The targeting properties of folate-conjugated Pluronic F127/poly(lactic-co-glycolic) nanoparticles
The targeting properties of folate-conjugated Pluronic F127/poly(lactic-co-glycolic) nanoparticles
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DOI：
10.1016/j.ijbiomac.2017.07.085
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发表时间：
2017-12-01
影响因子：
8.2
通讯作者：
Li, Yu Ping
中科院分区：
文献类型：
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作者：
Luo, Yue Yuan;Xiong, Xiang Yuan;Li, Yu Ping
合成了新型叶酸Pluronic F127/聚乳酸-羟基乙酸共聚物（FA-F127-PLGA）和PLGA-F127-PLGA嵌段共聚物，并通过透析法制备了这两种共聚物的自组装纳米粒。紫杉醇（PTX）成功地封装在这两个纳米粒子。根据载紫杉醇纳米粒的体外释放研究，在最初的11 h内初始突释后，包封的紫杉醇在随后的82 h内缓慢释放。细胞毒性研究表明，紫杉醇可以通过将紫杉醇封装到PLGA-F127-PLGA纳米粒中来提高其体外抗肿瘤作用。此外，当在叶酸受体过表达的OVCAR-3细胞中递送PTX时，叶酸靶向FA-F127-PLGA纳米颗粒比PLGA-F127-PLGA更有效，这主要是由于FA受体介导的内吞作用。随着治疗时间的延长，靶向作用更加明显。还通过测量纳米颗粒的细胞摄取来研究FA-F127-PLGA纳米颗粒的体外靶向作用。结果表明，FA-F127-PLGA纳米粒比PLGA-F127-PLGA纳米粒更容易被OVCAR-3细胞摄取。体内药代动力学研究表明，FA-F127-PLGA纳米粒延长了PTX在血浆中的循环时间，并延迟了PTX的血液清除。这些结果表明，叶酸FA-F127-PLGA可能是一种潜在的紫杉醇长期给药载体。(C)2017爱思唯尔B.V.保留所有权利。
Novel Folated Pluronic F127/poly (lactic-co-glycolic) (FA-F127-PLGA) and PLGA-F127-PLGA block copolymer were synthesized and nanoparticles self-assembled from these two copolymers were prepared by dialysis method. Paclitaxel (PTX) was successfully encapsulated in these two nanoparticles. According to in vitro release studies of PTX-loaded nanoparticles, after an initial burst release during the first 11 h, the entrapped PTX released slowly in the following 82 h. The cytotoxicity studies demonstrated that the in vitro antitumor effect of PTX could be improved by encapsulating PTX into PLGA-F127-PLGA nanoparticles. Moreover, folate-targeted FA-F127-PLGA nanoparticles were more effective than PLGA-F127-PLGA when delivering PTX in folate receptor overexpressing OVCAR-3 cells, which mainly due to the FA receptor-meditated endocytosis. As the treatment time became longer, the targeting effects were more obvious. The targeting effect of FA-F127-PLGA nanoparticles was also investigated in vitro by measuring the cellular uptake of the nanoparticles. The results showed that FA-F127-PLGA nanoparticles were more easily to be uptaken by OVCAR-3 cells in comparison with PLGA-F127-PLGA nanoparticles. In vivo pharmacokinetic studies indicated that FA-F127-PLGA nanoparticles prolong the circulation time of PTX in plasma, and delay the blood clearance of PTX. These results indicated that Folated FA-F127-PLGA could be a potential carrier in long-term PTX delivery. (C) 2017 Elsevier B.V. All rights reserved.