Carvalheiro Manuela, Jorge João, Eleutério Carla, Pinhal Ana F, Sousa Ana C, Morais José G, Cruz M Eugénia M
Unit of New Forms of Bioactive Agents, National Institute of Engineering Technology and Innovation, Lisbon, Portugal.
Eur J Pharm Biopharm. 2009 Feb;71(2):292-6. doi: 10.1016/j.ejpb.2008.08.001. Epub 2008 Aug 12.
The purpose of this study was to increase the therapeutic index of the antiparasitic drug, trifluralin (TFL), to allow its parenteral administration without the need of toxic solvents. This was achieved by incorporating TFL in liposomes with high loading capacity. These formulations were stable in freeze-dried form during at least one year and in frozen form during at least three months. Therapeutic activity, assessed on a visceral model of infection, showed that TFL liposomes reduced the number of parasites by up to one third or one half as compared to negative control and to free TFL, respectively.
本研究的目的是提高抗寄生虫药物氟乐灵（TFL）的治疗指数，使其无需使用有毒溶剂即可进行肠胃外给药。这是通过将TFL包封于具有高载药量的脂质体中来实现的。这些制剂在冻干形式下至少一年内稳定，在冷冻形式下至少三个月内稳定。在内脏感染模型上评估的治疗活性表明，与阴性对照和游离TFL相比，TFL脂质体分别使寄生虫数量减少多达三分之一或二分之一。
