Journal of Chinese Pharmaceutical Sciences ›› 2019, Vol. 28 ›› Issue (2): 121-133.DOI: 10.5246/jcps.2019.02.012

• Original articles • Previous Articles     Next Articles

The cellular uptake and anti-tumor activity of conjugated linoleic acid-paclitaxel-loaded iRGD-modified lysolipid-containing thermosensitive liposomes

Yanli Hao1,2, Ting Zhong1,2, Ruo Du2, Hua Zhang3, Bilin Liu4, Xuan Zhang1,2*   

  1. 1. Beijing Key Laboratory of Molecular Pharmaceutics and New Drug Delivery Systems, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China
    2. Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China
    3. Key Laboratory of Xinjiang Phytomedicine Resources and Utilization of Ministry of Education, School of Pharmacy, Shihezi University, Shihezi 832000, China
    4. College of Pharmaceutical Engineering, Chongqing Chemical Industry Vocational College, Chongqing 401228, China
  • Received:2018-09-14 Revised:2018-10-29 Online:2019-02-28 Published:2019-01-03
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  • Supported by:

    National Natural Science Foundation of China (Grant No. 81172992) and the National Key Research and Development Program of China (Grant No. 2017YFA0205600).


In the present study, we prepared the iRGD-modified lysolipid-containing thermosensitive liposomes (LTSL) containing conjugated linoleic acid-paclitaxel (CLA-PTX), also known as iRGD-LTSL-CLA-PTX. The in vitro cellular uptake and invitro cytotoxicity of iRGD-LTSL-CLA-PTX were evaluated in B16-F10 melanoma cells. The in vivo anti-tumor effect of iRGD-LTSL-CLA-PTX was investigated using B16-F10 tumor-bearing C57BL/6 mice. The results of the cellular uptake experimentindicated that the increased cellular uptake of CLA-PTX in the iRGD-LTSL-CLA-PTX-treated groups was 2.05-, 3.31- or 4.83-foldcompared with that in the SSL-CLA-PTX group after a 2-, 4- or 6-h incubation at 42°C, respectively. The in vivo antitumor results showed that iRGD-LTSL-CLA-PTX/heat significantly inhibited the growth of B16-F10 tumors compared with the CLA-PTX solution (LTSL-CLA-PTX, LTSL-CLA-PTX/heat and iRGD-LTSL-CLA-PTX) (P<0.01). In conclusion, the antitumor effect of iRGD-LTSL-CLA-PTX was confirmed on B16-F10 melanoma in vitro and in vivo, which was induced by both the effect of iRGD and LTSL.

Key words: iRGD, Lysolipid-containing thermosensitive liposomes, CLA-PTX, Antitumor effect, In vitro, In vivo

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