Williams D M, Carter K C, Baillie A J
Department of Immunology, University of Strathclyde, Glasgow.
J Drug Target. 1995;3(1):1-7. doi: 10.3109/10611869509015926.
Five non-ionic surfactants (Surfactants V-IX) were screened for their ability to produce vesicles for the delivery of sodium stibogluconate. Mean vesicle diameter and antimony content were determined prior to in vivo assessment of antiparasitic activity in a mouse model of acute visceral leishmaniasis. V/D suspensions (i.e. stibogluconate loaded vesicles kept in the hydrating drug solution) were more effective against spleen, liver and bone marrow parasites than drug loaded vesicle suspensions that had unentrapped drug removed. A Surfactant IX V/D suspension was the most active antileishmanial preparation causing 74 +/- 10%, 99 +/- 1% and 38 +/- 8% suppression of liver, spleen and bone marrow parasite burdens respectively. Contrary to previous findings, a reduction in splenic and bone marrow parasite burdens was achieved using large vesicles (mean diameter > 800nm). The significance of these results is discussed.
筛选了五种非离子表面活性剂（表面活性剂V-IX），以评估它们产生用于递送葡萄糖酸锑钠的囊泡的能力。在急性内脏利什曼病小鼠模型中进行体内抗寄生虫活性评估之前，测定了平均囊泡直径和锑含量。与去除了未包封药物的载药囊泡悬浮液相比，V/D悬浮液（即保存在水合药物溶液中的载葡萄糖酸锑钠囊泡）对脾脏、肝脏和骨髓寄生虫更有效。表面活性剂IX V/D悬浮液是最具活性的抗利什曼制剂，分别使肝脏、脾脏和骨髓中的寄生虫负荷抑制74±10%、99±1%和38±8%。与之前的研究结果相反，使用大囊泡（平均直径>800nm）可降低脾脏和骨髓中的寄生虫负荷。讨论了这些结果的意义。
