Journal of Chinese Pharmaceutical Sciences ›› 2018, Vol. 27 ›› Issue (4): 229-240.DOI: 10.5246/jcps.2018.04.024

• Original articles • Previous Articles     Next Articles

Construction of folate-conjugated epirubicin liposomes for enhancing the cellular uptake and the co-localization with nuclei of invasive breast cancer cells

Yingzi Bu, Limin Mu, Lei Liu, 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:2018-01-22 Revised:2018-02-22 Online:2018-04-30 Published:2018-03-05
  • Contact: Tel./Fax: +86-010-82802683, E-mail:
  • Supported by:
    The National Natural Science Foundation of China (Grant No. 81373343 and 81673367).


Drug resistance of anthracycline in the invasive cancer is associated with the lowered cellular drug uptake and diminished co-localization of drug with nuclei. In the present study, we aimed to construct the folate-conjugated epirubicin liposomes by incorporating a synthesized folate-lipid derivative; and to assess the effects on cellular drug uptake, co-localization of drug with nuclei and efficacy in treatment of invasive breast cancer cells. The studies were performed on invasive human breast cancer cells. The folate-PEG2000-DSPE conjugate was synthesized, and the constructed folate-conjugated epirubicin liposomes were approximately 100 nm in size. The in vitro studies demonstrated that the folate-conjugated epirubicin liposomes had the strongest cellular drug uptake and co-localization with nuclei of the invasive breast cancer cells. Besides, the liposomes displayed the most significant efficacy in killing the invasive cancer cells, in preventing their invasive potential, and in penetrating ability into breast cancer spheroid as well. In conclusion, the constructed folate-conjugated epirubicin liposomes were able to enhance the efficacy in treatment of invasive breast cancer by improving the cellular drug uptake and increasing the co-localization with nuclei, hence offering a new strategy for potentially eradicating the invasive breast cancer cells.

Key words: Folate conjugated liposomes, Epirubicin, Cellular uptake, Co-localization with nuclei, Invasive breast cancer

CLC Number: