Targeted doxorubicin delivery to hepatocarcinoma cells by lactobionic acid-modified laponite nanodisksElectronic supplementary information (ESI) available: Additional experimental results. See DOI: 10.1039/c4nj01916d

• Main Authors: Chen, Guangxiang, Li, Du, Li, Jingchao, Cao, Xueyan, Wang, Jianhua, Shi, Xiangyang, Guo, Rui
• Format: Article
• Language: English
• ISSN: 1144-0546; 1369-9261
• DOI: 10.1039/c4nj01916d

In this study, we covalently conjugated polyethylene glycol-linked lactobionic acid (PEG-LA) onto the surface of laponite (LAP) nanodisks for the targeted delivery of doxorubicin (DOX) to liver cancer cells. LAP nanodisks were firstly modified with 3-aminopropyldimethylethoxysilane to introduce amino groups on the surface, and then PEG-LA were successfully conjugated to form targeted LM-PEG-LA nanodisks via EDC chemistry. Finally, the anticancer drug DOX was encapsulated into the synthesized nanocarriers with an exceptionally high loading efficiency of 91.5%. In vitro release studies showed that LM-PEG-LA/DOX could release drugs in a sustained manner with a higher speed under acidic conditions than that under physiological ones. MTT assay results proved that LM-PEG-LA/DOX displayed a significant higher therapeutic efficacy in inhibiting the growth of hepatocellular carcinoma cells (HepG2 cells) than untargeted ones at the same DOX concentration. The targeting specificity of LM-PEG-LA/DOX was further demonstrated by flow cytometric analysis and confocal laser scanning microscopy. The developed LA-modified LAP nanodisks could serve as a targeted carrier for efficient loading and specific delivery of different anticancer drugs to liver cancer cells. Lactobionic acid-modified laponite can deliver doxorubicin specifically to hepatocarcinoma cells overexpressing the asialoglycoprotein receptor and display a significantly enhanced therapeutic efficacy.