Development of a theranostic prodrug for colon cancer therapy by combining ligand-targeted delivery and enzyme-stimulated activation. (February 2018)

• Record Type: Journal Article
• Authors: Sharma, Amit; Kim, Eun-Joong; Shi, Hu; Lee, Jin Yong; Chung, Bong Geun; Kim, Jong Seung
• Is Part Of: Biomaterials. Volume 155(2018)
• Page Start: 145
• Page End: 151
• Publication Date: 2018-02
• Subjects: Targeted drug delivery -- Colon cancer -- Theranostic -- β-Galactosidase -- Doxorubicin; Biomedical materials -- Periodicals; Biocompatible Materials -- Periodicals; Biomatériaux -- Périodiques; 610.28
• DOI: 10.1016/j.biomaterials.2017.11.019
• Languages: English
• ISSNs: 0142-9612

Abstract

Abstract: The high incidence of colorectal cancer worldwide is currently a major health concern. Although conventional chemotherapy and surgery are effective to some extent, there is always a risk of relapse due to associated side effects, including post-surgical complications and non-discrimination between cancer and normal cells. In this study, we developed a small molecule-based theranostic system, Gal-Dox, which is preferentially taken up by colon cancer cells through receptor-mediated endocytosis. After cancer-specific activation, the active drugDox (doxorubicin) is released with a fluorescence turn-on response, allowing both drug localization and site of action to be monitored. The therapeutic potency ofGal-Dox was also evaluated, both in vivo and ex vivo, thus illustrating the potential ofGal-Dox as a colorectal cancer theranostic with great specificity. Graphical abstract: Herein, we developed a small molecule-based theranostic system, Gal-Dox, which is preferentially taken up by colon cancer cells through receptor-mediated endocytosis. After cancer-specific activation, the active drugDox (doxorubicin) is released with a fluorescence turn-on response, allowing both drug localization and site of action to be monitored. The therapeutic potency ofGal-Dox was also monitored, both in vivo and ex vivo, thus illustrating the potential ofGal-Dox as a colorectal cancer theranostic with great specificity.