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Updated: Mar 17, 2026

Polymalic Acid-based Nano Biopolymers for Targeting of Multiple Tumor Markers: An Opportunity for Personalized Medicine?
Published on: June 13, 2014
Tumor Microenvironmental Stimuli-Responsive Linear-Dendritic Polymeric Conjugate as Potential Nanomedicine
Yongchao Wang1, Pan Xiang1, Yinggang Li1
1Department of Radiology, Institution of Radiology and Medical Imaging, Huaxi MR Research Center (HMRRC), Department of Thoracic Surgery and Institute of Thoracic Oncology, Frontiers Science Center for Disease-Related Molecular Network, West China Hospital, Sichuan University, Chengdu, China.
None:
A linear-dendritic polymer has been explored as a drug delivery vehicle for cancer therapy. In this study, we successfully prepared a tumor microenvironment-responsive, dendronized and block poly[N-(2-hydroxypropyl) methacrylamide] (polyHPMA)-based copolymer-doxorubicin conjugate (pHPMA-block-pDendron-DOX) via two-step reversible addition-fragmentation chain transfer (RAFT) polymerization. The conjugate self-assembled into nanoparticles (NPs). Due to the presence of the Gly-Phe-Leu-Gly (GFLG) tetrapeptide and the hydrazone bond in the structure of the conjugate, cathepsin B-responsive degradation and pH-responsive drug release were realized within the tumor microenvironment. The NPs displayed a distinctive cytotoxic effect on 4T1 cells after internalization through endocytosis pathways. Significant improvements in the accumulation of doxorubicin (DOX) from the NPs were observed at the tumor site in a 4T1 murine breast cancer xenograft model, leading to promising anti-cancer effects. In addition, the side effects of DOX were significantly diminished in the NPs at a high dose. The prepared linear-dendritic conjugate could be used as an efficient and safe nanomedicine.
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