Hydroxymethylnitrofurazone Lymphatic Uptake with Nanostructured Lipid Carrier After Oral Administration in Rats

• DOI: 10.2217/nnm-2023-0263
• Publication Date: 2024-01-25T13:29:48Z
• Authors: Aline de Souza; Cauê Benito Scarim; Paulo Cesar Cotrim; Fernando Barbosa ...; Bruno Alves Rocha; Leandro Augusto C...; Cristiano Jesus C...; Gabriel Lima de B...; Raimar Löbenberg; Nádia Araci Bou-C...; Ana Cristina Brei...
• Keywords: Drug Carriers; Nitrofurazone; Chylomicrons; Animals; Administration, Oral; Dimethyl Sulfoxide; Particle Size; Leishmaniasis; Rats; Nanostructures

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.