Volume 53, Issue 48 pp. 13126-13130
Communication

Cationic Vesicles Based on Amphiphilic Pillar[5]arene Capped with Ferrocenium: A Redox-Responsive System for Drug/siRNA Co-Delivery

Yincheng Chang

Yincheng Chang

College of Science, Northwest A&F University, Yangling, Shaanxi 712100 (P.R. China)

These authors contributed equally.

Search for more papers by this author
Kui Yang

Kui Yang

College of Science, Northwest A&F University, Yangling, Shaanxi 712100 (P.R. China)

These authors contributed equally.

Search for more papers by this author
Peng Wei

Peng Wei

College of Science, Northwest A&F University, Yangling, Shaanxi 712100 (P.R. China)

Search for more papers by this author
Sisi Huang

Sisi Huang

College of Science, Northwest A&F University, Yangling, Shaanxi 712100 (P.R. China)

Search for more papers by this author
Prof. Dr. Yuxin Pei

Corresponding Author

Prof. Dr. Yuxin Pei

College of Science, Northwest A&F University, Yangling, Shaanxi 712100 (P.R. China)

College of Science, Northwest A&F University, Yangling, Shaanxi 712100 (P.R. China)Search for more papers by this author
Wei Zhao

Wei Zhao

College of Science, Northwest A&F University, Yangling, Shaanxi 712100 (P.R. China)

Search for more papers by this author
Prof. Dr. Zhichao Pei

Corresponding Author

Prof. Dr. Zhichao Pei

College of Science, Northwest A&F University, Yangling, Shaanxi 712100 (P.R. China)

College of Science, Northwest A&F University, Yangling, Shaanxi 712100 (P.R. China)Search for more papers by this author
First published: 29 September 2014
Citations: 332

This research work was supported by the National Natural Science Foundation of China (NSFC 21174113 and NSFC 31270861). We thank Yihan Pei (Clare College, Cambridge) for language help.

Graphical Abstract

Simultaneous delivery of an anticancer drug and siRNA was achieved with cationic vesicles self-assembled from a novel ferrocenium-capped amphiphilic pillar[5]arene. These systems exhibit low cytotoxicity to healthy cells and are redox-responsive in the presence of a reductant/oxidant.

Abstract

A novel ferrocenium capped amphiphilic pillar[5]arene (FCAP) was synthesized and self-assembled to cationic vesicles in aqueous solution. The cationic vesicles, displaying low cytotoxicity and significant redox-responsive behavior due to the redox equilibrium between ferrocenium cations and ferrocenyl groups, allow building an ideal glutathione (GSH)-responsive drug/siRNA co-delivery system for rapid drug release and gene transfection in cancer cells in which higher GSH concentration exists. This is the first report of redox-responsive vesicles assembled from pillararenes for drug/siRNA co-delivery; besides enhancing the bioavailability of drugs for cancer cells and reducing the adverse side effects for normal cells, these systems can also overcome the drug resistance of cancer cells. This work presents a good example of rational design for an effective stimuli-responsive drug/siRNA co-delivery system.

The full text of this article hosted at iucr.org is unavailable due to technical difficulties.