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α-Conotoxin ImI-modified polymeric micelles as potential nanocarriers for targeted docetaxel delivery to α7-nAChR overexpressed non-small cell lung cancer

Drug delivery, 2018, Vol.25 (1), p.493-503 [Peer Reviewed Journal]

2018 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. 2018 ;2018 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. This work is licensed under the Creative Commons Attribution License http://creativecommons.org/licenses/by/4.0/ (the “License”). Notwithstanding the ProQuest Terms and Conditions, you may use this content in accordance with the terms of the License. ;2018 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. 2018 The Author(s) ;ISSN: 1071-7544 ;EISSN: 1521-0464 ;DOI: 10.1080/10717544.2018.1436097 ;PMID: 29426250

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  • Title:
    α-Conotoxin ImI-modified polymeric micelles as potential nanocarriers for targeted docetaxel delivery to α7-nAChR overexpressed non-small cell lung cancer
  • Author: Mei, Dong ; Zhao, Libo ; Chen, Binlong ; Zhang, Xiaoyan ; Wang, Xiaoling ; Yu, Zhiying ; Ni, Xin ; Zhang, Qiang
  • Subjects: Breast cancer ; Cancer therapies ; Cell growth ; Cytotoxicity ; Drugs ; Epidemiology ; Hospitals ; Kinases ; Laboratories ; Ligands ; Lung cancer ; Medical research ; Nanoparticles ; Nicotine ; non-small cell lung cancer (NSCLC) ; PEG-DSPE micelles ; Peptides ; Pharmaceutical sciences ; Surveillance ; targeted delivery ; α-Conotoxin ImI ; α7-nAChR
  • Is Part Of: Drug delivery, 2018, Vol.25 (1), p.493-503
  • Description: A micelle system modified with α-Conotoxin ImI (ImI), a potently antagonist for alpha7 nicotinic acetylcholine receptor (α7-nAChR) previously utilized for targeting breast cancer, was constructed. Its targeting efficiency and cytotoxicity against non-small cell lung cancer (NSCLC) highly expressing α7-nAChR was investigated. A549, a non-small cell lung cancer cell line, was selected as the cell model. The cellular uptake study showed that the optimal modification ratio of ImI on micelle surface was 5% and ImI-modification increased intracellular delivery efficiency to A549 cells via receptor-mediated endocytosis. Intracellular Ca 2+ transient assay demonstrated that ImI modification led to enhanced molecular interaction between nanocarriers and A549 cells. The in vivo near-infrared fluorescence imaging further revealed that ImI-modified micelles could facilitate the drug accumulation in tumor sites compared with non-modified micelles via α7-nAChR mediation. Moreover, docetaxel (DTX) was loaded in ImI-modified nanomedicines to evaluate its in vitro cytotoxicity. As a result, DTX-loaded ImI-PMs exhibited greater anti-proliferation effect on A549 cells compared with non-modified micelles. Generally, our study proved that ImI-modified micelles had targeting ability to NSCLC in addition to breast cancer and it may provide a promising strategy to deliver drugs to NSCLC overexpressing α7-nAChR.
  • Publisher: England: Taylor & Francis
  • Language: English
  • Identifier: ISSN: 1071-7544
    EISSN: 1521-0464
    DOI: 10.1080/10717544.2018.1436097
    PMID: 29426250
  • Source: Open Access: PubMed Central
    Taylor & Francis Open Access
    AUTh Library subscriptions: ProQuest Central
    DOAJ Directory of Open Access Journals
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