In this study, folic acid-coated gold nanoparticles conjugated with fluorophore FITC through amine terminated poly(ethylene glycol) were prepared and confocal microscopy together with bright-field differential interference contrast imaging data showed that folic acid-coated gold nanoparticles accumulated mainly in cytoplasm of primary human fibroblasts, without causing any observable cytotoxicity upon exposure for 48 hours. Through the further development of a drug delivery system that conjugates doxorubicin onto the surface of gold nanoparticles with a poly(ethylene glycol) spacer via an SMCC linker, we demonstrated that multidrug resistance in cancer cells can be significantly overcome by a combination of highly efficient cellular entry and enhanced cytotoxicity of Au-SMCC-DOX nanoconjugates, as revealed both by confocal microscopy imaging and cytotoxicity assay. The prepared Au-SMCC-DOX nanoconjugates demonstrated enhanced drug accumulation and retention in multidrug resistant hepG2-R cancer cells when it was compared with free doxorubicin, with a cytoplasm accumulation profile. The results indicated that gold nanoparticles are a kind of promising drug delivery vehicle with good biocompatibility and suitable for further applications in drug delivery for improved chemotherapy, especially for overcoming multidrug resistance.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / administration & dosage
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacokinetics
  • Coated Materials, Biocompatible* / chemistry
  • Coated Materials, Biocompatible* / therapeutic use
  • Doxorubicin / administration & dosage
  • Doxorubicin / chemistry
  • Doxorubicin / pharmacokinetics
  • Drug Carriers / chemical synthesis
  • Drug Carriers / chemistry
  • Drug Carriers / therapeutic use
  • Drug Delivery Systems*
  • Drug Evaluation, Preclinical
  • Drug Resistance, Neoplasm / drug effects
  • Gold / chemistry*
  • Hep G2 Cells
  • Humans
  • Materials Testing
  • Metal Nanoparticles / chemistry
  • Metal Nanoparticles / therapeutic use*
  • Models, Biological
  • Nanoconjugates / administration & dosage
  • Nanoconjugates / chemistry
  • Polyethylene Glycols / administration & dosage
  • Polyethylene Glycols / chemistry
  • Surface Properties

Substances

  • Antineoplastic Agents
  • Coated Materials, Biocompatible
  • Drug Carriers
  • Nanoconjugates
  • Polyethylene Glycols
  • Gold
  • Doxorubicin