The preparation and characterization of gold-conjugated polyphenol nanoparticles as a novel delivery system

Int J Nanomedicine. 2012:7:1623-33. doi: 10.2147/IJN.S30060. Epub 2012 Mar 28.

Abstract

Nanogold particles are commonly used in nanomedicine. We generated physical nanogold (pNG) conjugated with different ratios of epigallocatechin-3-gallate (EGCG) and evaluated its physicochemical properties, antioxidant activity, and cytotoxicity in vitro as well as anticancer activity in vivo. Results showed that the EGCG-pNG conjugates were successfully prepared at ratios between 23:1 and 23:5, with the percentage of EGCG content increasing with the EGCG:pNG ratio from 23:1 (2.0% ± 0.02%) to 23:5 (28% ± 0.3%). EGCG-pNG particles at ratios of 23:1 and 23:5 demonstrated significantly decreased size from 500 to 20 nm and decreasing zeta potentials of 21 mV to -22 mV, respectively. At a ratio of 23:2.5, the EGCG-pNG particles (27% EGCG, 50 nm in size, zeta potential of -8 mV) showed longer EGCG activity half-life (110 days vs 5 hours), controlled release (2 hours vs 30 minutes), and higher antioxidant activity (four times), as well as inhibition of tumor cell growth, than controls. The present study indicated that EGCG-pNG possesses promising therapeutic potential, based on its strong free-radical scavenging and anticancer activities.

Keywords: EGCG; antioxidant; antitumor activity; nanogold; nanoparticles.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / administration & dosage
  • Antineoplastic Agents / chemistry*
  • Antioxidants / administration & dosage
  • Antioxidants / chemistry*
  • Catechin / administration & dosage
  • Catechin / analogs & derivatives*
  • Catechin / chemistry
  • Cell Survival / drug effects
  • Chromatography, High Pressure Liquid
  • Drug Carriers / administration & dosage
  • Drug Carriers / chemistry*
  • Drug Stability
  • Female
  • Gold / chemistry*
  • Hydrogen-Ion Concentration
  • Metal Nanoparticles / chemistry*
  • Mice
  • Mice, Inbred C3H
  • Microsomes, Liver / metabolism
  • Neoplasms, Experimental / drug therapy
  • Neoplasms, Experimental / metabolism
  • Neoplasms, Experimental / pathology
  • Particle Size
  • Time Factors
  • Xenograft Model Antitumor Assays

Substances

  • Antineoplastic Agents
  • Antioxidants
  • Drug Carriers
  • Gold
  • Catechin
  • epigallocatechin gallate