Abstract: Epigallocatechin-3-gallate (EGCG) is a pleiotropic compound with anticancer,
anti-inflammatory, and antioxidant properties. To enhance EGCG anticancer efficacy, it was loaded
onto gold nanoparticles (GNPs). EGCG-GNPs were prepared by a simple green synthesis method
and were evaluated using different techniques. Hemocompatibility with human blood and in vivo
anticancer efficacy in Ehrlich ascites carcinoma-bearing mice were evaluated. EGCG/gold chloride
molar ratio had a marked effect on the formation and properties of EGCG-GNPs where well-dispersed
spherical nanoparticles were obtained at a molar ratio not more than 0.8:1. The particle size ranged
from ~26 to 610 nm. High drug encapsulation efficiency and loading capacity of ~93 and 32%,
respectively were obtained. When stored at 4 °C for three months, EGCG-GNPs maintained over 90%
of their drug payload and had small changes in their size and zeta potential. They were non-hemolytic
and had no deleterious effects on partial thromboplastin time, prothrombin time, and complement
protein C3 concentration. EGCG-GNPs had significantly better in vivo anticancer efficacy compared
with pristine EGCG as evidenced by smaller tumor volume and weight and higher mice body weight.
These results confirm that EGCG-GNPs could serve as an efficient delivery system for EGCG with a
good potential to enhance its anticancer efficacy.