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An Amphiphilic PEGylated Peptide Dendron-Gemcitabine Prodrug-Based Nanoagent for Cancer Therapy.

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机构： [1]Laboratory of Stem Cell Biology, and Huaxi MR Research Center (HMRRC), Department of Radiology, National Clinical Research Center for Geriatrics, Functional and Molecular Imaging Key Laboratory of Sichuan Province, West China Hospital, Sichuan University Chengdu, Chengdu, 610041, P. R. China. [2]School of Pharmacy, Fujian Medical University, Fuzhou, 350122, China. [3]Department of Radiology, Southwest Hospital, Third Military Medical University (Army Medical University), Chongqing, 400038, China. [4]Amgen Bioprocessing Centre, Keck Graduate Institute, Claremont, CA, 91711, USA.

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关键词： amphiphilic enzyme sensitive nanosized prodrug peptide dendrimer

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An amphiphilic peptide dendrimer conjugated with gemcitabine (GEM), PEGylated dendron-Gly-Phe-Leu-Gly-GEM (PEGylated dendron-GFLG-GEM), is developed as a nano-prodrug for breast cancer therapy. The self-assembled behavior is observed under a transmission electron microscopy and dynamic light scattering. The negatively charged surface and hydrodynamic size of the amphiphilic nanosized prodrug supported that the prodrug can maintain the stability of GEM during circulation and accumulate in the tumor tissue. Drug release assays are conducted to monitor the release of GEM from this nanodrug delivery system in response to the tumor microenvironment, and these assays confirm that GEM released from the nanocarrier is identical to free GEM. The GEM prodrug can prevent proliferation of tumor cells. The therapeutic effect against breast cancer is systematically investigated using an in vivo animal model. Immunohistochemical results are aligned with the significantly enhanced anticancer efficacy of GEM released from the prodrug. This self-assembled amphiphilic drug delivery nanocarrier may broaden the application for GEM and other anticancer agents for breast cancer chemotherapy. © 2021 Wiley-VCH GmbH.

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出版当年[2021]版：

大类 | 3 区化学

小类 | 2 区高分子科学

最新[2023]版：

大类 | 3 区化学

小类 | 3 区高分子科学

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第一作者机构： [1]Laboratory of Stem Cell Biology, and Huaxi MR Research Center (HMRRC), Department of Radiology, National Clinical Research Center for Geriatrics, Functional and Molecular Imaging Key Laboratory of Sichuan Province, West China Hospital, Sichuan University Chengdu, Chengdu, 610041, P. R. China. [2]School of Pharmacy, Fujian Medical University, Fuzhou, 350122, China.

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