Folate-targeted redox-responsive polymersomes loaded with chemotherapeutic drugs and tariquidar to overcome drug resistance

Yu Qin, Zhiming Zhang, Chenlu Huang, Fan Fan, Lanxia Liu, Li Lu, Hai Wang, Zhipeng Liu, Jun Yang, Chun Wang, Hu Yang, Hongfan Sun, Xigang Leng, Deling Kong, Linhua Zhang, Dunwan Zhu

Research output: Contribution to journalArticlepeer-review

6 Scopus citations


Tumor multidrug resistance (MDR) is a fatal obstacle to cancer chemotherapy. The combination of P-glycoprotein (P-gp) inhibitor and chemotherapeutic drugs is one of the effective strategies to reverse tumor MDR. Herein, a folate-decorated PCL-ss-PEG-ss-PCL based redox-responsive polymersome (FA-TQR-Co-PS) was constructed, which was loaded with P-gp inhibitor tariquidar (TQR), anticancer drugs doxorubicin (DOX) and paclitaxel (PTX). The results suggested that the FA-TQR-Co-PS with an apparent bilayered lamellar structure displayed good monodispersity, high drug loading capacity, superior stability and redox-stimulated drug release peculiarity. In vitro cellular uptake study demonstrated that FA-TQR-Co-PS increased drug accumulation into MCF-7/ADR cells via the TQR-induced P-gp efflux inhibition, and further improved targeting to tumor cells due to folate receptor-mediated endocytosis. Furthermore, the DOX and PTX cytotoxicity and proapoptotic activity against MCF-7/ADR was enhanced dramatically along with the administration of TQR, and the cell cycle was profoundly blocked in G2/M phase. The folate-targeted redox-responsive polymersomes loaded with chemotherapeutic drugs and P-gp inhibitor demonstrated noticeable synergistic effect against human MDR MCF-7 cells and successfully reversed drug resistance, which displayed high potential in overcoming tumor MDR as a novel drug delivery system.

Original languageEnglish (US)
Pages (from-to)1705-1718
Number of pages14
JournalJournal of Biomedical Nanotechnology
Issue number10
StatePublished - Oct 2018


  • Combination Therapy
  • Drug Resistance
  • Polymersome
  • Redox-Responsive
  • Tariquidar

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