Poloxamer 407 (Pluronic(®) F127)-based polymeric micelles for amphotericin B: In vitro biological activity, toxicity and in vivo therapeutic efficacy against murine tegumentary leishmaniasis.

摘要: In the present study, a Poloxamer 407-based amphotericin B (AmpB)-containing polymeric micelles system (AmpB/M) was employed in treatment of Leishmania amazonensis-infected BALB/c mice. Initially, in vitro antileishmanial activity (IC50 value) AmpB/M and B-AmpB/M (empty micelles) against stationary promastigotes amastigotes-like forms parasites determined, results were 1.83 ± 0.4 22.1 ± 0.7 μM, respectively, for promastigotes, 2.27 ± 0.5 33.98 ± 2.6 μM, amastigotes-like. The cytotoxic concentration (CC50) values these products also evaluated, we found 119.5 ± 9.6 134.7 ± 10.3 μM, respectively. With values, selectivity index (SI) calculated 65.3 5.4, 59.3 3.96, parasites. Free AmpB showed IC50 1.2 ± 0.3 2.5 ± 0.5 μM amastigotes-like, whereas CC50 value 9.5 ± 0.4 μM. SI this drug 7.9 3.8, promastigote amastigote-like stages After, animals infected received saline or treated subcutaneously with free AmpB, B-AmpB/M. results, AmpB-treated mice reductions their body weight, which associated hepatic renal damage; however, no organic alteration observed AmpB/M-treated animals. addition, significant lesion average size parasite burden all evaluated tissue organs, when compared to other groups; as well significantly higher levels IFN-γ, IL-12, GM-CSF nitrite, low production IL-4, IL-10 IgG1 isotype antibodies. conclusion, could be considered an alternative future studies tegumentary leishmaniasis.