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Paclitaxel-loaded stealth liposomes: Development, characterization, pharmacokinetics, and biodistribution

机译:载有紫杉醇的隐形脂质体:研发,鉴定,药代动力学和生物分布

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Abstract Aim: In the present paper, paclitaxel (PTX)-loaded stealth liposomes were prepared with thin film hydration technique in order to prolong the time of circulation. Method: The liposomes’ characterization, in vitro release, pharmacokinetics, and biodistribution profile of the drug were investigated. Results: Microscope showed that the liposomes were spherical in shape with a smooth surface and the size was uniform and appropriate for administration via intravenous injection. The encapsulation efficiency was 91.1 ± 4.3%, and the mean diameter was 82.2 ± 7.6 nm from three batches. The results of in vivo studies indicated that PTX-loaded stealth liposomes show favorable pharmacokinetics and biodistribution compared to the free drug. In comparison with free PTX, the AUC0-t of PTX liposomes and stealth liposomes increased 1.91- and 3.39-fold, respectively. The stealth liposomes were long-circulating showing a half-life time of 34.2 h against 13.7 h for the conventional ones. Conclusions: These results suggest that stealth liposomes would serve as a potent PTX delivery vehicle for the future cancer chemotherapy and represent a suitable platform for the development of targeted liposomal PTX systems.
机译:摘要目的:采用薄膜水化技术制备载有紫杉醇(PTX)的隐形脂质体,以延长其循环时间。方法:研究该药物的脂质体特性,体外释放,药代动力学和生物分布特征。结果:显微镜检查显示脂质体为球形,表面光滑,大小均匀,适合静脉注射给药。三批次的封装效率为91.1±4.3%,平均直径为82.2±7.6 nm。体内研究结果表明,与游离药物相比,载有PTX的隐形脂质体显示出良好的药代动力学和生物分布。与游离PTX相比,PTX脂质体和隐形脂质体的AUC0-t分别增加了1.91倍和3.39倍。隐性脂质体是长循环的,显示半衰期为34.2小时,而传统脂质体的半衰期为13.7小时。结论:这些结果表明,隐形脂质体将作为未来癌症化疗的有效PTX传递载体,并代表开发靶向脂质体PTX系统的合适平台。

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