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Issue 39, 2013
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Selective delivery of an anticancer drug with aptamer-functionalized liposomes to breast cancer cells in vitro and in vivo

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Abstract

Selective targeting of cancer cells is a critical step in cancer diagnosis and therapy. To address this need, DNA aptamers have attracted significant attention as possible targeting ligands. However, while their use in targeting cancer cells in vitro has been reported, their effectiveness has rarely been established in vivo. Here we report the development of a liposomal drug delivery system for targeted anticancer chemotherapy. Liposomes were prepared containing doxorubicin as a payload, and functionalized with AS1411, a DNA aptamer with strong binding affinity for nucleolin. AS1411 aptamer-functionalized liposomes increased cellular internalization and cytotoxicity to MCF-7 breast cancer cells as compared to non-targeting liposomes. Furthermore, targeted liposomal doxorubicin improved antitumor efficacy against xenograft MCF-7 breast tumors in athymic nude mice, attributable to their enhanced tumor tissue penetration. This study suggests that AS1411 aptamer-functionalized liposomes can recognize nucleolin overexpressed on MCF-7 cell surface, and therefore enable drug delivery with high specificity.

Graphical abstract: Selective delivery of an anticancer drug with aptamer-functionalized liposomes to breast cancer cells in vitro and in vivo

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Publication details

The article was received on 24 Mar 2013, accepted on 11 Jul 2013 and first published on 12 Jul 2013


Article type: Paper
DOI: 10.1039/C3TB20412J
Citation: J. Mater. Chem. B, 2013,1, 5288-5297
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    Selective delivery of an anticancer drug with aptamer-functionalized liposomes to breast cancer cells in vitro and in vivo

    H. Xing, L. Tang, X. Yang, K. Hwang, W. Wang, Q. Yin, N. Y. Wong, L. W. Dobrucki, N. Yasui, J. A. Katzenellenbogen, W. G. Helferich, J. Cheng and Y. Lu, J. Mater. Chem. B, 2013, 1, 5288
    DOI: 10.1039/C3TB20412J

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