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pH-Dependent Molecular Gate Mesoporous Microparticles for Biological Control of Giardia intestinalis

Giardiasis is a parasitism produced by the protozoa Giardia intestinalis that lives as trophozoite in the small intestine (mainly in the duodenum) attached to the intestinal villus by means of billed discs. The first line treatment is metronidazole, a drug with high bioavailability, which is why to...

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Autores principales: González-Alvarez, Isabel, Vivancos, Verónica, Coll, Carmen, Sánchez-Dengra, Bárbara, Aznar, Elena, Ruiz-Picazo, Alejandro, Bermejo, Marival, Sancenón, Félix, Dea-Ayuela, María Auxiliadora, Gonzalez-Alvarez, Marta, Martínez-Máñez, Ramón
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7828499/
https://www.ncbi.nlm.nih.gov/pubmed/33451061
http://dx.doi.org/10.3390/pharmaceutics13010094
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author González-Alvarez, Isabel
Vivancos, Verónica
Coll, Carmen
Sánchez-Dengra, Bárbara
Aznar, Elena
Ruiz-Picazo, Alejandro
Bermejo, Marival
Sancenón, Félix
Dea-Ayuela, María Auxiliadora
Gonzalez-Alvarez, Marta
Martínez-Máñez, Ramón
author_facet González-Alvarez, Isabel
Vivancos, Verónica
Coll, Carmen
Sánchez-Dengra, Bárbara
Aznar, Elena
Ruiz-Picazo, Alejandro
Bermejo, Marival
Sancenón, Félix
Dea-Ayuela, María Auxiliadora
Gonzalez-Alvarez, Marta
Martínez-Máñez, Ramón
author_sort González-Alvarez, Isabel
collection PubMed
description Giardiasis is a parasitism produced by the protozoa Giardia intestinalis that lives as trophozoite in the small intestine (mainly in the duodenum) attached to the intestinal villus by means of billed discs. The first line treatment is metronidazole, a drug with high bioavailability, which is why to obtain therapeutic concentrations in duodenum, it is necessary to administer high doses of drug to patients with the consequent occurrence of side effects. It is necessary to developed new therapeutical approaches to achieve a local delivery of the drug. In this sense, we have developed gated mesoporous silica microparticles loaded with metronidazole and with a molecular gate pH dependent. In vitro assays demonstrated that the metronidazole release is practically insignificant at acidic pHs, but in duodenum conditions, the metronidazole delivery from the microparticles is effective enough to produce an important parasite destruction. In vivo assays indicate that this microparticulate system allows to increase the concentration of the drug in duodenum and reduce the concentration in plasma avoiding systemic effects. This system could be useful for other intestinal local treatments in order to reduce doses and increase drug availability in target tissues.
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spelling pubmed-78284992021-01-25 pH-Dependent Molecular Gate Mesoporous Microparticles for Biological Control of Giardia intestinalis González-Alvarez, Isabel Vivancos, Verónica Coll, Carmen Sánchez-Dengra, Bárbara Aznar, Elena Ruiz-Picazo, Alejandro Bermejo, Marival Sancenón, Félix Dea-Ayuela, María Auxiliadora Gonzalez-Alvarez, Marta Martínez-Máñez, Ramón Pharmaceutics Article Giardiasis is a parasitism produced by the protozoa Giardia intestinalis that lives as trophozoite in the small intestine (mainly in the duodenum) attached to the intestinal villus by means of billed discs. The first line treatment is metronidazole, a drug with high bioavailability, which is why to obtain therapeutic concentrations in duodenum, it is necessary to administer high doses of drug to patients with the consequent occurrence of side effects. It is necessary to developed new therapeutical approaches to achieve a local delivery of the drug. In this sense, we have developed gated mesoporous silica microparticles loaded with metronidazole and with a molecular gate pH dependent. In vitro assays demonstrated that the metronidazole release is practically insignificant at acidic pHs, but in duodenum conditions, the metronidazole delivery from the microparticles is effective enough to produce an important parasite destruction. In vivo assays indicate that this microparticulate system allows to increase the concentration of the drug in duodenum and reduce the concentration in plasma avoiding systemic effects. This system could be useful for other intestinal local treatments in order to reduce doses and increase drug availability in target tissues. MDPI 2021-01-13 /pmc/articles/PMC7828499/ /pubmed/33451061 http://dx.doi.org/10.3390/pharmaceutics13010094 Text en © 2021 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
González-Alvarez, Isabel
Vivancos, Verónica
Coll, Carmen
Sánchez-Dengra, Bárbara
Aznar, Elena
Ruiz-Picazo, Alejandro
Bermejo, Marival
Sancenón, Félix
Dea-Ayuela, María Auxiliadora
Gonzalez-Alvarez, Marta
Martínez-Máñez, Ramón
pH-Dependent Molecular Gate Mesoporous Microparticles for Biological Control of Giardia intestinalis
title pH-Dependent Molecular Gate Mesoporous Microparticles for Biological Control of Giardia intestinalis
title_full pH-Dependent Molecular Gate Mesoporous Microparticles for Biological Control of Giardia intestinalis
title_fullStr pH-Dependent Molecular Gate Mesoporous Microparticles for Biological Control of Giardia intestinalis
title_full_unstemmed pH-Dependent Molecular Gate Mesoporous Microparticles for Biological Control of Giardia intestinalis
title_short pH-Dependent Molecular Gate Mesoporous Microparticles for Biological Control of Giardia intestinalis
title_sort ph-dependent molecular gate mesoporous microparticles for biological control of giardia intestinalis
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7828499/
https://www.ncbi.nlm.nih.gov/pubmed/33451061
http://dx.doi.org/10.3390/pharmaceutics13010094
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