Abstract：
Background: Leishmaniasis, caused by the protozoan Leishmania sp., infects phagocyte cells present in lymphatic organs. This study demonstrates the influence of nanostructured lipid carrier-loaded hydroxymethylnitrofurazone (NLC-NFOH) on lymphatic uptake using a chylomicron-blocking flow model in rats. Method: Lymphatic uptake of NFOH was assessed 1 h after oral administration of dimethyl sulfoxide with NFOH or NLC-NFOH with and without cycloheximide pretreatment. Result: Dimethyl sulfoxide with NFOH and NLC-NFOH showed NFOH serum concentrations of 0.0316 and 0.0291 μg/ml, respectively. After chylomicron blocking, NFOH was not detected. Conclusion: Despite log P below 5, NFOH was successfully taken up by the lymphatic system. Long-chain fatty acids and particle size might be main factors in these findings. NLC-NFOH is a promising and convenient platform for treating leishmaniasis via oral administration.
摘要：
背景：利什曼病，由原生动物利什曼原虫引起。,感染淋巴器官中存在的吞噬细胞。这项研究证明了使用乳糜微粒阻塞流模型在大鼠中装载纳米结构脂质载体的羟甲基硝基呋喃酮（NLC-NFOH）对淋巴摄取的影响。方法：在口服二甲亚砜和NFOH或NLC-NFOH后1小时，在有和没有环己酰亚胺预处理的情况下评估NFOH的淋巴吸收。结果:二甲基亚砜与NFOH和NLC-NFOH显示NFOH血清浓度为0.0316和0.0291μg/ml,分别。乳糜微粒阻断后，未检测到NFOH。结论：尽管logP低于5，但NFOH已被淋巴系统成功吸收。长链脂肪酸和粒径可能是这些发现的主要因素。NLC-NFOH是通过口服给药治疗利什曼病的有前途且方便的平台。
