目的 对表柔比星-白藜芦醇复方脂质体的制备工艺进行研究,并对其抗肿瘤作用进行评价。方法 采用薄膜分散法-硫酸铵梯度法制备复方脂质体,并对处方进行优化;用RP-HPLC测定复方脂质体的包封率;磺酰罗丹明B蛋白染色法(sulforhodamine B,SRB)评价体外抗肿瘤作用。结果 采用最优处方,以薄膜分散法-硫酸铵梯度法制备的复方脂质体中表柔比星与白藜芦醇包封率分别为87%、61%;制备得到的复方脂质体对C6胶质瘤细胞具有较强的抑制作用。结论 本方法制备复方脂质体操作简便、重复性好,包封率较高,体外抗肿瘤作用强。
Abstract
OBJECTIVE To study the preparation process of epirubicin-resveratrol compound liposomes (EPI-RES-L) and investigate its anticancer effects in vitro. METHODS The compound liposomes were prepared by film dispersion-pH gradient method. The formulation was optimized, and the encapsulation efficiency was determined by RP-HPLC. The anticancer effect of EPI-RES-L in vitro was studied by sulforhodamine B (SRB) protein staining method. RESULTS The encapsulation efficiencies were 87% and 61% for epirubicin (EPI) and resveratrol (RES), respectively. The cytotoxicity of EPI-RES-L was significantly higher than that of free drugs against C6 glioma cells. CONCLUSION The film dispersion-pH gradient method is simple, reproducible, and has high drug encapsulation efficiency. EPI-RES-L has potent anticancer effect.
关键词
表柔比星 /
白藜芦醇 /
脂质体 /
高效液相色谱法 /
体外抗肿瘤作用
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Key words
epirubicin /
resveratrol /
liposome /
HPLC /
entrapment efficiency
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中图分类号:
R944
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参考文献
[1] SUN Y. New milestone in the development of clinical oncology-molecular targeted therapy.Anti-tumor Pharmacy(肿瘤药学),2011,1(1):1-5.[2] LV L.The study of the epirubicin poly-butylcyanoacrylate magnetic nanoparticles and obseration of therapeutic effect in the targeted therapy of the hepatoma.China, Hunan: Central South University,2006. [3] ZHANG W, FEI Z, ZHEN H N, et al. Resveratrol inhibits cell growth and induces apoptosis of rat C6 glioma cells. Neurooncol, 2007, 81(3):231-240. [4] GAGLIANO N, ALDINI G, COLOMBO G, et al.The potential of resveratrol against human gliomas. Anticancer Drugs, 2010, 21(2):140-150.[5] ZHAO Y,YU B,DENG Y H,et al. Preparation of liposomes entrapped vincristine sulfate by active loading and determination of its entrapment efficiency . Chin Pharm J(中国药学杂志),2005, 40(20):1559-1561.[6] ZHOU J Y. The effect of the combination of epirubicin and resveratrol on many human cancer cell. Beijing: Peking Union Medical College,2010. [7] GUO J, HONG Z W, FANG X L . Optimization of epirubicin liposome formulation using Box-Behnken experimental design. Fudan Univ J Med Sci(复旦学报:医学版), 2007,34(6):816-820.[8] HAN Z K, SUN J B, LIU D, et al. Preparation and evaluation of long-circulating liposomes of paraoxonase. J China Med Univ(中国医科大学学报),2010,39(2):87-91.[9] TAN W D, JIN H, LUO D X, et al. Comparison of MTT with SRB assays in vitro anticancer drug screening. Nat Prod Res Develop(天然产物研究与开发),2003,11(3):19-21. KIMBERLY S S, TRICIA S, DENISE B, et al. Resveratrol exerts differential effects in vitro and in vivo against ovarian cancer cells . Res Comm, 2010, 13(4):1333-1340.
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脚注
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基金
国家自然科学基金资助项目(81160396);石河子大学重大攻关计划项目(gxjs2010-zdgg04-03);石河子大学高层次人才科研项目(RCZX201029)
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