期刊
MACROMOLECULAR RAPID COMMUNICATIONS
卷 42, 期 12, 页码 -出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/marc.202100111
关键词
amphiphilic; enzyme sensitive; nanosized prodrug; peptide dendrimer
资金
- National Natural Science Foundation of China [51703245, 81701807, 51873120, 51673127, 81621003]
- Natural Science Foundation of Fujian Province [2020J01621]
- Natural Science Foundation of Jiangsu Province [BK20170733]
- West China Hospital of Sichuan University [ZYGD18028, 2020HXBH072]
- Research Initiate Funds of Fujian Medical University [XRCZX2020001]
An amphiphilic peptide dendrimer conjugated with gemcitabine has been developed as a nano-prodrug for breast cancer therapy, showing self-assembled behavior and effective release of the drug. In vivo studies confirm the therapeutic efficacy of the drug against breast cancer, indicating potential applications for gemcitabine and other anticancer agents.
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.
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