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Article

Improved safety and efficacy of a lipid emulsion loaded with a paclitaxel-cholesterol complex for the treatment of breast tumors

  • Authors:
    • Jun Ye
    • Yuling Liu
    • Xuejun Xia
    • Luhua Meng
    • Wujun Dong
    • Renyun Wang
    • Zhaodi Fu
    • Hongyan Liu
    • Rui Han
  • View Affiliations / Copyright

    Affiliations: State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, P.R. China
  • Pages: 399-409
    |
    Published online on: May 6, 2016
       https://doi.org/10.3892/or.2016.4787
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Abstract

The aim of the present study was to develop a lipid emulsion loaded with a paclitaxel-cholesterol complex (PTX-CH Emul) in order to improve the safety and efficacy of paclitaxel (PTX) and evaluate its antitumor activity against commercially available formulation Taxol®. PTX-CH Emul resembling a low density lipoprotein lipid structure, exhibited an ideal particle size, high drug loading capability, high drug encapsulation efficiency and excellent stability. PTX-CH Emul showed superior in vitro anticancer efficacy against triple-negative MDA-MB-231 breast cancer cells when compared with a paclitaxel emulsion (PTX Emul) and Taxol. The IC70 value of PTX-CH Emul was almost 1.5- and 2.4-fold lower than that of PTX Emul and Taxol, respectively. Compared with PTX Emul and Taxol, PTX-CH Emul exhibited stronger and more rapid inhibitory effects on 3D tumor spheroids of MDA-MB-231 cells. Additionally, in vivo tumor-targeting study showed that PTX-CH Emul had higher specificity and efficiency in intratumoral accumulation as compared to PTX Emul. Finally, the maximum tolerated dose (MTD) of PTX-CH Emul was 2.25‑fold higher than that of Taxol, suggesting that PTX-CH Emul exhibited better safety profiles in vivo than Taxol. At the MTDs, PTX-CH Emul exhibited superior antitumor efficacy in nude mice bearing MDA-MB-231 xenografts in comparison to Taxol. Therefore, PTX-CH Emul as reported here showed high potential as a drug carrier for PTX in clinical applications involving the targeting of triple-negative breast cancer.
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Copy and paste a formatted citation
Spandidos Publications style
Ye J, Liu Y, Xia X, Meng L, Dong W, Wang R, Fu Z, Liu H and Han R: Improved safety and efficacy of a lipid emulsion loaded with a paclitaxel-cholesterol complex for the treatment of breast tumors. Oncol Rep 36: 399-409, 2016.
APA
Ye, J., Liu, Y., Xia, X., Meng, L., Dong, W., Wang, R. ... Han, R. (2016). Improved safety and efficacy of a lipid emulsion loaded with a paclitaxel-cholesterol complex for the treatment of breast tumors. Oncology Reports, 36, 399-409. https://doi.org/10.3892/or.2016.4787
MLA
Ye, J., Liu, Y., Xia, X., Meng, L., Dong, W., Wang, R., Fu, Z., Liu, H., Han, R."Improved safety and efficacy of a lipid emulsion loaded with a paclitaxel-cholesterol complex for the treatment of breast tumors". Oncology Reports 36.1 (2016): 399-409.
Chicago
Ye, J., Liu, Y., Xia, X., Meng, L., Dong, W., Wang, R., Fu, Z., Liu, H., Han, R."Improved safety and efficacy of a lipid emulsion loaded with a paclitaxel-cholesterol complex for the treatment of breast tumors". Oncology Reports 36, no. 1 (2016): 399-409. https://doi.org/10.3892/or.2016.4787
Copy and paste a formatted citation
x
Spandidos Publications style
Ye J, Liu Y, Xia X, Meng L, Dong W, Wang R, Fu Z, Liu H and Han R: Improved safety and efficacy of a lipid emulsion loaded with a paclitaxel-cholesterol complex for the treatment of breast tumors. Oncol Rep 36: 399-409, 2016.
APA
Ye, J., Liu, Y., Xia, X., Meng, L., Dong, W., Wang, R. ... Han, R. (2016). Improved safety and efficacy of a lipid emulsion loaded with a paclitaxel-cholesterol complex for the treatment of breast tumors. Oncology Reports, 36, 399-409. https://doi.org/10.3892/or.2016.4787
MLA
Ye, J., Liu, Y., Xia, X., Meng, L., Dong, W., Wang, R., Fu, Z., Liu, H., Han, R."Improved safety and efficacy of a lipid emulsion loaded with a paclitaxel-cholesterol complex for the treatment of breast tumors". Oncology Reports 36.1 (2016): 399-409.
Chicago
Ye, J., Liu, Y., Xia, X., Meng, L., Dong, W., Wang, R., Fu, Z., Liu, H., Han, R."Improved safety and efficacy of a lipid emulsion loaded with a paclitaxel-cholesterol complex for the treatment of breast tumors". Oncology Reports 36, no. 1 (2016): 399-409. https://doi.org/10.3892/or.2016.4787
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