Drug delivery system: Targeting of pentamidines to specific sites using sugar grafted liposomes

Drug delivery system: Targeting of pentamidines to specific sites using sugar grafted liposomes
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DOI:
10.1093/jac/38.1.145
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发表时间:
1996-07-01
影响因子:
5.2
通讯作者:
Basu, MK
Basu, MK
中科院分区:
医学2区
文献类型:
--
作者:
Banerjee, G;Nandi, G;Basu, MK

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以经典药物羟乙基磺酸喷他脒及其甲氧基衍生物为靶点,制备了不同糖接枝脂质体,并进行了体内抗实验性利什曼病试验。当包封在糖接枝脂质体中时,发现这两种药物与正常脂质体包封的药物或游离药物相比更有效。此外,与葡萄糖或半乳糖脂质体相比,甘露糖接枝脂质体在降低脾脏寄生虫负荷方面被判定为最佳。当包封在甘露糖接枝的脂质体中时,发现羟乙基磺酸喷他脒的治疗效果优于其甲氧基衍生物,尽管后者似乎比羟乙基磺酸喷他脒本身毒性更小。
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 comparision 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.