Hydroxymethylnitrofurazone lymphatic uptake with nanostructured lipid carrier after oral administration in rats.

Nanomedicine (London, England) Pub Date : 2024-02-01 Epub Date: 2024-01-25 DOI:10.2217/nnm-2023-0263

Aline de Souza, Cauê Benito Scarim, Paulo Cesar Cotrim, Fernando Barbosa Junior, Bruno Alves Rocha, Leandro Augusto Calixto, Cristiano Jesus Correia, Gabriel Lima de Barros Araújo, Raimar Löbenberg, Nádia Araci Bou-Chacra, Ana Cristina Breithaupt-Faloppa

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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.

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纳米结构脂质载体在大鼠口服羟甲基硝基呋喃酮后的淋巴吸收。

背景：由原生动物利什曼病引起的利什曼病感染淋巴器官中的吞噬细胞。本研究利用乳糜微粒阻断大鼠流动模型，证明了纳米结构脂质载体负载的羟甲基硝呋酮（NLC-NFOH）对淋巴摄取的影响。方法口服含 NFOH 或 NLC-NFOH 的二甲基亚砜 1 小时后，评估 NFOH 的淋巴摄取量（有无环己亚胺预处理）。结果含 NFOH 的二甲基亚砜和 NLC-NFOH 的 NFOH 血清浓度分别为 0.0316 和 0.0291 μg/ml。阻断乳糜微粒后，未检测到 NFOH。结论尽管对数P低于5，NFOH仍能被淋巴系统成功吸收。长链脂肪酸和颗粒大小可能是导致这些发现的主要因素。NLC-NFOH是通过口服治疗利什曼病的一种前景广阔且方便的平台。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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Nanomedicine (London, England)

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