Journal of Capital Medical University ›› 2015, Vol. 36 ›› Issue (2): 172-177.doi: 10.3969/j.issn.1006-7795.2015.02.004

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Preparation and anti-tumor activity of a novel liposome-loaded drug

Lu Xuemei1, Wang Yuji2, Wu Jianhui2, Cui Chunying1   

  1. 1. Department of Pharmaceutics, School of Chemical Biology and Pharmaceutical Sciences, Capital Medical University, Beijing 100069, China;
    2. Department of Medicinal Chemistry, School of Chemical Biology and Pharmaceutical Sciences, Capital Medical University, Beijing 100069, China
  • Received:2014-12-08 Online:2015-04-21 Published:2015-04-16
  • Supported by:
    This study was supported by Significant New Drugs Creation "Five-year" Plan Special Science and Technology Major(2011ZX09302-007-01).

Abstract: Objective To prepare an Arg-Gly-Asp-Phe-fatty alcohol(RGDFOC12) liposomes-loaded 17-allylamino-17-demethoxygeldanamycin(17-AAG). Methods RGDFOC12 liposomes-loaded 17-AAG(RLAs) was prepared by film dispersion method and evaluated by particle size analysis, Zeta potential, encapsulation efficiency, the release in vitro, plasma stability, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide(MTT) assay and the anti-tumor activity in vivo. Results The RLAs was stable colloidal dispersion system in spherical shape of (130.6±0.6)nm in diameter and the Zeta potential was (-28.37±1.67)mV. The release of RLAs in vitro showed that the released percentage of RLAs in pH 5.4 is more than that in pH 7.4. The MTT assay proved that RLAs inhibited the proliferation of cancer cells. The anti-tumor assay showed that RLAs inhibited tumor growth and reduced the toxicity. Conclusion The RLAs were prepared by film dispersion method. RLAs showed anti-tumor activity in vivo and good potential in cancer therapy.

Key words: anti-tumor, 17-allylamino-17-demethoxygeldanamycin(17-AAG), Arg-Gly-Asp-Phe-fatty alcohol(RGDFOC12)

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