Chinese Journal of Tissue Engineering Research ›› 2016, Vol. 20 ›› Issue (30): 4489-4495.doi: 10.3969/j.issn.2095-4344.2016.30.012

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Long-circulating methotrexate-loaded liposomes exhibit an antitumor effect on human osteosarcoma in vitro

Qin Ying-zhou, Chen Han, Zhang Yang, Zhang Qi-qing, Liu Ling-rong   

  1. Institute of Biomedical Engineering, Chinese Academy of Medical Science & Peking Union Medical College, Tianjin 300192, China
  • Online:2016-07-15 Published:2016-07-15
  • Contact: Liu Ling-rong, Associate researcher, Institute of Biomedical Engineering, Chinese Academy of Medical Science & Peking Union Medical College, Tianjin 300192, China
  • About author:Qin Ying-zhou, Studying for master’s degree, Institute of Biomedical Engineering, Chinese Academy of Medical Science & Peking Union Medical College, Tianjin 300192, China
  • Supported by:

    the National Natural Science Foundation of China, No. 31170917

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Abstract:

BACKGROUND: Liposomes as a new drug delivery system are characterized by few adverse reactions, no immunogenicity and biodegradation. Furthermore, methotrexate-loaded liposomes can significantly reduce drug toxicity and improve anti-tumor effect.
OBJECTIVE: To prepare long-circulating methotrexate-loaded liposomes and to evaluate its antitumor activity in MG-63 in vitro.
METHODS: The methotrexate-loaded liposomes were prepared using the film dispersion method, and the long-circulating ones were prepared using the post-insertion method. The initial concentrations of methotrexate were 9.1, 1.82, 0.364 g/L. The ultracentrifugation method and spin column method with Sephadex G-10 or G-50 as packing were employed to separate free drugs from the methotrexate-loaded liposomes. Their recovery, size, morphology, encapsulation efficiency and drug-to-lipid ratio were evaluated. The cytotoxity of the long-circulating methotrexate-loaded liposomes purified with ultracentrifugation method and spin column G-50 method under three dose levels (0, 1, 5, 25 mg/L) were determined by MTS method.
RESULTS AND CONCLUSION: According to the recovery rates of three methods, the spin column G-50 method was considered as optimal for the long-circulating methotrexate-loaded liposomes. The long-circulating liposomes were spherical or ellipsoidal under transmission electron microscope, about  200 nm in size. At the certain initial concentration of methotrexate, the encapsulation efficiency and drug-to-lipid ratio of the liposomes purified using the spin column G-50 method were remarkably higher than those purified using the other two methods. At the same mass concentration, the cytotoxity of the liposomes purified with ultracentrifugation or spin column G-50 was significantly higher than that of free methotrexate, and furthermore, the cytotoxity of the liposomes purified with spin column G-50 was higher than that of the liposomes purified with ultracentrifugation method. To conclude, the long-circulating methotrexate-loaded liposomes show a higher antitumor activity than free methotrexate in MG-63 cells in vitro, providing the basis for further investigation of its antitumor effect on human osteosarcoma in vivo.

中国组织工程研究杂志出版内容重点：生物材料；骨生物材料; 口腔生物材料; 纳米材料; 缓释材料; 材料相容性；组织工程

Key words: Liposomes, Methotrexate, Osteosarcoma, Tissue Engineering

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