Banerjee G, Nandi G, Mahato S B, Pakrashi A, Basu M K
Indian Institute of Chemical Biology, Calcutta, India.
J Antimicrob Chemother. 1996 Jul;38(1):145-50. doi: 10.1093/jac/38.1.145.
Different sugar-grafted liposomes were prepared and tested against experimental leishmaniasis in vivo using the classical drug pentamidine isethionate and its methoxy derivative. Both the drugs, when encapsulated in sugar-grafted liposomes were found to be more potent in comparison to normal liposome-encapsulated drug or to the free drug. Moreover, the mannose-grafted liposomes were adjudged to be the best in lowering of spleen parasite load in comparison with those bearing glucose or galactose. When encapsulated in mannose-grafted liposomes the therapeutic efficacy of pentamidine isethionate was found to be better than that of its methoxy derivative, although the latter seemed to be less toxic than the pentamidine isethionate itself.
制备了不同的糖基化脂质体,并使用经典药物喷他脒异硫氰酸盐及其甲氧基衍生物对实验性利什曼病进行了体内测试。当这两种药物封装在糖基化脂质体中时,与正常脂质体封装的药物或游离药物相比,发现它们更有效。此外,与携带葡萄糖或半乳糖的脂质体相比,甘露糖基化脂质体在降低脾脏寄生虫负荷方面被判定为最佳。当喷他脒异硫氰酸盐封装在甘露糖基化脂质体中时,发现其治疗效果优于其甲氧基衍生物,尽管后者似乎比喷他脒异硫氰酸盐本身毒性更小。