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Short Communication

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

    Aline de Souza

    Faculty of Pharmaceutical Sciences, University of São Paulo, São Paulo, SP, 05508-000, Brazil

    ,
    Cauê Benito Scarim

    Department of Drugs & Medicines, School of Pharmaceutical Sciences, São Paulo State University, Araraquara, 14800-901, Brazil

    ,
    Paulo Cesar Cotrim

    Seroepidemiology, Cellular & Molecular Immunology Laboratory, Institute of Tropical Medicine, University of São Paulo, Dr. Enéas de Carvalho Aguiar 470, Jardim América, São Paulo, SP, 05403-000, Brazil

    ,
    Fernando Barbosa Junior

    Laboratory of Toxicology & Essentiality of Metals, Faculty of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, Ribeirão Preto, SP, 14040-903, Brazil

    ,
    Bruno Alves Rocha

    Laboratory of Toxicology & Essentiality of Metals, Faculty of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, Ribeirão Preto, SP, 14040-903, Brazil

    ,
    Leandro Augusto Calixto

    Federal University of São Paulo, Department of Pharmaceutical Sciences, Institute of Environmental, Chemical & Pharmaceutical Sciences, Diadema – SP, 09913-030, Brazil

    ,
    Cristiano Jesus Correia

    Laboratório de Cirurgia Cardiovascular e Fisiopatologia da Circulação (LIM-11), Instituto do Coração (InCor), Faculdade de Medicina da Universidade de São Paulo, São Paulo, 01246-903, Brazil

    ,
    Gabriel Lima de Barros Araújo

    Faculty of Pharmaceutical Sciences, University of São Paulo, São Paulo, SP, 05508-000, Brazil

    ,
    Raimar Löbenberg

    University of Alberta, Faculty of Pharmacy & Pharmaceutical Sciences, Edmonton, AB, T6G 2T9, Canada

    ,
    Nádia Araci Bou-Chacra

    *Author for correspondence: Tel.: +55 113 091 3628;

    E-mail Address: chacra@usp.br

    Faculty of Pharmaceutical Sciences, University of São Paulo, São Paulo, SP, 05508-000, Brazil

    &
    Ana Cristina Breithaupt-Faloppa

    Laboratório de Cirurgia Cardiovascular e Fisiopatologia da Circulação (LIM-11), Instituto do Coração (InCor), Faculdade de Medicina da Universidade de São Paulo, São Paulo, 01246-903, Brazil

    Published Online:https://doi.org/10.2217/nnm-2023-0263

    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.

    Papers of special note have been highlighted as: • of interest; •• of considerable interest

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