Department of Pharmaceutics and Pharmaceutical Technology, School of Pharmacy, University of Navarra, E-31080 Pamplona, Spain.
Cancer Lett. 2013 Jul 1;334(2):302-10. doi: 10.1016/j.canlet.2013.01.018. Epub 2013 Jan 23.
Although current therapies have improved leukemia survival rates, adverse drug effects and relapse are frequent. Encapsulation of edelfosine (ET) in lipid nanoparticles (LNs) improves its oral bioavailability and decreases its toxicity. Here we evaluated the efficacy of ET-LN in myeloid leukemia cell lines. Drug-loaded LN were as effective as free ET in sensitive leukemia cell lines. Moreover, the encapsulated drug overcame the resistance of the K562 cell line to the drug. LN containing ET might be used as a promising drug delivery system in leukemia due to their capacity to overcome the in vivo pitfalls of the free drug and their efficacy in vitro in leukemia cell lines.
尽管目前的治疗方法已经提高了白血病的存活率，但药物的不良反应和复发仍然很常见。将埃德尔福辛（ET）包封在脂质纳米粒（LN）中可以提高其口服生物利用度并降低其毒性。在这里，我们评估了 ET-LN 在髓系白血病细胞系中的疗效。载药 LN 与游离 ET 一样对敏感白血病细胞系有效。此外，包裹的药物克服了 K562 细胞系对药物的耐药性。由于 LN 能够克服游离药物的体内缺陷，并且在白血病细胞系中具有体外疗效，因此含有 ET 的 LN 可能成为治疗白血病的一种有前途的药物递送系统。
