Applications of graphene-based nanomaterials in drug design: The good, the bad and the ugly

ABSTRACT

Introduction

Graphene-based materials (GBMs) have unique physicochemical properties that make them extremely attractive as platforms for the design of new drugs. Indeed, their bidimensional (2D) morphology, high surface area, mechanical and optical properties, associated to different possibilities for functionalization of their surface, provides opportunities for their use as nanomedicines for drug delivery and/or phototherapies.

Areas covered

This opinion paper provides an overview of the current status of GBMs in drug design, with a focus on their therapeutic applications, potential environmental and health risks, and some controversial results. The authors discuss the chemical modifications of GBMs for the treatment of various diseases. The potential toxicity associated with some GBMs is also presented, along with a safe-by-design approach to minimize the risks. Finally, the authors address some issues associated to the use of GBMs in the biomedical field, such as contradictory antibacterial effects, fluorescence quenching and imprecise chemical functionalization.

Expert opinion

GBMs are a promising and exciting area of research in drug delivery. It is however important that responsible and safe use of these materials is ensured to fully exploit their advantages and overcome their drawbacks.

KEYWORDS:

• Graphene-based materials
• functionalization
• safety
• toxicity
• biomedicine

Article highlights

• GBMs can be covalently or non-covalently functionalized for drug design, and their combination with phototherapies, chemotherapy and gene therapy can enhance therapeutic outcomes

• GBMs exhibit biodegradability, and strategies to improve degradation have been explored for safer drug delivery applications

• The potential environmental and health risks associated with GBMs are discussed, including the risks of oxidative stress, cell membrane damage, and genotoxicity

• Strategies to minimize the negative effects of GBMs, such as a suitable functionalization and the formation of a protein corona, are proposed

• There are controversial studies on the antimicrobial and fluorescence properties of GO, as the mechanisms are not fully clarified, and quenching is occurring when fluorescent probes are conjugated to GO

• A controlled functionalization of GBMs is essential for reproducibility and reducing potential toxicity

• A thorough characterization of GBMs is needed to confirm the chemical reaction outcomes and to assess actual structure and morphology of the final conjugates

Declaration of interest

Z Gao and S Qin have received PhD internships from the Chinese Scholarship Council. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

Reviewer Disclosures

Peer reviewers on this manuscript have no relevant financial or other relationships to disclose.

Additional information

Funding

The authors gratefully acknowledge the support of the Centre National de la Recherche Scientifique (CNRS) and the International Center for Frontier Research in Chemistry (icFRC), as well as financial support from the Agence Nationale de la Recherche (ANR) through the Interdisciplinary Thematic Institute ITI- CSC via the IdEx Unistra (ANR-10- IDEX-0002) within the program “Investissements d’Avenir”. The authors also declare support from the EU Graphene Flagship (Grant Agreement ID: 881603).