Magnetic graphene oxide as a carrier for targeted delivery of chemotherapy drugs in cancer therapy

• Published in: Journal of magnetism and magnetic materials Vol. 427; pp. 34 - 40
• Main Authors: Huang, Ya-Shu, Lu, Yu-Jen, Chen, Jyh-Ping
• Format: Journal Article
• Language: English
• Published: Amsterdam Elsevier B.V 01.04.2017; Elsevier BV
• Subjects: Cancer; Chemical compounds; Chemical precipitation; Chemotherapy; Chitosan; Circulation; Controlled release; Cytotoxicity; Doxorubicin; Drug delivery; Drug delivery systems; Drugs; Graphene; In vitro methods and tests; Irinotecan; Iron oxides; Magnesium oxide; Magnetic graphene oxide; Magnetic nanoparticles; MPEG encoders; Platelets (materials); Polyethylene glycol; Polyethylenes; Toxicity; Video compression; Irinotecan; Drug delivery; Magnetic graphene oxide; Doxorubicin; Magnetic nanoparticles
• ISSN: 0304-8853; 1873-4766
• DOI: 10.1016/j.jmmm.2016.10.042

A magnetic targeted functionalized graphene oxide (GO) complex is constituted as a nanocarrier for targeted delivery and pH-responsive controlled release of chemotherapy drugs to cancer cells. Magnetic graphene oxide (mGO) was prepared by chemical co-precipitation of Fe3O4 magnetic nanoparticles on GO nano-platelets. The mGO was successively modified by chitosan and mPEG-NHS through covalent bindings to synthesize mGOC-PEG. The polyethylene glycol (PEG) moiety is expected to prolong the circulation time of mGO by reducing the reticuloendothelial system clearance. Irinotecan (CPT-11) or doxorubicin (DOX) was loaded to mGOC-PEG through π-π stacking interactions for magnetic targeted delivery of the cancer chemotherapy drug. The best values of loading efficiency and loading content of CPT-11 were 54% and 2.7% respectively; whereas for DOX, they were 65% and 393% The pH-dependent drug release profile was further experimented at different pHs, in which ~60% of DOX was released at pH 5.4 and ~10% was released at pH 7.4. In contrast, ~90% CPT-11 was released at pH 5.4 and ~70% at pH 7.4. Based on the drug loading and release characteristics, mGOC-PEG/DOX was further chosen for in vitro cytotoxicity tests against U87 human glioblastoma cell line. The IC50 value of mGOC-PEG/DOX was found to be similar to that of free DOX but was reduced dramatically when subject to magnetic targeting. It is concluded that with the high drug loading and pH-dependent drug release properties, mGOC-PEG will be a promising drug carrier for targeted delivery of chemotherapy drugs in cancer therapy. •mGO was prepared by chemical co-precipitation of Fe3O4 MNP on GO nano-platelets.•mGO was further modified by chitosan and mPEG-NHS to synthesize mGOC-PEG.•mGOC-PEG showed higher drug loading of doxorubicin (DOX) than irinotecan.•mGOC-PEG showed pH-responsive controlled release of chemotherapy drugs.•Magnetic targeting enhanced cytotoxicity of mGOC-PEG/DOX toward U87 cancer cells.