Transferrin-functionalized nanographene oxide for delivery of platinum complexes to enhance cancer-cell selectivity and apoptosis-inducing efficacy

Abstract

Hai Zhu,1 Binwei Zhou,2 Leung Chan,2 Yanxin Du,1 Tianfeng Chen1 1Department of Internal Medicine and Orthopedics, Guangdong Provincial Hospital of Traditional Chinese Medicine, 2Department of Chemistry, Jinan University, Guangzhou, China Abstract: Rational design and construction of delivery nanosystems for anticancer metal complexes is a crucial strategy to improve solubility under physiological conditions and permeability and retention behavior in tumor cells. Therefore, in this study, we designed and synthesize a transferrin (Tf)-conjugated nanographene oxide (NGO) nanosystem as a cancer-targeted nanocarrier of Pt complexes (Tf-NGO@Pt). This nanodelivery system exhibited good solubility under physiological conditions. Moreover, Tf-NGO@Pt showed higher anticancer efficacy against MCF human breast cancer cells than the free Pt complex, and effectively inhibited cancer-cell migration and invasion, with involvement of reactive oxygen species overproduction. In addition, nanolization also enhanced the penetration ability and inhibitory effect of the Pt complex toward MCF7 breast cancer-cell tumor spheroids. The enhancement of anticancer efficacy was positively correlated with increased cellular uptake and cellular drug retention. This study provides a new strategy to facilitate the future application of metal complexes in cancer therapy. Keywords: cancer targeting, nanographene oxide, nanomedicine, transferrin, platinum complex, cell apoptosis

Keywords

• cancer targeting
• nanographene oxide nanomedicine
• transferrin
• platinum complex
• cell apoptosis