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Updated: Feb 1, 2026

Scalable Syntheses of Graphene Oxide and Reduced Graphene Oxide using Cascade Design Oxidation and Highly Basic Reduction Reactions
Published on: July 3, 2025
Targeted Graphene Oxide Networks: Cytotoxicity and Synergy with Anticancer Agents
Elham Bidram1, Adrian Sulistio2, Hyun-Jung Cho
1Department of Biotechnology, Faculty of Advanced Sciences & Technologies , University of Isfahan , Isfahan 81746 , Iran.
Abstract:
An effective strategy to inhibit endocytosis in cancer cells is presented where modified net-type graphene oxide (GO) sheets, bound with multiple cell surface receptors, are introduced and synthesized as novel anticancer agents. The results suggest that the binding connects GO sheets with neighboring lipid rafts, neutralizes endocytosis, and causes metabolic deprivation. As a result, tumor cell survival and proliferation are reduced. Live cell confocal microscopy imaging reveals that GO-PEGFA (folate-PEGylated GO) (PEG, polyethylene glycol) is internalized by tumor cells, while GO-PEGRGD (tripeptide Arg-Gly-Asp PEGylated GO) associates with the external cell membrane (not internalized). In vitro exposure of tumor cells to GO-PEGFA or GO-PEGRGD reduces the cell viability by 35%, compared to 50% reduction using methotrexate (100 μM). The combination of modified GO sheets with methotrexate or doxorubicin shows a greater toxicity (80% reduction in cell viability) than the individual agents. The proposed setup demonstrates a significant synergy in limiting tumor cell growth.
Insights
Modified graphene oxide (GO) sheets effectively inhibit cancer cell endocytosis and reduce tumor growth. This novel anticancer strategy shows significant synergy when combined with existing chemotherapy drugs, enhancing toxicity.
Area of Science:
- Biomedical Engineering
- Materials Science
- Oncology
Background:
- Endocytosis is a key mechanism for cancer cell survival and proliferation.
- Developing novel agents to inhibit endocytosis is a promising anticancer strategy.
- Graphene oxide (GO) possesses unique properties suitable for biomedical applications.
Purpose of the Study:
- To synthesize and evaluate modified graphene oxide (GO) sheets as novel anticancer agents.
- To investigate the mechanism of GO-mediated inhibition of cancer cell endocytosis.
- To assess the synergistic effects of modified GO with chemotherapy drugs.
Main Methods:
- Synthesis of folate-PEGylated GO (GO-PEGFA) and Arg-Gly-Asp-PEGylated GO (GO-PEGRGD).
- Live cell confocal microscopy to track GO internalization and cell membrane association.
- In vitro cell viability assays to determine cytotoxicity of GO agents and drug combinations.
Main Results:
- GO-PEGFA was internalized by tumor cells, while GO-PEGRGD associated with the cell membrane.
- GO-PEGFA and GO-PEGRGD reduced tumor cell viability by 35% compared to methotrexate (50% reduction).
- Combination therapy with modified GO and methotrexate or doxorubicin achieved an 80% reduction in cell viability, demonstrating significant synergy.
Conclusions:
- Modified GO sheets effectively inhibit cancer cell endocytosis and reduce tumor growth.
- The synergistic effect of GO combined with chemotherapy drugs offers a potent strategy for cancer treatment.
- This approach presents a novel and effective method for limiting tumor cell proliferation.
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