Nanostructured lipid carriers as novel carrier for parenteral delivery of docetaxel
Nanostructured lipid carriers as novel carrier for parenteral delivery of docetaxel
复制标题
DOI：
10.1016/j.colsurfb.2011.02.038
复制
发表时间：
2011-07-01
影响因子：
5.8
通讯作者：
Zhang, Na
中科院分区：
文献类型：
--
作者：
Liu, Donghua;Liu, Zhihong;Zhang, Na
本研究旨在设计多西他赛负载的纳米结构脂质载体（DTX-NLC）以降低毒性并提高治疗效果。采用改进膜超声-分散法制备了多西他赛负载的纳米结构脂质载体。采用粒径分布、zeta电位和包封效率对DTX-NLC进行表征。采用MTT法评价DTX-NLC对3种人癌细胞系和1种小鼠恶性黑色素瘤（B16）的体外细胞毒性。AnnexinV-FITC试剂盒检测多帕菲(R)或DTX-NLC诱导的细胞凋亡百分比。对昆明小鼠恶性黑色素瘤（B16）进行体内抗肿瘤疗效评价。与多帕菲(R)相比，DTX-NLC对A549细胞表现出更强的细胞毒性，诱导更多的细胞凋亡和G2/M阻滞。多帕菲(R)、DTX-NLC （10 mg/kg）和DTX-NLC （20 mg/kg）的抑制率分别为42.74%、62.69%和90.36%，表明DTX-NLC能更有效地抑制肿瘤生长。小鼠体重变化结果也显示，与多帕菲(R)相比，DTX-NLC在治疗过程中毒性更低。这些结果表明，DTX-NLC可能是一种很有前途的癌症治疗药物传递系统。据我们所知，这是关于DTX-NLC治疗小鼠恶性黑色素瘤的第一篇报道。(C) 2011 Elsevier B.V.版权所有
The aim of this study was to design docetaxel-loaded nanostructured lipid carriers (DTX-NLC) to reduce toxicity and improve therapeutic efficacy. Docetaxel-loaded nanostructured lipid carriers (DTX-NLC) were prepared by the modified film ultrasonication-dispersion method. The DTX-NLC were characterized by particle size distribution, zeta potential and entrapment efficiency. In vitro cytotoxicity of DTX-NLC was evaluated by MTT assay against three human cancer cell lines and one murine malignant melanoma (B16). AnnexinV-FITC kit was used to measure the percentage of apoptosis induced by Duopafei(R) or DTX-NLC. In vivo anti-tumor efficacy was evaluated in Kunming mice bearing murine malignant melanoma (B16). Compared with Duopafei(R), DTX-NLC revealed more cytotoxicity against A549 cells by inducing more apoptosis and more G2/M arrest. The inhibition rates of Duopafei(R), DTX-NLC (10 mg/kg) and DTX-NLC (20 mg/kg) were 42.74%, 62.69% and 90.36%, respectively, indicating that DTX-NLC could more effectively inhibit tumor growth. The results of the body weight variations of mice also showed that compared with Duopafei(R), DTX-NLC had lower toxicity during the therapeutic procedure. These results suggest that DTX-NLC may be a promising drug delivery system for cancer therapy. To our knowledge, this was the first report about DTX-NLC for murine malignant melanoma treatment. (C) 2011 Elsevier B.V. All rights reserved.