Anti-cancer active nano carbon drug conjugate based on an Aryl Azide using the classical ‘click’ chemistry

Objective(s): Nano Carbon Drug Conjugates (NCDCs) are created by attaching therapeutic agents to nanocarbon structures such as Fullerene (C60), Single-Walled Carbon Nanotubes (SWCNT), Graphene Oxide (GO), and Reduced Graphene Oxide (rGO). These conjugated nanocarriers exhibit outstanding characteristics, including a high surface area, ease of functionalization, and the ability to penetrate biological barriers.Materials and Methods: The conjugation of drugs to these nanocarriers enhances the solubility, stability, and bioavailability of the drugs, potentially overcoming the limitations of conventional drug delivery systems, such as cytotoxicity and side effects. The design of Nano Carbon Drug Conjugates (NCDCs) requires careful consideration of factors like the Drug-to-Nanocarbon Ratio (DNR), the choice of linker, and the selection of a targeting moiety to ensure selective accumulation in diseased tissues while minimizing off-target effects. NCDCs have broad applications in various medical fields, with a significant emphasis on cancer therapy (oncology), where they can deliver cytotoxic agents directly to tumor cells, thereby reducing systemic toxicity.Results: This paper focuses on synthesis and characterizing a novel nanocarbon drug conjugate based on conventional 'click' chemistry, offering an improved approach for conjugating nanocarbons [(e.g. Fullerene C60)] with therapeutic agents. Additionally, it explores whether these conjugates could serve as theranostic agents.Conclusions: The cytotoxicity of the newly prepared conjugate was evaluated using the MTT assay, and the cell survival rate was 87.68% at 10 µM and 79.73% at 20 µM, respectively, after 36 hours of treatment. Western blot analysis revealed significant expression of apoptosis markers, including Bax, Caspase 9, Cleaved Caspase 9, and Cytc, at 10 µM and 20 µM concentrations.