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Development and Characterization of a Semi-Solid Dosage Form of Meglumine Antimoniate for Topical Treatment of Cutaneous Leishmaniasis

Cutaneous leishmaniasis (CL) is treated with painful intralesional injections of meglumine antimoniate (MA). With the aim of developing an alternative topical treatment for CL, a gel-based formulation with 30% MA was prepared and its physicochemical properties, stability and rheological behavior wer...

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Autores principales: Berenguer, Diana, Sosa, Lilian, Alcover, Magdalena, Sessa, Marcella, Halbaut, Lyda, Guillén, Carme, Fisa, Roser, Calpena-Campmany, Ana Cristina, Riera, Cristina
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6920791/
https://www.ncbi.nlm.nih.gov/pubmed/31731660
http://dx.doi.org/10.3390/pharmaceutics11110613
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author Berenguer, Diana
Sosa, Lilian
Alcover, Magdalena
Sessa, Marcella
Halbaut, Lyda
Guillén, Carme
Fisa, Roser
Calpena-Campmany, Ana Cristina
Riera, Cristina
author_facet Berenguer, Diana
Sosa, Lilian
Alcover, Magdalena
Sessa, Marcella
Halbaut, Lyda
Guillén, Carme
Fisa, Roser
Calpena-Campmany, Ana Cristina
Riera, Cristina
author_sort Berenguer, Diana
collection PubMed
description Cutaneous leishmaniasis (CL) is treated with painful intralesional injections of meglumine antimoniate (MA). With the aim of developing an alternative topical treatment for CL, a gel-based formulation with 30% MA was prepared and its physicochemical properties, stability and rheological behavior were studied. The following were assessed: drug release on propylene hydrophilic membranes ex vivo human skin permeation, tolerance in healthy volunteers, cytotoxicity in three cell lines and anti-leishmanial activity against Leishmania infantum promastigotes and amastigotes. The MA gel formulation was found to have suitable pH, and good spreadability and stability. Low quantities of pentavalent antimony (Sb(V)) were observed in release and permeation tests, whereas retention was high in both non-damaged and damaged skin (71,043.69 ± 10,641.57 and 10,728 ± 2254.61 µg/g/cm(2) of Sb(V), respectively). The formulation did not have a toxic effect on the cell lines, and presented lower Sb(V) IC(50) values against amastigotes (15.76 ± 4.81 µg/mL) in comparison with the MA solution. The high amount of drug retained in the skin and the Sb(V) IC(50) values obtained suggest that this semi-solid dosage form has potential as an alternative treatment of CL.
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spelling pubmed-69207912019-12-24 Development and Characterization of a Semi-Solid Dosage Form of Meglumine Antimoniate for Topical Treatment of Cutaneous Leishmaniasis Berenguer, Diana Sosa, Lilian Alcover, Magdalena Sessa, Marcella Halbaut, Lyda Guillén, Carme Fisa, Roser Calpena-Campmany, Ana Cristina Riera, Cristina Pharmaceutics Article Cutaneous leishmaniasis (CL) is treated with painful intralesional injections of meglumine antimoniate (MA). With the aim of developing an alternative topical treatment for CL, a gel-based formulation with 30% MA was prepared and its physicochemical properties, stability and rheological behavior were studied. The following were assessed: drug release on propylene hydrophilic membranes ex vivo human skin permeation, tolerance in healthy volunteers, cytotoxicity in three cell lines and anti-leishmanial activity against Leishmania infantum promastigotes and amastigotes. The MA gel formulation was found to have suitable pH, and good spreadability and stability. Low quantities of pentavalent antimony (Sb(V)) were observed in release and permeation tests, whereas retention was high in both non-damaged and damaged skin (71,043.69 ± 10,641.57 and 10,728 ± 2254.61 µg/g/cm(2) of Sb(V), respectively). The formulation did not have a toxic effect on the cell lines, and presented lower Sb(V) IC(50) values against amastigotes (15.76 ± 4.81 µg/mL) in comparison with the MA solution. The high amount of drug retained in the skin and the Sb(V) IC(50) values obtained suggest that this semi-solid dosage form has potential as an alternative treatment of CL. MDPI 2019-11-15 /pmc/articles/PMC6920791/ /pubmed/31731660 http://dx.doi.org/10.3390/pharmaceutics11110613 Text en © 2019 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Berenguer, Diana
Sosa, Lilian
Alcover, Magdalena
Sessa, Marcella
Halbaut, Lyda
Guillén, Carme
Fisa, Roser
Calpena-Campmany, Ana Cristina
Riera, Cristina
Development and Characterization of a Semi-Solid Dosage Form of Meglumine Antimoniate for Topical Treatment of Cutaneous Leishmaniasis
title Development and Characterization of a Semi-Solid Dosage Form of Meglumine Antimoniate for Topical Treatment of Cutaneous Leishmaniasis
title_full Development and Characterization of a Semi-Solid Dosage Form of Meglumine Antimoniate for Topical Treatment of Cutaneous Leishmaniasis
title_fullStr Development and Characterization of a Semi-Solid Dosage Form of Meglumine Antimoniate for Topical Treatment of Cutaneous Leishmaniasis
title_full_unstemmed Development and Characterization of a Semi-Solid Dosage Form of Meglumine Antimoniate for Topical Treatment of Cutaneous Leishmaniasis
title_short Development and Characterization of a Semi-Solid Dosage Form of Meglumine Antimoniate for Topical Treatment of Cutaneous Leishmaniasis
title_sort development and characterization of a semi-solid dosage form of meglumine antimoniate for topical treatment of cutaneous leishmaniasis
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6920791/
https://www.ncbi.nlm.nih.gov/pubmed/31731660
http://dx.doi.org/10.3390/pharmaceutics11110613
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