Deep penetration of a PDT drug into tumors by noncovalent drug-gold nanoparticle conjugates

J Am Chem Soc. 2011 Mar 2;133(8):2583-91. doi: 10.1021/ja108846h. Epub 2011 Feb 4.


Efficient drug delivery to tumors is of ever-increasing importance. Single-visit diagnosis and treatment sessions are the goal of future theranostics. In this work, a noncovalent PDT cancer drug-gold nanoparticle (Au NP) conjugate system performed a rapid drug release and deep penetration of the drug into tumors within hours. The drug delivery mechanism of the PDT drug through Au NPs into tumors by passive accumulation was investigated via fluorescence imaging, elemental analysis, and histological staining. The pharmacokinetics of the conjugates over a 7-day test period showed rapid drug excretion, as monitored via the fluorescence of the drug in urine. Moreover, the biodistribution of Au NPs in this study period indicated clearance of the NPs from the mice. This study suggests that noncovalent delivery via Au NPs provides an attractive approach for cancer drugs to penetrate deep into the center of tumors.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / administration & dosage
  • Antineoplastic Agents / pharmacokinetics*
  • Antineoplastic Agents / therapeutic use
  • Cell Line, Tumor
  • Drug Delivery Systems*
  • Female
  • Fluorescence Resonance Energy Transfer
  • Fluorescent Dyes / chemistry
  • Fluorescent Dyes / pharmacokinetics
  • Glioma / drug therapy*
  • Glioma / pathology
  • Gold / chemistry
  • Gold / pharmacology*
  • Metal Nanoparticles / chemistry*
  • Mice
  • Mice, Nude
  • Photochemotherapy*
  • Rats
  • Tissue Distribution
  • Xenograft Model Antitumor Assays


  • Antineoplastic Agents
  • Fluorescent Dyes
  • Gold