Paclitaxel targeting to lungs by way of liposomes prepared by the effervescent dispersion technique
Paclitaxel targeting to lungs by way of liposomes prepared by the effervescent dispersion technique
复制标题
紫杉醇通过泡腾分散技术制备的脂质体靶向肺部
DOI：
10.1007/s12272-013-0181-8
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发表时间：
2013-06
期刊：
影响因子：
--
通讯作者：
Wei Y, Xue Z, Ye Y, Huang Y, Zhao L*（赵领）（通讯作者）
中科院分区：
文献类型：
--
作者：
Wei Y, Xue Z, Ye Y, Huang Y, Zhao L*（赵领）（通讯作者）
为研制新型肺靶向紫杉醇（PTX）大粒径脂质体给药系统（LTDDS），以紫杉醇（PTX）、磷脂酰肌醇90 H和吐温-80为原料，采用微球分散技术制备了紫杉醇脂质体。脂质体的粒径相对均匀（8.166 ± 0.459 μm），zeta电位为负（−12.45 ± 1.34 mv），包封率较高（92.20 ± 2.56%）。它们保持稳定至少3个月，并表现出缓慢释放行为，没有任何溶血反应。与注射液相比，PTX脂质体在家兔体内的平均滞留时间和消除半衰期延长，血药浓度-时间曲线下面积增大，同时改变了其生物分布，具有明显的肺靶向性。如肺的相对摄入率（Re）和峰浓度比（Ce）分别为14.87和26.44。与心、肝、脾、肾相比，肺靶向效率脂质体与肺靶向效率注射液的比值分别增加了20.08、11.10、6.97和14.41倍。因此，脂质体作为紫杉醇的LTDDS有可能成为一种很好的肺癌治疗药物载体。
In order to develop a novel lung targeting drug delivery system (LTDDS) with large-sized liposomes containing paclitaxel (PTX), the liposomes composed of PTX, phosopholipon 90H and tween-80 were prepared by the effervescent dispersion technique with optimal formulation composition. The liposomes were found to be relatively uniform in particle size (8.166 ± 0.459 μm) with a negative zeta-potential (−12.45 ± 1.34 mv), and high entrapment efficiency (92.20 ± 2.56 %). They kept stable for at least 3 months and exhibited a slow release behavior without any hemolysis reaction. Via intravenous administration in rabbits, the PTX liposomes presented a longer mean residence time and elimination half-life, and a much larger area under the plasma drug concentration–time curve compared with its injection; meanwhile, the liposomes altered its biodistribution and exhibited a significant lung targeting characteristic. For example, the relative intake rate (Re) and the ratio of peak concentration (Ce) of lung were 14.87 and 26.44, respectively. Compared with heart, liver, spleen and kidney, the ratios of targeting efficacy (Te)liposomesto (Te)injectionof lung were increased by a factor of 20.08, 11.10, 6.97 and 14.41, respectively. To sum up, the liposome could be a promising drug carrier for PTX as LTDDS for lung cancer treatment.
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DOI：
--
发表时间：
2005-03
期刊：
Yao xue xue bao = Acta pharmaceutica Sinica
影响因子：
--
作者：
Jiansong Wang;Jia-bi Zhu;Ruicong Lu;W. Shen
通讯作者：
Jiansong Wang;Jia-bi Zhu;Ruicong Lu;W. Shen
影响因子：
4.5
作者：
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通讯作者：
Zhu Jia-Bi
影响因子：
4.5
作者：
Sun, Weitong;Zou, Weiwei;Zhang, Na
通讯作者：
Zhang, Na
影响因子：
3.3
作者：
Ling Zhao;Yun Ye;Juan Li;Yu-meng Wei
通讯作者：
Ling Zhao;Yun Ye;Juan Li;Yu-meng Wei
影响因子：
10.8
作者：
Crosasso, P;Ceruti, M;Cattel, L
通讯作者：
Cattel, L