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Multivalent Aptamer–RNA Conjugates for Simple and Efficient Delivery of Doxorubicin/siRNA into Multidrug‐Resistant Cells
Author(s) -
Jeong Hyosook,
Lee Soo Hyeon,
Hwang Yeonju,
Yoo Hyundong,
Jung Heesun,
Kim Sun Hwa,
Mok Hyejung
Publication year - 2017
Publication title -
macromolecular bioscience
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.924
H-Index - 105
eISSN - 1616-5195
pISSN - 1616-5187
DOI - 10.1002/mabi.201600343
Subject(s) - aptamer , doxorubicin , nucleic acid , chemistry , multiple drug resistance , small interfering rna , transfection , intracellular , cancer cell , drug delivery , pharmacology , biochemistry , microbiology and biotechnology , cancer , biology , antibiotics , chemotherapy , genetics , organic chemistry , gene
Multivalent aptamer–siRNA conjugates containing multiple mucin‐1 aptamers and BCL2 ‐specific siRNA are synthesized, and doxorubicin, an anthracycline anticancer drug, is loaded into these conjugates through intercalation with nucleic acids. These doxorubicin‐incorporated multivalent aptamer–siRNA conjugates are transfected to mucin‐1 overexpressing MCF‐7 breast cancer cells and their multidrug‐resistant cell lines. Doxorubicin‐incorporated multivalent aptamer–siRNA conjugates exert promising anticancer effects, such as activation of caspase‐3/7 and decrease of cell viability, on multidrug‐resistant cancer cells because of their high intracellular uptake efficiency. Thus, this delivery system is an efficient tool for combination oncotherapy with chemotherapeutics and nucleic acid drugs to overcome multidrug resistance.