title: Selective Delivery of an Anticancer Drug with Aptamer-Functionalized Liposomes to Breast Cancer Cellsin Vitroandin Vivo.
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 cellsin vitrohas been reported, their effectiveness has rarely been establishedin 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 and selectivity.
authors.affiliation: Department of Chemistry, University of Illinois at Urbana-Champaign, Urbana, Illinois 61801, USA. Tel: +1-217-333-2619 ; Beckman Institute for Advanced Science and Technology, University of Illinois at Urbana-Champaign, Urbana, Illinois 61801, USA. Tel: +1-217-244-5023.
authors.forename: Hang
authors.initials: H
authors.lastname: Xing
authors.forename: Li
authors.initials: L
authors.lastname: Tang
authors.forename: Xujuan
authors.initials: X
authors.lastname: Yang
authors.forename: Kevin
authors.initials: K
authors.lastname: Hwang
authors.forename: Wendan
authors.initials: W
authors.lastname: Wang
authors.forename: Qian
authors.initials: Q
authors.lastname: Yin
authors.forename: Ngo Yin
authors.initials: NY
authors.lastname: Wong
authors.forename: Lawrence W
authors.initials: LW
authors.lastname: Dobrucki
authors.forename: Norio
authors.initials: N
authors.lastname: Yasui
authors.forename: John A
authors.initials: JA
authors.lastname: Katzenellenbogen
authors.forename: William G
authors.initials: WG
authors.lastname: Helferich
authors.forename: Jianjun
authors.initials: J
authors.lastname: Cheng
authors.forename: Yi
authors.initials: Y
authors.lastname: Lu
keywords: DNA aptamer; breast cancer; cancer targeting; liposome; nucleolin; targeted drug delivery