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Poloxamer 407 (Pluronic® F127)-based polymeric micelles for amphotericin B: In vitro biological activity, toxicity and in vivo therapeutic efficacy against murine tegumentary leishmaniasis by Débora V.C. Mendonça; Letícia M.R. Lage; Daniela P. Lage; Miguel A. Chávez-Fumagalli; Fernanda Ludolf; Bruno M. Roatt; Daniel Menezes-Souza; André A.G. Faraco; Rachel O. Castilho; Carlos A.P. Tavares; José Mário Barichello; Mariana C. Duarte; Eduardo A.F. Coelho is a Medicine article available to read on EtoBox.

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In the present study, a Poloxamer 407-based amphotericin B (AmpB)-containing polymeric micelles system (AmpB/M) was employed in the treatment of Leishmania amazonensis-infected BALB/c mice. Initially, the in vitro antileishmanial activity (IC50 value) of AmpB/M and B-AmpB/M (empty micelles) against stationary promastigotes and amastigotes-like forms of the parasites was determined, and results were of 1.83 ± 0.4 and 22.1 ± 0.7 μM, respectively, for the promastigotes, and of 2.27 ± 0.5 and 33.98 ± 2.6 μM, respectively, for the amastigotes-like. The cytotoxic concentration (CC50) values of these products were also evaluated, and we found the results of 119.5 ± 9.6 and 134.7 ± 10.3 μM, respectively. With these values, the selectivity index (SI) was calculated and results were of 65.3 and 5.4, respectively, for the promastigotes, and of 59.3 and 3.96, respectively, for the amastigotes-like of the parasites. Free AmpB showed IC50 values of 1.2 ± 0.3 and 2.5 ± 0.5 μM for the promastigotes and amastigotes-like, respectively, whereas the CC50 value was of 9.5 ± 0.4 μM. The SI values of this drug were of 7.9 and 3.8, respectively, for the promastigote and amastigote-like stages of the paras

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Author

Débora V.C. Mendonça; Letícia M.R. Lage; Daniela P. Lage; Miguel A. Chávez-Fumagalli; Fernanda Ludolf; Bruno M. Roatt; Daniel Menezes-Souza; André A.G. Faraco; Rachel O. Castilho; Carlos A.P. Tavares; José Mário Barichello; Mariana C. Duarte; Eduardo A.F. Coelho

Publisher

Elsevier BV

Published

2016

Language

EN

Field

Medicine (Health Sciences)