Development of a biocompatible polymeric chitosan system for the release of compounds with leishmanicidal activity

Leishmaniasis is a tropical disease caused by parasites of the genus Leishmania spp; it presents different clinical manifestations, of which cutaneous leishmaniasis is the most common form, and it is endemic in more than 70 countries worldwide. Only four drugs are registered for the treatment of the...

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Autores principales: Jorge Higuita-Castro, Iván D. Vélez, Diana M. Escobar, Javier Murillo, Tatiana Pineda, Victoria Ospina, Sara M. Robledo
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Publicado: Elsevier 2021
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Acceso en línea:https://doaj.org/article/e3207489cef647789f04466d3db7679c
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spelling oai:doaj.org-article:e3207489cef647789f04466d3db7679c2021-11-12T04:24:42ZDevelopment of a biocompatible polymeric chitosan system for the release of compounds with leishmanicidal activity0264-127510.1016/j.matdes.2021.110232https://doaj.org/article/e3207489cef647789f04466d3db7679c2021-12-01T00:00:00Zhttp://www.sciencedirect.com/science/article/pii/S0264127521007875https://doaj.org/toc/0264-1275Leishmaniasis is a tropical disease caused by parasites of the genus Leishmania spp; it presents different clinical manifestations, of which cutaneous leishmaniasis is the most common form, and it is endemic in more than 70 countries worldwide. Only four drugs are registered for the treatment of the disease, all associated with high toxicity. Recently, the in vitro and in vivo leishmanicidal activity of a mixture of the benzoic acid 2-(2,3-dihydro-4H-1-benzopyran-4-ylidene) hydrazide (TC2) and the compounds present in the plant extract Sapindus saponaria L (SS) were reported. In the present study were prepared soft capsules of chitosan incorporating TC2 and SS in 1:1 (CQ) ratio showed low cytotoxicity in U937 macrophages but moderate cytotoxicity in Detroit 551 fibroblast and had high antileishmanial activity against intracellular L. braziliensis amastigotes. The kinetics of TC2 release from CQ was fitted to the Korsmeyer-Peppas model. Finally, CQ was effective in treating experimental cutaneous leishmaniasis induced in the hamster model. In conclusion, the CQ are biocompatible and can help treat cutaneous leishmaniasis.Jorge Higuita-CastroIván D. VélezDiana M. EscobarJavier MurilloTatiana PinedaVictoria OspinaSara M. RobledoElsevierarticleCutaneous leishmaniasisPlant extractsLeishmanicidal activityDrug release kineticsIn vitro assaysIn vivo studiesMaterials of engineering and construction. Mechanics of materialsTA401-492ENMaterials & Design, Vol 212, Iss , Pp 110232- (2021)
institution DOAJ
collection DOAJ
language EN
topic Cutaneous leishmaniasis
Plant extracts
Leishmanicidal activity
Drug release kinetics
In vitro assays
In vivo studies
Materials of engineering and construction. Mechanics of materials
TA401-492
spellingShingle Cutaneous leishmaniasis
Plant extracts
Leishmanicidal activity
Drug release kinetics
In vitro assays
In vivo studies
Materials of engineering and construction. Mechanics of materials
TA401-492
Jorge Higuita-Castro
Iván D. Vélez
Diana M. Escobar
Javier Murillo
Tatiana Pineda
Victoria Ospina
Sara M. Robledo
Development of a biocompatible polymeric chitosan system for the release of compounds with leishmanicidal activity
description Leishmaniasis is a tropical disease caused by parasites of the genus Leishmania spp; it presents different clinical manifestations, of which cutaneous leishmaniasis is the most common form, and it is endemic in more than 70 countries worldwide. Only four drugs are registered for the treatment of the disease, all associated with high toxicity. Recently, the in vitro and in vivo leishmanicidal activity of a mixture of the benzoic acid 2-(2,3-dihydro-4H-1-benzopyran-4-ylidene) hydrazide (TC2) and the compounds present in the plant extract Sapindus saponaria L (SS) were reported. In the present study were prepared soft capsules of chitosan incorporating TC2 and SS in 1:1 (CQ) ratio showed low cytotoxicity in U937 macrophages but moderate cytotoxicity in Detroit 551 fibroblast and had high antileishmanial activity against intracellular L. braziliensis amastigotes. The kinetics of TC2 release from CQ was fitted to the Korsmeyer-Peppas model. Finally, CQ was effective in treating experimental cutaneous leishmaniasis induced in the hamster model. In conclusion, the CQ are biocompatible and can help treat cutaneous leishmaniasis.
format article
author Jorge Higuita-Castro
Iván D. Vélez
Diana M. Escobar
Javier Murillo
Tatiana Pineda
Victoria Ospina
Sara M. Robledo
author_facet Jorge Higuita-Castro
Iván D. Vélez
Diana M. Escobar
Javier Murillo
Tatiana Pineda
Victoria Ospina
Sara M. Robledo
author_sort Jorge Higuita-Castro
title Development of a biocompatible polymeric chitosan system for the release of compounds with leishmanicidal activity
title_short Development of a biocompatible polymeric chitosan system for the release of compounds with leishmanicidal activity
title_full Development of a biocompatible polymeric chitosan system for the release of compounds with leishmanicidal activity
title_fullStr Development of a biocompatible polymeric chitosan system for the release of compounds with leishmanicidal activity
title_full_unstemmed Development of a biocompatible polymeric chitosan system for the release of compounds with leishmanicidal activity
title_sort development of a biocompatible polymeric chitosan system for the release of compounds with leishmanicidal activity
publisher Elsevier
publishDate 2021
url https://doaj.org/article/e3207489cef647789f04466d3db7679c
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