Somatostatin Receptor-Mediated Tumor-Targeting Nanocarriers Based on Octreotide-PEG Conjugated Nanographene Oxide for Combined Chemo and Photothermal Therapy

• Published in: Small (Weinheim an der Bergstrasse, Germany) Vol. 12; no. 26; pp. 3578 - 3590
• Main Authors: Zhang, Xuyuan, Yang, Chongyin, Zhou, Jianping, Huo, Meirong
• Format: Journal Article
• Language: English
• Published: Germany Blackwell Publishing Ltd 01-07-2016; Wiley Subscription Services, Inc
• Subjects: Animals; Antibiotics, Antineoplastic - administration & dosage; Antibiotics, Antineoplastic - chemistry; Antibiotics, Antineoplastic - therapeutic use; Biocompatibility; Breast Neoplasms - drug therapy; Breast Neoplasms - metabolism; Cancer; cancer therapy; Cell Survival; Cellular; Doxorubicin - administration & dosage; Doxorubicin - chemistry; Doxorubicin - therapeutic use; Drug Carriers; Drug delivery systems; Drugs; Dynamic Light Scattering; Female; graphene oxide; Graphite - chemistry; Humans; MCF-7 Cells; Mice; Mice, Nude; Microscopy, Electron, Transmission; Nanostructure; Nanotechnology; octreotide; Octreotide - chemistry; Oxides; photothermal therapy; Polyethylene Glycols - chemistry; Receptors, Somatostatin - metabolism; somatostatin receptors; Therapy; Toxicity; tumor targeting; Xenograft Model Antitumor Assays; cancer therapy; graphene oxide; tumor targeting; octreotide; photothermal therapy; somatostatin receptors
• ISSN: 1613-6810; 1613-6829
• DOI: 10.1002/smll.201600618

Nano‐sized in vivo active targeting drug delivery systems have been developed to a high anti‐tumor efficacy strategy against certain cancer‐cells‐specific. Graphene based nanocarriers with unique physical and chemical properties have shown significant potentials in this aspect. Here, octreotide (OCT), an efficient biotarget molecule, is conjugated to PEGylated nanographene oxide (NGO) drug carriers for the first time. The obtained NGO‐PEG‐OCT complex shows low toxicity and excellent stability in vivo and is able to achieve somatostatin receptor‐mediated tumor‐specific targeting delivery. Owing to the high loading efficiency and accurate targeting delivery of anti‐cancer drug doxorubicin (DOX), our DOX loaded NGO‐PEG‐OCT complex offers a remarkably improved cancer‐cell‐specific cellular uptake, chemo‐cytotoxicity, and decreased systemic toxicity compared to free DOX or NGO‐PEG. More importantly, due to its strong near‐infrared absorption, the NGO‐PEG‐OCT complex further enhances efficient photothermal ablation of tumors, delivering combined chemo and photothermal therapeutic effect against cancer cells.
Efficient biotarget molecule octreotide conjugated nanographene oxide delivers somatostatin receptor‐mediated tumor‐specific targeting effect as tumor therapy agent. This active targeting offers a remarkably improved cancer‐cell‐specific cellular uptake, chemo‐cytotoxicity, and decreased systemic toxicity, which also enables combined chemo and photothermal therapeutic effect against cancer cells.