title: Multi-functional self-fluorescent unimolecular micelles for tumor-targeted drug delivery and bioimaging.
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.
authors: Materials Science Program, University of Wisconsin-Madison, Madison, WI 53715, USA; Wisconsin Institutes for Discovery, University of Wisconsin-Madison, Madison, WI 53715, USA.
authors: Guojun
authors: G
authors: Chen
authors: Wisconsin Institutes for Discovery, University of Wisconsin-Madison, Madison, WI 53715, USA; Department of Biomedical Engineering, University of Wisconsin-Madison, Madison, WI 53715, USA.
authors: Liwei
authors: L
authors: Wang
authors: Department of Biomedical Engineering, University of Wisconsin-Madison, Madison, WI 53715, USA.
authors: Travis
authors: T
authors: Cordie
authors: Laboratory for Optical and Computational Instrumentation, University of Wisconsin-Madison, Madison, WI 53706, USA.
authors: Corinne
authors: C
authors: Vokoun
authors: Laboratory for Optical and Computational Instrumentation, University of Wisconsin-Madison, Madison, WI 53706, USA.
authors: Kevin W
authors: KW
authors: Eliceiri
authors: Materials Science Program, University of Wisconsin-Madison, Madison, WI 53715, USA; Wisconsin Institutes for Discovery, University of Wisconsin-Madison, Madison, WI 53715, USA; Department of Biomedical Engineering, University of Wisconsin-Madison, Madison, WI 53715, USA; University of Wisconsin Carbone Cancer Center, University of Wisconsin-Madison, Madison, WI 53792, USA. Electronic address: sgong@engr.wisc.edu.
authors: Shaoqin
authors: S
authors: Gong
mesh_terms: D045744:Cell Line, Tumor; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems; D006801:Humans; D057446:Hydrodynamics; D006863:Hydrogen-Ion Concentration; D039302:Integrin alphaVbeta3 / Q000737:chemistry; D009682:Magnetic Resonance Spectroscopy; D008823:Micelles; D008856:Microscopy, Fluorescence; D009389:Neovascularization, Pathologic; D009842:Oligopeptides / Q000737:chemistry; D010455:Peptides / Q000737:chemistry; D017785:Photons; D011092:Polyethylene Glycols / Q000737:chemistry*; D011108:Polymers / Q000737:chemistry; D017550:Spectroscopy, Fourier Transform Infrared
chemical_list: D004337:Drug Carriers; D039302:Integrin alphaVbeta3; D008823:Micelles; D009842:Oligopeptides; D010455:Peptides; D011108:Polymers; D011092:Polyethylene Glycols; C047981:arginyl-glycyl-aspartic acid
keywords: Bioimaging probe; Cancer theranostics; Drug delivery; Drug nanocarrier; Self-fluorescence; Unimolecular micelles