کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
9918608 | 1557550 | 2005 | 10 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Targeting primaquine into liver using chylomicron emulsions for potential vivax malaria therapy
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کلمات کلیدی
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
علوم دارویی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
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.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: International Journal of Pharmaceutics - Volume 303, Issues 1â2, 13 October 2005, Pages 143-152
Journal: International Journal of Pharmaceutics - Volume 303, Issues 1â2, 13 October 2005, Pages 143-152
نویسندگان
Annie M. Dierling, Zhengrong Cui,