Journal
BIOMATERIALS SCIENCE
Volume 3, Issue 1, Pages 182-191Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c4bm00305e
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Funding
- National Natural Science Foundation of China [51403198, 51321062, 21174143]
- Ministry of Science and Technology of China (863 Project) [SS2012AA020603]
- 100 Talents Program of Chinese Academy of Sciences [KGCX2YW- 802]
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The main obstacles to cancer therapy are the inability to target cancer cells and the acquired drug resistance after a period of chemotherapy. Reduced drug uptake and DNA repair are the two main mechanisms involved in cisplatin resistance. In the present investigation, canthaplatin, a Pt(IV) pro-drug of cisplatin and a protein phosphatase 2A (PP2A) inhibitor (4-(3-carboxy-7-oxa-bicyclo[2.2.1]heptane-2-carbonyl)piperazine-1-carboxylic acid tert-butyl ester), was designed and delivered using PEG-b-PLGA micelles for combination chemotherapy. Polymer/canthaplatin micelles facilitated the delivery of the drug into cancer cells through endocytosis and diminished DNA repair by PP2A inhibition, resulting in enhanced anti-tumor efficiency and excellent reversal ability of tumor resistance to cisplatin both in vitro and in vivo. Additionally, the polymer/canthaplatin micelles could prolong drug residence in the blood and decrease the side effects when compared to cisplatin.
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