Gabriela Muniz Félix Araújo, Gabriela Muniz Félix Araújo, Alana Rafaela Albuquerque Barros, Alana Rafaela Albuquerque Barros, João Augusto Oshiro-Junior, João Augusto Oshiro-Junior, Leonardo Ferreira Soares, Leonardo Ferreira Soares, Louisianny Guerra da Rocha, Louisianny Guerra da Rocha, Ádley Antonini Neves de Lima, Ádley Antonini Neves de Lima, José Alexsandro da Silva, José Alexsandro da Silva, Attilio Converti*, Attilio Converti*, Bolívar Ponciano Goulart de Lima Damasceno and Bolívar Ponciano Goulart de Lima Damasceno Pages 1616 - 1622 ( 7 )
Leishmaniasis is one of the most neglected diseases in the world. Its most severe clinical form, called visceral, if left untreated, can be fatal. Conventional therapy is based on the use of pentavalent antimonials and includes amphotericin B (AmB) as a second-choice drug. The micellar formulation of AmB, although effective, is associated with acute and chronic toxicity. Commercially-available lipid formulations emerged to overcome such drawbacks, but their high cost limits their widespread use. Drug delivery systems such as nanoemulsions (NE) have proven ability to solubilize hydrophobic compounds, improve absorption and bioavailability, increase efficacy and reduce toxicity of encapsulated drugs. NE become even more attractive because they are inexpensive and easy to prepare. The aim of this work was to incorporate AmB in NE prepared by sonicating a mixture of surfactants, Kolliphor® HS15 (KHS15) and Brij® 52, and an oil, isopropyl myristate. NE exhibited neutral pH, conductivity values consistent with oil in water systems, spherical structures with negative Zeta potential value, monomodal size distribution and average diameter of drug-containing droplets ranging from 33 to 132 nm. AmB did not modify the thermal behavior of the system, likely due to its dispersion in the internal phase. Statistically similar antileishmanial activity of AmB-loaded NE to that of AmB micellar formulation suggests further exploring them in terms of toxicity and effectiveness against amastigotes, with the aim of offering an alternative to treat visceral leishmaniasis.
Amphotericin B, new drug delivery system, physicochemical characterization, visceral leishmaniasis, Kolliphor® HS15, Brij® 52.
Laboratory of Development and Characterization of Pharmaceutical Products, Department of Pharmacy, Center for Biological and Health Sciences, State University of Paraíba (UEPB), Campina Grande, PB, Laboratory of Development and Characterization of Pharmaceutical Products, Department of Pharmacy, Center for Biological and Health Sciences, State University of Paraíba (UEPB), Campina Grande, PB, Laboratory of Development and Characterization of Pharmaceutical Products, Department of Pharmacy, Center for Biological and Health Sciences, State University of Paraíba (UEPB), Campina Grande, PB, Laboratory of Development and Characterization of Pharmaceutical Products, Department of Pharmacy, Center for Biological and Health Sciences, State University of Paraíba (UEPB), Campina Grande, PB, Laboratory of Development and Characterization of Pharmaceutical Products, Department of Pharmacy, Center for Biological and Health Sciences, State University of Paraíba (UEPB), Campina Grande, PB, Laboratory of Development and Characterization of Pharmaceutical Products, Department of Pharmacy, Center for Biological and Health Sciences, State University of Paraíba (UEPB), Campina Grande, PB, Laboratory of Development and Characterization of Pharmaceutical Products, Department of Pharmacy, Center for Biological and Health Sciences, State University of Paraíba (UEPB), Campina Grande, PB, Laboratory of Development and Characterization of Pharmaceutical Products, Department of Pharmacy, Center for Biological and Health Sciences, State University of Paraíba (UEPB), Campina Grande, PB, Department of Microbiology and Parasitology, Federal University of Rio Grande do Norte, Natal, RN, Department of Microbiology and Parasitology, Federal University of Rio Grande do Norte, Natal, RN, Department of Pharmacy, Federal University of Rio Grande do Norte, Natal, RN, Department of Pharmacy, Federal University of Rio Grande do Norte, Natal, RN, Laboratory of Development and Characterization of Pharmaceutical Products, Department of Pharmacy, Center for Biological and Health Sciences, State University of Paraíba (UEPB), Campina Grande, PB, Laboratory of Development and Characterization of Pharmaceutical Products, Department of Pharmacy, Center for Biological and Health Sciences, State University of Paraíba (UEPB), Campina Grande, PB, Department of Civil, Chemical and Environmental Engineering, Polytechnic School, University of Genoa, Genoa, Department of Civil, Chemical and Environmental Engineering, Polytechnic School, University of Genoa, Genoa, Laboratory of Development and Characterization of Pharmaceutical Products, Department of Pharmacy, Center for Biological and Health Sciences, State University of Paraíba (UEPB), Campina Grande, PB, Laboratory of Development and Characterization of Pharmaceutical Products, Department of Pharmacy, Center for Biological and Health Sciences, State University of Paraíba (UEPB), Campina Grande, PB