Gabriela Muniz Félix Araújo
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Gabriela Muniz Félix Araújo
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Alana Rafaela Albuquerque Barros
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Alana Rafaela Albuquerque Barros
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João Augusto Oshiro-Junior
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...
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.
Biorelevant dissolution of candesartan cilexetil
