期刊
CHEMMEDCHEM
卷 13, 期 24, 页码 2644-2652出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.201800575
关键词
anticancer; fucose; gemcitabine; graphene oxide nanosheets; targeted delivery
资金
- Central University of Gujarat, Gandhinagar
- Department of Science and Technology, New Delhi
- University Grant Commission
Targeted drug delivery has shown promise in improving the therapeutic efficacy of anticancer drugs. Gemcitabine hydrochloride (GEM) is a broad-range chemotherapeutic agent for the treatment of various cancers. However, systemic use of free GEM is restricted because of its poor physicochemical properties and nonspecific drug delivery, resulting in dose-dependent adverse effects. In this study, a fucose-conjugated graphene oxide (GO)-based smart targeted nanocarrier system was designed to provide high loading, sustained release, and targeted high concentrations of GEM to cancer cells. Fucose-conjugated GO nanosheets (FGONS) and GEM-loaded fucose-conjugated GO nanosheets (GEM-FGONS) were prepared and characterized by various techniques. About 36.2 % of GEM was loaded to the FGONS, which showed a pH-dependent release over a period of 48 h. A colloidal suspension of GEM-FGONS was found to be physiochemically stable for up to 96 h. In cytotoxicity studies, GEM-FGONS demonstrated time- and dose-dependent high toxicities on fucose-receptor-overexpressing MDA-MB-231 human breast cancer cells and A549 human lung cancer cells. Moreover, targeted formulations were more efficacious than non-targeted or free GEM. Overall, bioconjugation of fucose helps in the stabilizing and targeting of graphene oxide nanosheets.
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