期刊
JOURNAL OF CONTROLLED RELEASE
卷 331, 期 -, 页码 460-471出版社
ELSEVIER
DOI: 10.1016/j.jconrel.2021.01.037
关键词
Synergistic therapy; Nanoprodrug; COX-2 inhibitor; Cisplatin; Drug-drug conjugate
资金
- National Natural Science Foundation of China [82020108029, 82073398, 81773667, 81970717, 81873185]
- Priority Academic Program Development of Jiangsu Higher Education Institutions
- Project of State Key Laboratory of Natural Medicines, China Pharmaceutical University [SKLNMZZ202021]
- 111 Project from the Ministry of Education of China
- State Administration of Foreign Experts Affairs of China [B16046]
- Project of State Key Laboratory of Pathogenesis, Xinjiang Medical University [SKL-HIDCA-2019-7]
- Double first-class project [CPU2018GY06]
- Key Research and Development Program of Jiangsu Province [BE2018742]
Tolfplatin is a carrier-free self-delivered nanopmdrug that can inhibit tumor proliferation and metastasis by reducing PGE2 secretion and inducing apoptotic cell death.
Cisplatin is one of the most used first-line anticancer drugs for various solid tumor therapies. However, cisplatin-based chemotherapy can induce tumor cells to secrete excessive prostaglandin E2 (PGE2) catalyzed by cyclooxygenase-2 (COX-2), which, in turn, counteracts its chemotherapeutic effect and further accelerates tumor metastasis. Here, we report a carrier-free self-delivered nanopmdrug based on platinum (II) coordination bonding coupled with tolfenamic acid (Toll) (named Tolfplatin). Tolfplatin can spontaneously assemble into uniformly sized nanoparticles (NPs) with a high drug-loading capacity. Compared with cisplatin, Tolfplatin NPs can facilitate cellular uptake, significantly decrease PGE2 secretion by COX-2 inhibition, which further down-regulate tumorous anti-apoptotic and metastasis-associated proteins, thereby efficiently inducing apoptotic cell death and significantly inhibit tumor metastasis in vitro and in vivo. Therefore, as the carrier-free nanopmdrug, Tolfplatin NPs are promising anti-tumoral agents to inhibit tumor proliferation and metastasis by enriching the function and promoting the anti-tumor activity of cisplatin.
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