In Vitro Efficacy and Toxicity Assessment of an Amphotericin B Gel for the Treatment of Cutaneous Leishmaniasis
<b>Background/Objectives</b>: Leishmaniasis is a neglected tropical disease caused by a protozoan parasite of <i>Leishmania</i>. This study aimed to evaluate the in vitro efficacy and toxicity of a previously developed amphotericin gel as a possible treatment for cutaneous le...
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| Main Authors: | , , , , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2025-03-01
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| Series: | Pharmaceuticals |
| Subjects: | |
| Online Access: | https://www.mdpi.com/1424-8247/18/3/427 |
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| Summary: | <b>Background/Objectives</b>: Leishmaniasis is a neglected tropical disease caused by a protozoan parasite of <i>Leishmania</i>. This study aimed to evaluate the in vitro efficacy and toxicity of a previously developed amphotericin gel as a possible treatment for cutaneous leishmaniasis. <b>Methods</b>: First, quality control of the AmB-gel was carried out, including microbiological stability. The permeated and retained drug was tested on healthy and lacerated human skin. Tolerance to the AmB-gel was tested in vitro using HaCaT, RAW 264.7, and J774 cell lines and by an irritation test (HET-CAM). Promastigotes and amastigotes of various <i>Leishmania</i> species were tested, and the microscopic morphology of promastigotes exposed to the formulation was analyzed. Computational analysis was performed on the drug, polymer, and ergosterol in the promastigote. <b>Results</b>: The AmB-gel presented appropriate characteristics for topical use, including no microbial contamination after storage. The amount of drug retained on the intact and injured skin was 1180.00 ± 13.54 µg/g/cm<sup>2</sup> and 750.18 ± 5.43 µg/g/cm<sup>2</sup>, respectively. The AmB-gel did not cause significant signs of toxicity. The IC<sub>50</sub> of the AmB-gel for promastigotes was less than 1 µg/mL for the four species examined, i.e., <i>Leishmania infantum</i>, <i>Leishmania tropica</i>, <i>Leishmania major</i>, and <i>Leishmania braziliensis</i>, and less than 2 µg/mL for amastigotes of <i>Leishmania infantum</i> and <i>Leishmania tropica</i>. The AmB-gel caused notable effects on the surface of promastigotes. Computational analysis revealed primarily hydrophobic and van der Waals interactions between AmB and Pluronic<sup>®</sup> F127 and ergosterol. <b>Conclusions</b>: Based on the drug retention content and IC<sub>50</sub> values observed for both parasite stages, the AmB-gel may be a promising candidate for in vivo studies in patients with cutaneous leishmaniasis. |
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| ISSN: | 1424-8247 |