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Herein, treatment of multidrug\u2010resistant tumors using red\u2010light\u2010responsive metallopolymer nanocarriers that are conjugated with the anticancer drug chlorambucil (CHL) and encapsulated with the anticancer drug doxorubicin (DOX) is reported. An amphiphilic metallopolymer PolyRuCHL that contains a poly(ethylene glycol) (PEG) block and a red\u2010light\u2010responsive ruthenium (Ru)\u2010containing block is synthesized. Chlorambucil is covalently conjugated to the Ru moieties of PolyRuCHL. Encapsulation of DOX into PolyRuCHL in an aqueous solution results in DOX@PolyRuCHL micelles. The DOX@PolyRuCHL micelles are efficiently taken up by the multidrug\u2010resistant breast cancer cell line MCF\u20107R and which carries DOX into the cells. Free DOX, without the nanocarriers, is not taken up by MCF\u20107R or pumped out of MCF\u20107R via P\u2010glycoproteins. Red light irradiation of DOX@PolyRuCHL micelles triggers the release of chlorambucil\u2010conjugated Ru moieties and DOX. Both act synergistically to inhibit the growth of multidrug\u2010resistant cancer cells. Furthermore, the inhibition of the growth of multidrug\u2010resistant tumors in a mouse model using DOX@PolyRuCHL micelles is demonstrated. The design of red\u2010light\u2010responsive metallopolymer nanocarriers with both conjugated and encapsulated drugs opens up an avenue for photoactivated chemotherapy against multidrug\u2010resistant tumors.<\/jats:p>","DOI":"10.1002\/smll.202201672","type":"journal-article","created":{"date-parts":[[2022,6,3]],"date-time":"2022-06-03T21:15:20Z","timestamp":1654290920000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":23,"title":["Red\u2010Light\u2010Responsive Metallopolymer Nanocarriers with Conjugated and Encapsulated Drugs for Phototherapy Against Multidrug\u2010Resistant Tumors"],"prefix":"10.1002","volume":"18","author":[{"given":"Mingjia","family":"Chen","sequence":"first","affiliation":[{"name":"Max Planck Institute for Polymer Research  Ackermannweg 10 55128 Mainz Germany"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Ningqiang","family":"Gong","sequence":"additional","affiliation":[{"name":"CAS 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