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Adenine‐Functionalized Supramolecular Micelles for Selective Cancer Chemotherapy
Author(s) -
Ilhami Fasih Bintang,
Alemayehu Yihalem Abebe,
Fan WenLu,
Tsai HsiehChih,
Kao ChenYu,
Cheng ChihChia
Publication year - 2020
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.202000233
Subject(s) - micelle , chemistry , internalization , cancer cell , cytotoxicity , biophysics , drug delivery , drug , supramolecular chemistry , apoptosis , combinatorial chemistry , in vitro , cancer , biochemistry , aqueous solution , cell , pharmacology , organic chemistry , biology , molecule , genetics
Functional supramolecular micelles containing self‐complementary multiple hydrogen bonding adenine groups (A‐PPG) can spontaneously self‐assemble into stable nanosized micelles in aqueous solution. These micelles can be used to selectively deliver anticancer drugs to cancer cells and effectively promote tumor cell death via apoptosis, without harming normal cells. The drug‐loaded micelles exhibit tunable drug‐loading capacity and rapid pH‐triggered drug release under acidic conditions, as well as a high drug‐entrapment stability in serum‐rich media due to the reversible hydrogen‐bonded adenine–adenine interactions within the micellar interior; these properties are critical to achieving effective chemotherapeutic drug delivery and controlled drug release. In vitro assays show that the drug‐loaded micelles exert significant cytotoxic effects on cancer cells, with minimal effects on normal cells under physiological conditions. Cytotoxicity assays using A‐PPG micelles loaded with different anticancer drugs confirm these effects. Importantly, cellular internalization and flow cytometric analyses demonstrate that the adenine moieties within A‐PPG micelles significantly increase selective endocytic uptake of the supramolecular micelles by cancer cells, which in turn induce apoptotic cell death and substantially enhance the response to chemotherapy. Thus, A‐PPG micelles can improve the safety and efficacy of cancer chemotherapy.