Nanotech 2010

AS1411 aptamer-conjugated polymeric micelle for targetable cancer therapy

P.S. Lai, C.L. Pai, C.Y. Hsu
National Chung Hsing University, TW

Keywords: aptamer, nucleolin, micelle, cancer targeting


Targetable drug delivery system is a promising tool for cancer treatments. Herein we report a novel strategy of using G-quadruplex AS1411 aptamer-conjugated polyethylene-polylactide formed polymeric micelles (apt-PEG-PLA-PM) as a drug carrier to target cancer cells for chemotherapy. G-quadruplex AS1411 aptamer is known to target to nucleolin over-expressed in cancer cells, in this study, the effect of AS1411 aptamer-conjugated polymeric micelle for paclitaxel delivery into cancer cells by nucleolin-mediated internalization was investigated. Our results showed that the apt-PEG-PLA-PM exhibited higher intracellular paclitaxel accumulation and cytotoxicity in MCF-7 breast cancer cells than in M10 normal epithelium cells. The intracellular of apt-PEG-PLA-PM co-localized with anti-nucleolin antibody and the microtubules bundled in MCF-7 cells were observed after paclitaxel-loaded apt-PEG-PLA-PM co-incubation by confocal microscopy using immunofluorescence staining. It indicated that the apt-PEG-PLA-PM was mainly internalized into cells via the specific interaction of AS1411 aptamer with nucleolin on the cell surface and this nucleolin-targetable polymeric micelle can be a potential drug carrier for cancer therapy.
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