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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...
Autores principales: | , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2019
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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. |
format | Online Article Text |
id | pubmed-6920791 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2019 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
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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