Alemayehu, Y.A.Y.A.AlemayehuFan, W.-L.W.-L.FanIlhami, F.B.F.B.IlhamiChiu, C.-W.C.-W.ChiuLee, D.-J.D.-J.LeeCheng, C.-C.C.-C.ChengDUU-JONG LEE2021-02-042021-02-042020Alemayehu, Y.A.;Fan, W.-L.;Ilhami, F.B.;Chiu, C.-W.;Lee, D.-J.;Cheng, C.-C.https://www.scopus.com/inward/record.url?eid=2-s2.0-85087368920&partnerID=40&md5=1d003921414e2fd022c10819f0cf3729https://scholars.lib.ntu.edu.tw/handle/123456789/547624The development of stimuli-responsive supramolecular micelles with high drug-loading contents that specifically induce significant levels of apoptosis in cancer cells remains challenging. Herein, we report photosensitive uracil-functionalized supramolecular micelles that spontaneously form via self-assembly in aqueous solution, exhibit sensitive photo-responsive behavior, and effectively encapsulate anticancer drugs at high drug-loading contents. Cellular uptake analysis and double-staining flow cytometric assays confirmed the presence of photo-dimerized uracil groups within the irradiated micelles remarkably enhanced endocytic uptake of the micelles by cancer cells and subsequently led to higher levels of apoptotic cell death, and thus improved the therapeutic effect in vitro. Thus, photo-dimerized uracil-functionalized supramolecular micelles may potentially represent an intelligent nanovehicle to improve the safety, efficacy, and applicability of cancer chemotherapy, and could also enable the development of nucleobase-based supramolecular micelles for multifunctional biomaterials and novel biomedical applications. ? 2020 by the authors. Licensee MDPI, Basel, Switzerland.Chemotherapy; Drug delivery; Photodimerization; Supramolecular micelle; Uracil[SDGs]SDG3antineoplastic agent; biomaterial; doxorubicin; nanocarrier; nucleic acid base; uracil; antineoplastic agent; drug carrier; apoptosis; Article; biocompatibility; cancer cell; cancer chemotherapy; cell death; cell viability; confocal laser scanning microscopy; controlled study; cytotoxicity; dimerization; drug delivery system; drug efficacy; drug release; drug safety; flow cytometry; fluorescence imaging; HeLa cell line; human; human cell; IC50; micelle; mitochondrial membrane potential; MTT assay; particle size; photosensitivity; physical chemistry; static electricity; supramolecular chemistry; therapy effect; transmission electron microscopy; tumor growth; tumor microenvironment; ultraviolet irradiation; ultraviolet spectrophotometry; zeta potential; chemistry; endocytosis; Antineoplastic Agents; Apoptosis; Dimerization; Drug Carriers; Endocytosis; Micelles; Uraciljournal article10.3390/ijms21134677326300692-s2.0-85087368920WOS:000550289600001