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Title: Theranostic unimolecular micelles of highly fluorescent conjugated polymer bottlebrushes for far red/near infrared bioimaging and efficient anticancer drug delivery
Authors: Yang, Cangjie
Huang, Shuo
Wang, Xiaochen
Wang, Mingfeng
Keywords: Conjugated polymers
Issue Date: 2016
Source: Yang, C., Huang, S., Wang, X., & Wang, M. (2016). Theranostic unimolecular micelles of highly fluorescent conjugated polymer bottlebrushes for far red/near infrared bioimaging and efficient anticancer drug delivery. Polymer Chemistry, 7(48), 7455-7468.
Series/Report no.: Polymer Chemistry
Abstract: We report the molecular design, synthesis and characterization of multifunctional unimolecular micelles formed by amphiphilic bottlebrush-like grafted block copolymers with theranostic functions of bright far red/near infrared (FR/NIR) fluorescence and anticancer drug delivery. Specifically, conjugated polymer poly(fluorene-alt-(4,7-bis(hexylthien)-2,1,3-benzothiadiazole)) (PFTB) was utilized as a fluorescent backbone and a macroinitiator for grafting with polycaprolactone (PCL) and poly[oligo(ethylene glycol) methyl ether methacrylate] (POEGMA) blocks via ring opening polymerization (ROP) and atom transfer radical polymerization (ATRP) successively, resulting in highly fluorescent polymer bottlebrushes, PFTB-g-(PCL-b-POEGMA). The amphiphilic and branched nature of these grafted block copolymers enabled the formation of unimolecular micelles (UMs) that were well dispersible in aqueous media. A series of PFTB-g-(PCL-b-POEGMA) polymers with the same conjugated backbone but different lengths of PCL and POEGMA side chains form UMs with different sizes and morphologies. A morphological transition of UMs from a spherical to a flower-like structure was observed with the increase of the POEGMA chain length. Compared to polymer PFTB-g-POEGMA, the introduction of hydrophobic and biodegradable PCL segments improved the fluorescence quantum yield from 0.16 to 0.25, accompanied by an obvious enhancement of the photostability of the UMs. These optical properties and the good biocompatibility of these UMs make them attractive as bioimaging probes for the visualization of biological systems. Moreover, the hydrophobic PCL domains in these fluorescent UMs provide a reservoir for loading hydrophobic anticancer drugs such as doxorubicin (DOX). The effect of PCL and POEGMA chain lengths on the drug loading and release was studied. These DOX-loaded UMs could be taken up well by HeLa and L929 cells and showed selectively higher cytotoxicity against HeLa cells than L929 cells, thereby representing a promising candidate for cancer theranostics.
ISSN: 1759-9954
DOI: 10.1039/C6PY01838F
Schools: School of Chemical and Biomedical Engineering 
Rights: © 2016 The Royal Society of Chemistry. This is the author created version of a work that has been peer reviewed and accepted for publication by Polymer Chemistry, The Royal Society of Chemistry. It incorporates referee’s comments but changes resulting from the publishing process, such as copyediting, structural formatting, may not be reflected in this document. The published version is available at: [].
Fulltext Permission: open
Fulltext Availability: With Fulltext
Appears in Collections:SCBE Journal Articles

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