Functional Graphene Oxide as a Nanocarrier for Controlled Loading and Targeted Delivery of Mixed Anticancer Drugs

TLDR

Combining multiple drugs often yields better therapeutic efficacy, so controlled loading and targeted delivery of mixed anticancer drugs with graphene‑based nanocarriers could have broad biomedical applications. The study reports a simple synthesis of functional nanoscale graphene oxide as a novel nanocarrier for loading and targeted delivery of anticancer drugs. The NGO is functionalized with sulfonic acid groups for physiological stability, covalently conjugated with folic acid for targeting MCF‑7 breast cancer cells, and loaded with doxorubicin and camptothecin via π‑π stacking and hydrophobic interactions. FA‑NGO loaded with both drugs showed specific targeting to MCF‑7 cells and markedly higher cytotoxicity than NGO loaded with either drug alone.

Abstract

A simple synthetic route for the preparation of functional nanoscale graphene oxide (NGO), a novel nanocarrier for the loading and targeted delivery of anticancer drugs, is reported. The NGO is functionalized with sulfonic acid groups, which render it stable in physiological solution, followed by covalent binding of folic acid (FA) molecules to the NGO, thus allowing it to specifically target MCF-7 cells, human breast cancer cells with FA receptors. Furthermore, controlled loading of two anticancer drugs, doxorubicin (DOX) and camptothecin (CPT), onto the FA-conjugated NGO (FA-NGO) via pi-pi stacking and hydrophobic interactions is investigated. It is demonstrated that FA-NGO loaded with the two anticancer drugs shows specific targeting to MCF-7 cells, and remarkably high cytotoxicity compared to NGO loaded with either DOX or CPT only. Considering that the combined use of two or more drugs, a widely adopted clinical practice, often displays much better therapeutic efficacy than that of a single drug, the controlled loading and targeted delivery of mixed anticancer drugs using these graphene-based nanocarriers may find widespread application in biomedicine.