Journal of Chinese Pharmaceutical Sciences ›› 2018, Vol. 27 ›› Issue (5): 332-341.DOI: 10.5246/jcps.2018.05.034

• Original articles • Previous Articles     Next Articles

Preparation, characterization and evaluation of multi-component-loaded liposomes containing Tat-TOS, phospholipase D inhibitor and doxorubicin

Maoyuan Song, Yuanyuan Zhang, Wenxi Zhang, Guanghua Peng, Jiaxing Wang, Mengya Yin, Jiajia Li, Yajie Liu, Xinru Li*   

  1. Beijing Key Laboratory of Molecular Pharmaceutics and New Drug System; School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China
  • Received:2018-02-12 Revised:2018-03-15 Online:2018-05-31 Published:2018-04-10
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  • Supported by:
    The National Natural Science Foundation of China (Grant No. 81541085).


In the present study, we aimed to co-load the α-TOS conjugate Tat-TOS with the phospholipase D inhibitor FIPI and the antitumor drug doxorubicin (DOX) in a liposome delivery system for antitumor metastasis. Firstly, Tat-TOS was synthesized by solid-phase synthesis, and its structure was confirmed. The ability of free and liposomal Tat-TOS to induce apoptosis in vitro was evaluated by flow cytometry. Biodistribution of Tat-TOS-loaded liposomes was investigated by a molecular imaging system. Multi-component-loaded liposomes modified with Tat-TOS containing FIPI and DOX was prepared by thin film dispersion method in combination with pH gradient method and post-insertion method. Physicochemical properties were determined, and the in vitro uptake ability of the formulations was evaluated. The results showed that the prepared liposomes were characterized by a uniform particle size distribution and small particle size. The encapsulation efficiency of FIPI and DOX exceeded 85%. Both free and liposomal Tat-TOS significantly improved the activity of inducing apoptosis of tumor cells. The liposomes modified with Tat-TOS were apparently accumulated in normal lung tissue and tumor metastasized lung. Multi-component-loaded liposomes exhibited the strongest cell uptake capacity, suggesting a stronger anti-metastatic effect and anti-tumor activity in vivo.

Key words: Doxorubicin, FIPI, Liposomes, α-TOS, Tat

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