Journal of Chinese Pharmaceutical Sciences ›› 2016, Vol. 25 ›› Issue (4): 266-274.DOI: 10.5246/jcps.2016.04.030

• Original articles • Previous Articles     Next Articles

The use of a new functional glucose conjugate material, TPGS1000-Glu, in treatment of brain glioma by incorporating into epirubicin liposomes

Limin Mu, Jiashuan Wu, Hongjun Xie, Lei Liu, Fan Zeng, Yan Yan, Yao Zhao, Yingjie Hu, Yingzi Bu, Wanliang Lu*   

  1. Beijing Key Laboratory of Molecular Pharmaceutics and New Drug System; State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China
  • Received:2015-12-16 Revised:2016-01-15 Online:2016-04-21 Published:2016-01-25
  • Contact: Tel.: 86-10-82802683, E-mail:
  • Supported by:

    National Basic Research Program of China (973 Program, Grant No. 2013CB932501), Beijing Natural Science Foundation (Grant No. 7131009), and National Natural Science Foundation of China (Grant No. 81373343).


Most of anticancer agents can not be used for treatment of brain glioma due to the existence of the blood brain barrier (BBB). The over-expression of glucose transporters (GLUTs) on the BBB and brain glioma cells enables the possibility that the GLUTs ligand modified drug carrier transports across the BBB, and targets to the brain glioma cells. The objectives of the present study were to synthesize a new glucose conjugate material, TPGS1000-Glu, develop a kind of TPGS1000-Glu modified epirubicin liposomes, and evaluate their efficacy. The studies were performed on the BBB co-culture model and brain glioma cells in vitro. TPGS1000-Glu was synthesized by conjugating TPGS1000-COOH with 4-aminophenyl-β-D-glucopyranoside (Glu), and confirmed by MALDI-TOF-MSspectrum. TPGS1000-Glu modified epirubicin liposomes were prepared with a high drug encapsulation efficiency (>97%), a nanosize (approximately 90 nm), and a minimal drug leakage in fetal bovine serum (FBS)-containing buffer system. The BBB co-culture model was established, and after applying TPGS1000-Glu modified epirubicin liposomes to the model, transport of liposomal drug across the BBB was evidenced. Besides, TPGS1000-Glu modified epirubicin liposomes showed the strongest cellular drug uptake and anti-glioma efficacy after transport across the BBB in vitro. The synthesized TPGS1000-Glu material could offer a new targeting ligand for the BBB, while the developed TPGS1000-Glu modified epirubicin liposomes might provide a potential anticancer formulation for treatment of brain glioma.

Key words: TPGS1000-Glu, Epirubicin, Liposomes, Glucose transporters, Brain glioma

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