Southeast University, School of Chemistry and Chemical Engineering, Nanjing 210000, China.
Colloids Surf B Biointerfaces. 2011 Dec 1;88(2):741-8. doi: 10.1016/j.colsurfb.2011.08.010. Epub 2011 Aug 18.
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 × 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.
Pluronic,F127,两亲性嵌段共聚物,被用于多种应用,包括药物传递系统。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传递系统中的应用受到限制,因为纳米级胶束在稀释时可能会解离。在此,硬脂酸(SA)通过 SA 的羧基和 F127 的羟基简单地偶联到 F127 上,形成了一种新型共聚物,命名为 SA-偶联 F127,其 CMC 显著降低。在 CMC 以上 6.9×10(-5)wt%,SA-偶联 F127 自组装形成稳定的纳米粒子,Zeta 电位为-36mV。载有阿霉素(DOX)的纳米粒子被制备,载药量(DL)为 5.7wt%,Zeta 电位为-36 至-39mV,并且纳米粒子呈现出明显的形状,其尺寸分布在 20 至 50nm 之间。载 DOX 的纳米粒子相对稳定,并表现出对 MCF-7 细胞的 DOX 依赖性细胞毒性。这些结果表明,SA-偶联 F127 有可能被应用于基于纳米技术的药物传递方法。