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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"
Authors : González Álvarez, Isabel
Vivancos Gómez, Verónica
Coll Merino, Carmen
Sánchez Dengra, Bárbara
Aznar Gimeno, Elena
Ruiz Picazo, Alejandro
Dea Ayuela, María Auxiliadora
Keywords: Lambliasis - Farmacoterapia.Giardiasis - Treatment.Intestino delgado - Parásitos.Lambliasis - Tratamiento.Medicamentos - Administración.Drugs - Administration.Giardiasis - Chemotherapy.Intestine, Small - Parasites.
Publisher: MDPI
Citation: González-Alvarez, I., Vivancos, V., Coll, C., Sánchez-Dengra, B., Aznar, E., Ruiz-Picazo, A., Bermejo, M., Sancenón, F., Dea-Ayuela, M.A., Gonzalez-Alvarez, M. & Martínez-Máñez, R. (2021). PH-dependent molecular gate mesoporous microparticles for biological control of "Giardia intestinalis". Pharmaceutics, vol. 13, i. 1 (13 jan.), art. 94. DOI:
Abstract: 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.
Description: Este artículo se encuentra disponible en la siguiente URL:
En este artículo de investigación también participan: Marival Bermejo, Félix Sancenón, Marta Gonzalez-Alvarez y Ramón Martínez-Máñez.
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ISSN: 1999-4923 (Electrónico)
Issue Date: 13-Jan-2021
Center : Universidad Cardenal Herrera-CEU
Appears in Collections:Dpto. Farmacia

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