pH-Dependent Molecular Gate Mesoporous Microparticles for Biological Control of <i>Giardia intestinalis</i>
Giardiasis is a parasitism produced by the protozoa <i>Giardia intestinalis</i> 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 bioavailabilit...
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| Format: | Article |
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MDPI AG
2021-01-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/13/1/94 |
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| author | Isabel González-Alvarez Verónica Vivancos Carmen Coll Bárbara Sánchez-Dengra Elena Aznar Alejandro Ruiz-Picazo Marival Bermejo Félix Sancenón María Auxiliadora Dea-Ayuela Marta Gonzalez-Alvarez Ramón Martínez-Máñez |
| author_facet | Isabel González-Alvarez Verónica Vivancos Carmen Coll Bárbara Sánchez-Dengra Elena Aznar Alejandro Ruiz-Picazo Marival Bermejo Félix Sancenón María Auxiliadora Dea-Ayuela Marta Gonzalez-Alvarez Ramón Martínez-Máñez |
| author_sort | Isabel González-Alvarez |
| collection | DOAJ |
| description | Giardiasis is a parasitism produced by the protozoa <i>Giardia intestinalis</i> 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. |
| first_indexed | 2024-03-09T04:55:10Z |
| format | Article |
| id | doaj.art-854f232ed04946b8826309069ad56fc2 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-09T04:55:10Z |
| publishDate | 2021-01-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-854f232ed04946b8826309069ad56fc22023-12-03T13:06:40ZengMDPI AGPharmaceutics1999-49232021-01-011319410.3390/pharmaceutics13010094pH-Dependent Molecular Gate Mesoporous Microparticles for Biological Control of <i>Giardia intestinalis</i>Isabel González-Alvarez0Verónica Vivancos1Carmen Coll2Bárbara Sánchez-Dengra3Elena Aznar4Alejandro Ruiz-Picazo5Marival Bermejo6Félix Sancenón7María Auxiliadora Dea-Ayuela8Marta Gonzalez-Alvarez9Ramón Martínez-Máñez10Department of Engineering, Pharmacokinetics and Pharmaceutical Technology Area, Miguel Hernandez University, Elche. San Juan Campus, 03550 San Juan, SpainDepartment of Engineering, Pharmacokinetics and Pharmaceutical Technology Area, Miguel Hernandez University, Elche. San Juan Campus, 03550 San Juan, SpainInstituto Interuniversitario de Investigación de Reconocimiento Molecular y Desarrollo Tecnológico, Universitat Politècnica de València and Universitat de València, Camino de Vera s/n, 46022 Valencia, SpainDepartment of Engineering, Pharmacokinetics and Pharmaceutical Technology Area, Miguel Hernandez University, Elche. San Juan Campus, 03550 San Juan, SpainInstituto Interuniversitario de Investigación de Reconocimiento Molecular y Desarrollo Tecnológico, Universitat Politècnica de València and Universitat de València, Camino de Vera s/n, 46022 Valencia, SpainDepartment of Engineering, Pharmacokinetics and Pharmaceutical Technology Area, Miguel Hernandez University, Elche. San Juan Campus, 03550 San Juan, SpainDepartment of Engineering, Pharmacokinetics and Pharmaceutical Technology Area, Miguel Hernandez University, Elche. San Juan Campus, 03550 San Juan, SpainInstituto Interuniversitario de Investigación de Reconocimiento Molecular y Desarrollo Tecnológico, Universitat Politècnica de València and Universitat de València, Camino de Vera s/n, 46022 Valencia, SpainDepartamento de Farmacia, Facultad de Ciencias de la Salud, Universidad Cardenal Herrera-CEU, C/Santiago Ramón y Cajal, s/n, Alfara del Patriarca, 46115 Valencia, SpainDepartment of Engineering, Pharmacokinetics and Pharmaceutical Technology Area, Miguel Hernandez University, Elche. San Juan Campus, 03550 San Juan, SpainInstituto Interuniversitario de Investigación de Reconocimiento Molecular y Desarrollo Tecnológico, Universitat Politècnica de València and Universitat de València, Camino de Vera s/n, 46022 Valencia, SpainGiardiasis is a parasitism produced by the protozoa <i>Giardia intestinalis</i> 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.https://www.mdpi.com/1999-4923/13/1/94mesoporous microparticles<i>G. intestinalis</i>molecular gatetargeted drug deliveryoral administration |
| spellingShingle | Isabel González-Alvarez Verónica Vivancos Carmen Coll Bárbara Sánchez-Dengra Elena Aznar Alejandro Ruiz-Picazo Marival Bermejo Félix Sancenón María Auxiliadora Dea-Ayuela Marta Gonzalez-Alvarez Ramón Martínez-Máñez pH-Dependent Molecular Gate Mesoporous Microparticles for Biological Control of <i>Giardia intestinalis</i> Pharmaceutics mesoporous microparticles <i>G. intestinalis</i> molecular gate targeted drug delivery oral administration |
| title | pH-Dependent Molecular Gate Mesoporous Microparticles for Biological Control of <i>Giardia intestinalis</i> |
| title_full | pH-Dependent Molecular Gate Mesoporous Microparticles for Biological Control of <i>Giardia intestinalis</i> |
| title_fullStr | pH-Dependent Molecular Gate Mesoporous Microparticles for Biological Control of <i>Giardia intestinalis</i> |
| title_full_unstemmed | pH-Dependent Molecular Gate Mesoporous Microparticles for Biological Control of <i>Giardia intestinalis</i> |
| title_short | pH-Dependent Molecular Gate Mesoporous Microparticles for Biological Control of <i>Giardia intestinalis</i> |
| title_sort | ph dependent molecular gate mesoporous microparticles for biological control of i giardia intestinalis i |
| topic | mesoporous microparticles <i>G. intestinalis</i> molecular gate targeted drug delivery oral administration |
| url | https://www.mdpi.com/1999-4923/13/1/94 |
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