J Biomed Nanotechnol. 2014 Apr;10(4):580-91. doi: 10.1166/jbn.2014.1746.
Fisetin (3,3',4',7-tetrahydroxyflavone) is a potential anti-tumor agent but poor water solubility hinders its application and complicates direct parenteral administration. Nanoparticle encapsulation is an efficient way to enhance the solubility of some hydrophobic drugs. In this study, methoxy poly(ethylene glycol)-polycaprolactone (MPEG-PCL) nanoparticles were successfully prepared for fisetin delivery in vitro and in vivo. Narrow distribution fisetin-loaded MPEG-PCL NPs (aproximately100 nm) were obtained via emulsification (O/W) and displayed a sustained release behavior in vitro. Moreover, hemolysis and cell cytotoxicity testing showed that MPEG-PCL is biocompatible and safe for intravenous injection. Most importantly, NPs encapsulation enhanced the anti-cancer activity of fisetin as shown in a subcutaneous LL/2 tumor model, and reduced the hepatotoxicity of fisetin. Therefore, our data demonstrate that fisetin-loaded MPEG-PCL NPs have potential application in cancer chemotherapy.
藤黄酚（3,3',4',7-四羟基黄酮）是一种有潜力的抗肿瘤药物，但较差的水溶性阻碍了其应用，也使其难以直接进行肠胃外给药。纳米颗粒包封是提高一些疏水性药物溶解度的有效方法。在这项研究中，成功制备了甲氧基聚乙二醇-聚己内酯（MPEG-PCL）纳米颗粒，用于藤黄酚的体内外递送。通过乳化（O/W）获得了窄分布的藤黄酚负载 MPEG-PCL NPs（约 100nm），并表现出体外的持续释放行为。此外，溶血和细胞毒性试验表明 MPEG-PCL 具有良好的生物相容性，可安全用于静脉注射。最重要的是，纳米颗粒包封增强了藤黄酚的抗癌活性，如在皮下 LL/2 肿瘤模型中所示，并降低了藤黄酚的肝毒性。因此，我们的数据表明，藤黄酚负载的 MPEG-PCL NPs 在癌症化疗中有潜在的应用。
