Synthesis and characterization of novel amphiphilic copolymer stearic acid-coupled F127 nanoparticles for nano-technology based drug delivery system

Synthesis and characterization of novel amphiphilic copolymer stearic acid-coupled F127 nanoparticles for nano-technology based drug delivery system
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DOI:
10.1016/j.colsurfb.2011.08.010
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发表时间:
2011-12-01
影响因子:
5.8
通讯作者:
Sun, Baiwang
Sun, Baiwang
中科院分区:
工程技术2区
文献类型:
--
作者:
Gao, Qihe;Liang, Qing;Sun, Baiwang

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Pluronic F127 两亲性嵌段共聚物可用于多种应用,包括药物输送系统。 F127的临界胶束浓度(CMC)约为0.26-0.8wt%,因此F127在基于纳米技术的药物递送系统中的效用受到限制,因为纳米级胶束在稀释时可能解离。在此,硬脂酸(SA)在SA的羧基和F127的羟基之间简单地与F127偶联,形成一种新型共聚物,命名为SA偶联F127,其CMC显着降低。高于 CMC 6.9 x 10(-5) wt%,SA 耦合的 F127 自组装稳定纳米颗粒,Zeta 电位为 -36 mV。制备了负载阿霉素(DOX)的纳米颗粒,载药量(DL)为5.7 wt%,Zeta电位为-36至-39 mV,纳米颗粒表现出独特的形状,尺寸分布为20至50 nm。负载 DOX 的纳米粒子相对稳定,并且在体外对 MCF-7 细胞表现出 DOX 依赖性细胞毒性。这些结果表明 SA 偶联的 F127 有可能用作基于纳米技术的药物输送方法。 (C) 2011 Elsevier B.V. 保留所有权利。
Pluronic, F127, amphiphilic block copolymers, are used for several applications, including drug delivery systems. The critical micelle concentration (CMC) of F127 is about 0.26-0.8 wt% so that the utility of F127 in nano-technology based drug delivery system is limited since the nano-sized micelles could dissociate upon dilution. Herein, stearic acid (SA) was simply coupled to F127 between the carboxyl group of SA and the hydroxyl group of F127, which formed a novel copolymer named as SA-coupled F127, with significantly lower CMC. Above the CMC 6.9 x 10(-5) wt%, SA-coupled F127 self-assembled stable nanoparticles with Zeta potential -36 mV. Doxorubicin (DOX)-loaded nanoparticles were made, with drug loading (DL) 5.7 wt% and Zeta potential -36 to -39 mV, and the nanoparticles exhibited distinct shape with the size distribution from 20 to 50 nm. DOX-loaded nanoparticles were relatively stable and exhibited DOX dependant cytotoxicity toward MCF-7 cells in vitro. These results suggest that SA-coupled F127 potentially could be applied as a nano-technology based drug delivery method. (C) 2011 Elsevier B.V. All rights reserved.