PEGylated Nano-Graphene Oxide for Delivery of Water Insoluble Cancer Drugs

TL;DR

This study developed a PEGylated nano-graphene oxide platform that enhances water solubility and delivery of hydrophobic cancer drugs, showing superior efficacy over existing treatments in vitro.

Contribution

The paper introduces a novel NGO-PEG conjugate capable of non-covalently attaching hydrophobic drugs, improving solubility and potency for cancer therapy.

Findings

NGO-PEG-SN38 exhibits high water solubility and cancer cell killing potency.

The NGO-PEG-SN38 complex outperforms FDA-approved irinotecan in efficacy.

Graphene-based materials show promise for delivering water-insoluble drugs in cancer treatment.

Abstract

It is known that many potent, often aromatic drugs are water insoluble, which has hampered their use for disease treatment. In this work, we functionalized nano-graphene oxide (NGO), a novel graphitic material, with branched polyethylene glycol (PEG) to obtain a biocompatible NGO-PEG conjugate stable in various biological solutions, and used them for attaching hydrophobic aromatic molecules including a camptothecin (CPT) analog, SN38 non-covalently via pi-pi stacking. The resulting NGO-PEG-SN38 complex exhibited excellent water solubility while maintaining its high cancer cell killing potency similar to that of the free SN38 molecules in organic solvents. The efficacy of NGO-PEG-SN38 was far higher than that of irinotecan (CPT-11), a FDA approved water soluble SN38 prodrug used for the treatment of colon cancer. Our results showed that graphene is a novel class of material promising for biological applications including future in vivo cancer treatment with various aromatic, low-solubility drugs.