紫杉醇
泊洛沙姆
体内
胶束
内吞作用
药理学
生物利用度
体外
多重耐药
药物输送
材料科学
化学
细胞
化疗
医学
生物化学
纳米技术
共聚物
生物
外科
有机化学
生物技术
抗生素
水溶液
复合材料
聚合物
作者
Wei Zhang,Yuan Shi,Yanzuo Chen,Ye Jiang,Xianyi Sha,Xiaoling Fang
出处
期刊:Biomaterials
[Elsevier]
日期:2011-04-01
卷期号:32 (11): 2894-2906
被引量:326
标识
DOI:10.1016/j.biomaterials.2010.12.039
摘要
The aim of this study was to exploit the possibility of combination of active targeting function of folic acid by folate receptor-mediated endocytosis and overcoming multidrug resistance (MDR) by Pluronic block copolymers to promote drug delivery to MDR tumor following intravenous administration with paclitaxel (PTX) as model drug. Folic acid functionalized Pluronic P123/F127 mixed micelles encapsulating PTX (FPF-PTX) was firstly developed and tested in vitro and in vivo, while PTX-loaded Pluronic P123/F127 mixed micelles (PF-PTX) and Taxol were used as control. FPF-PTX was about 20 nm in diameter with spherical shape and high encapsulation efficiency. Cellular uptake of FPF-PTX was found to be higher than that of PF-PTX due to the folate receptor-mediated endocytosis effect. In vitro cytotoxicity, cell apoptosis and cell cycle arrest studies also revealed that FPF-PTX was more potent than those of PF-PTX and Taxol. In vivo pharmacokinetic study in rats showed that the polymeric micelles significantly enhanced the bioavailability of PTX (∼3 fold) than Taxol. Moreover, in BALB/c mice bearing KBv MDR tumor xenografts, stronger antitumor efficacy was shown in FPF-PTX group, with good correlation between in vitro and in vivo. In conclusion, folate-conjugated Pluronic micelles could be a potential vehicle for delivering hydrophobic chemotherapeutic drugs to MDR tumors.
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