Multi-functional self-fluorescent unimolecular micelles for tumor-targeted drug delivery and bioimaging |
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| Institution: | 1. Materials Science Program, University of Wisconsin–Madison, Madison, WI 53715, USA;2. Wisconsin Institutes for Discovery, University of Wisconsin–Madison, Madison, WI 53715, USA;3. Department of Biomedical Engineering, University of Wisconsin–Madison, Madison, WI 53715, USA;4. Laboratory for Optical and Computational Instrumentation, University of Wisconsin–Madison, Madison, WI 53706, USA;5. University of Wisconsin Carbone Cancer Center, University of Wisconsin–Madison, Madison, WI 53792, USA;1. Laboratoire de Chimie des Matériaux, Université d’Oran 1, BP 1524 El-Mnaouer, 31000 Oran, Algeria;2. Nanoqam, Department of Chemistry, University of Quebec at Montreal, H3C-3P8 Canada;1. College of Materials Science and Engineering, China Jiliang University, Hangzhou 310018, China;2. College of Optical Science and Engineering, State Key Laboratory of Modern Optical Instrumentation, Zhejiang University, Hangzhou 310027, China;1. Department of Applied Science and Technology, A.C. Tech., Anna University, Chennai, India;2. Department of Biotechnology, PSG College of Technology, Coimbatore, India;1. Otolaryngological Department, Xintai People Hospital, Xintai, 271200, Shandong, China;2. Otolaryngological Department, The Second People''s Hospital of Liaocheng, Linqing, 252600, Shandong, China |
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| Abstract: | A novel type of self-fluorescent unimolecular micelle nanoparticle (NP) formed by multi-arm star amphiphilic block copolymer, Boltron® H40 (H40, a 4th generation hyperbranched polymer)-biodegradable photo-luminescent polymer (BPLP)-poly(ethylene glycol) (PEG) conjugated with cRGD peptide (i.e., H40-BPLP-PEG-cRGD) was designed, synthesized, and characterized. The hydrophobic BPLP segment was self-fluorescent, thereby making the unimolecular micelle NP self-fluorescent. cRGD peptides, which can effectively target αvβ3 integrin-expressing tumor neovasculature and tumor cells, were selectively conjugated onto the surface of the micelles to offer active tumor-targeting ability. This unique self-fluorescent unimolecular micelle exhibited excellent photostability and low cytotoxicity, making it an attractive bioimaging probe for NP tracking for a variety of microscopy techniques including fluorescent microscopy, confocal laser scanning microscopy (CLSM), and two-photon microscopy. Moreover, this self-fluorescent unimolecular micelle NP also demonstrated excellent stability in aqueous solutions due to its covalent nature, high drug loading level, pH-controlled drug release, and passive and active tumor-targeting abilities, thereby making it a promising nanoplatform for targeted cancer theranostics. |
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| Keywords: | Self-fluorescence Unimolecular micelles Drug nanocarrier Drug delivery Bioimaging probe Cancer theranostics |
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