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

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 co...

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Published in	Small (Weinheim an der Bergstrasse, Germany) Vol. 6; no. 4; pp. 537 - 544
Main Authors	Zhang, Liming, Xia, Jingguang, Zhao, Qinghuan, Liu, Liwei, Zhang, Zhijun
Format	Journal Article
Language	English
Published	Weinheim WILEY-VCH Verlag 22.02.2010 WILEY‐VCH Verlag
Subjects	Antineoplastic Agents - pharmacology Antitumor agents Breast cancer Camptothecin Camptothecin - pharmacology cancer therapy Carbon - chemistry Cell Line, Tumor Cell Survival - drug effects Cytotoxicity Doxorubicin Doxorubicin - pharmacology Drug Carriers - chemistry drug delivery Drug Delivery Systems - methods Folic acid Folic Acid - chemistry graphene oxide Humans Hydrophobicity Microscopy, Atomic Force nanomaterials oxides Rhodamines - metabolism Solutions Spectrometry, Fluorescence Spectrophotometry, Ultraviolet Spectroscopy, Fourier Transform Infrared Stacking sulfonic acid
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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 π–π 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. Nanoscale graphene oxide (NGO) with good biocompatibility and physiological stability is synthesized by functionalization with sulfonic acid groups and conjugation with folic acid. In the delivery of multiple drugs, cellular‐uptake experiments show the targeted delivery of the anticancer drugs doxorubicin and camptothecin into cells (see picture) by the NGO via receptor‐mediated endocytosis.
AbstractList	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 π–π 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. 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. 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 π–π 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. Nanoscale graphene oxide (NGO) with good biocompatibility and physiological stability is synthesized by functionalization with sulfonic acid groups and conjugation with folic acid. In the delivery of multiple drugs, cellular‐uptake experiments show the targeted delivery of the anticancer drugs doxorubicin and camptothecin into cells (see picture) by the NGO via receptor‐mediated endocytosis. 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.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.
Author	Zhang, Liming Zhao, Qinghuan Liu, Liwei Zhang, Zhijun Xia, Jingguang
Author_xml	– sequence: 1 givenname: Liming surname: Zhang fullname: Zhang, Liming organization: Suzhou Institute of Nano-tech and Nano-bionics Chinese Academy of Sciences 398 Ruoshui Road, Dushu Lake Higher Education Town Suzhou Industrial Park, Suzhou 215125 (P. R. China) – sequence: 2 givenname: Jingguang surname: Xia fullname: Xia, Jingguang organization: Suzhou Institute of Nano-tech and Nano-bionics Chinese Academy of Sciences 398 Ruoshui Road, Dushu Lake Higher Education Town Suzhou Industrial Park, Suzhou 215125 (P. R. China) – sequence: 3 givenname: Qinghuan surname: Zhao fullname: Zhao, Qinghuan organization: Suzhou Institute of Nano-tech and Nano-bionics Chinese Academy of Sciences 398 Ruoshui Road, Dushu Lake Higher Education Town Suzhou Industrial Park, Suzhou 215125 (P. R. China) – sequence: 4 givenname: Liwei surname: Liu fullname: Liu, Liwei organization: Suzhou Institute of Nano-tech and Nano-bionics Chinese Academy of Sciences 398 Ruoshui Road, Dushu Lake Higher Education Town Suzhou Industrial Park, Suzhou 215125 (P. R. China) – sequence: 5 givenname: Zhijun surname: Zhang fullname: Zhang, Zhijun email: zjzhang2007@sinano.ac.cn organization: Suzhou Institute of Nano-tech and Nano-bionics Chinese Academy of Sciences 398 Ruoshui Road, Dushu Lake Higher Education Town Suzhou Industrial Park, Suzhou 215125 (P. R. China)
BackLink	https://www.ncbi.nlm.nih.gov/pubmed/20033930$$D View this record in MEDLINE/PubMed
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Snippet	A simple synthetic route for the preparation of functional nanoscale graphene oxide (NGO), a novel nanocarrier for the loading and targeted delivery of...
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SubjectTerms	Antineoplastic Agents - pharmacology Antitumor agents Breast cancer Camptothecin Camptothecin - pharmacology cancer therapy Carbon - chemistry Cell Line, Tumor Cell Survival - drug effects Cytotoxicity Doxorubicin Doxorubicin - pharmacology Drug Carriers - chemistry drug delivery Drug Delivery Systems - methods Folic acid Folic Acid - chemistry graphene oxide Humans Hydrophobicity Microscopy, Atomic Force nanomaterials oxides Rhodamines - metabolism Solutions Spectrometry, Fluorescence Spectrophotometry, Ultraviolet Spectroscopy, Fourier Transform Infrared Stacking sulfonic acid
Title	Functional Graphene Oxide as a Nanocarrier for Controlled Loading and Targeted Delivery of Mixed Anticancer Drugs
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