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首页> 外文期刊>International Journal of Pharmaceutics >Targeting primaquine into liver using chylomicron emulsions for potential vivax malaria therapy.
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Targeting primaquine into liver using chylomicron emulsions for potential vivax malaria therapy.

机译：使用乳糜微粒乳剂将伯氨喹靶向肝，用于潜在的间日疟疾治疗。

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摘要

Primaquine (PQ) exerts a broad spectrum of activities against various stages of parasitic malaria. It remains as the only drug that destroys late hepatic stages and latent tissue forms of Plasmodium vivax and Plasmodium ovale. However, systems that can target PQ to liver hepatocytes, where malarial sporozoites reside, are needed to minimize the dose-limiting severe toxicities and side-effects caused by PQ. Recently, a reconstituted artificial chylomicron emulsion was generated using commercially available lipids and was shown to be preferentially taken up by liver hepatocytes following intravenous injection. We proposed to target PQ to hepatocytes by incorporating it into this chylomicron emulsion. We have shown that lipophilized PQ can be readily incorporated into the chylomicron emulsion. The PQ remained inside the emulsion without significant release. Moreover, PQ incorporated inside the emulsion was more stable than free PQ when incubated in serum. Finally, when intravenously injected into mice, the PQ-incorporated chylomicron emulsion led to significantly enhanced accumulation of PQ in liver, when compared to the injection of free PQ. This emulsion could be developed into a promising delivery system to target PQ into hepatocytes for vivax malaria therapy.
机译：primaquine（PQ）对各种阶段的寄生虫疟疾都有广泛的活动。它仍然是破坏晚期肝阶段和间日疟原虫和卵形疟原虫潜伏组织形式的唯一药物。但是，需要将PQ靶向疟疾子孢子所在的肝肝细胞的系统，以最大程度地减少剂量限制的严重毒性和由PQ引起的副作用。近来，使用可商购的脂质产生了重构的人造乳糜微粒乳剂，并显示其在静脉内注射后优先被肝肝细胞吸收。我们建议通过将PQ掺入这种乳糜微粒乳剂中来靶向肝细胞。我们已经表明，亲脂化的PQ可以很容易地掺入乳糜微粒乳液中。 PQ保留在乳液内部，没有明显释放。此外，当在血清中孵育时，掺入乳液中的PQ比游离PQ更稳定。最后，与游离PQ注射相比，当将PQ掺入的乳糜微粒乳剂静脉注射到小鼠体内时，可显着增强PQ在肝脏中的蓄积。这种乳剂可以开发成有希望的递送系统，以将PQ靶向肝细胞以治疗间质性疟疾。

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