Amoxicillin and Clarithromycin Mucoadhesive Delivery System for Helicobacter pylori Infection in a Mouse Model: Characterization, Pharmacokinetics, and Efficacy

Helicobacter pylori is the main pathogen responsible for gastric ulcers and a predisposing factor of stomach cancer. Although current treatment is usually successful, it requires high doses and frequent administration. An innovative mucoadhesive system (Mucolast®) loaded with amoxicillin and clarith...

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Autores: Villegas Lama, Isabel, Rosillo Ramírez, María de los Ángeles, Alarcón de la Lastra Romero, Catalina, Vázquez Román, María Victoria, Llorente, María, Sánchez, Susana, Fernández Campos, Francisco
Tipo de recurso: artículo
Estado:Versión publicada
Fecha de publicación:2021
País:España
Institución:Universidad de Sevilla (US)
Repositorio:idUS. Depósito de Investigación de la Universidad de Sevilla
OAI Identifier:oai:idus.us.es:11441/104881
Acceso en línea:https://hdl.handle.net/11441/104881
https://doi.org/10.3390/pharmaceutics13020153
Access Level:acceso abierto
Palabra clave:Helicobacter pylori
mucoadhesive
clarithromycin
amoxicillin
mice
pharmacokinetics
Mucolast®
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spelling Amoxicillin and Clarithromycin Mucoadhesive Delivery System for Helicobacter pylori Infection in a Mouse Model: Characterization, Pharmacokinetics, and EfficacyVillegas Lama, IsabelRosillo Ramírez, María de los ÁngelesAlarcón de la Lastra Romero, CatalinaVázquez Román, María VictoriaLlorente, MaríaSánchez, SusanaFernández Campos, FranciscoHelicobacter pylorimucoadhesiveclarithromycinamoxicillinmicepharmacokineticsMucolast®Helicobacter pylori is the main pathogen responsible for gastric ulcers and a predisposing factor of stomach cancer. Although current treatment is usually successful, it requires high doses and frequent administration. An innovative mucoadhesive system (Mucolast®) loaded with amoxicillin and clarithromycin is proposed to improve the efficacy of treatment against H. pylori. The drug product was optimized based on its viscoelastic properties to obtain long-term stability of the vehicle. The drug release mechanisms were different for both antibiotics based on their solubilization status. A systemic and stomach pharmacokinetic profile was obtained after three different doses were administered to mice, obtaining similar systemic exposure levels but an increase in drug concentration in the stomach. The efficacy results in mice infected with H. pylori also demonstrated the superiority of the antibiotics when administered in Mucolast®, as shown by the bacterial count in stomach tissue and under histopathological and biochemical evaluation. The proposed treatment was efficacious and safe and is presented as a realistic alternative to current treatment options to improve patient compliance and to reduce bacterial resistance.Ministerio de Ciencia e Innovación. Gobierno de España (programa RETOS)-RTC-2015-4437-1MDPIFarmacologíaCitología e Histología Normal y PatológicaMinisterio de Ciencia e Innovación (MICIN). España2021info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionapplication/pdfapplication/pdfhttps://hdl.handle.net/11441/104881https://doi.org/10.3390/pharmaceutics13020153reponame:idUS. Depósito de Investigación de la Universidad de Sevillainstname:Universidad de Sevilla (US)InglésPharmaceutics, 13 (2), 153.RTC-2015-4437-1https://doi.org/10.3390/pharmaceutics13020153info:eu-repo/semantics/openAccessoai:idus.us.es:11441/1048812026-06-17T12:51:07Z
dc.title.none.fl_str_mv Amoxicillin and Clarithromycin Mucoadhesive Delivery System for Helicobacter pylori Infection in a Mouse Model: Characterization, Pharmacokinetics, and Efficacy
title Amoxicillin and Clarithromycin Mucoadhesive Delivery System for Helicobacter pylori Infection in a Mouse Model: Characterization, Pharmacokinetics, and Efficacy
spellingShingle Amoxicillin and Clarithromycin Mucoadhesive Delivery System for Helicobacter pylori Infection in a Mouse Model: Characterization, Pharmacokinetics, and Efficacy
Villegas Lama, Isabel
Helicobacter pylori
mucoadhesive
clarithromycin
amoxicillin
mice
pharmacokinetics
Mucolast®
title_short Amoxicillin and Clarithromycin Mucoadhesive Delivery System for Helicobacter pylori Infection in a Mouse Model: Characterization, Pharmacokinetics, and Efficacy
title_full Amoxicillin and Clarithromycin Mucoadhesive Delivery System for Helicobacter pylori Infection in a Mouse Model: Characterization, Pharmacokinetics, and Efficacy
title_fullStr Amoxicillin and Clarithromycin Mucoadhesive Delivery System for Helicobacter pylori Infection in a Mouse Model: Characterization, Pharmacokinetics, and Efficacy
title_full_unstemmed Amoxicillin and Clarithromycin Mucoadhesive Delivery System for Helicobacter pylori Infection in a Mouse Model: Characterization, Pharmacokinetics, and Efficacy
title_sort Amoxicillin and Clarithromycin Mucoadhesive Delivery System for Helicobacter pylori Infection in a Mouse Model: Characterization, Pharmacokinetics, and Efficacy
dc.creator.none.fl_str_mv Villegas Lama, Isabel
Rosillo Ramírez, María de los Ángeles
Alarcón de la Lastra Romero, Catalina
Vázquez Román, María Victoria
Llorente, María
Sánchez, Susana
Fernández Campos, Francisco
author Villegas Lama, Isabel
author_facet Villegas Lama, Isabel
Rosillo Ramírez, María de los Ángeles
Alarcón de la Lastra Romero, Catalina
Vázquez Román, María Victoria
Llorente, María
Sánchez, Susana
Fernández Campos, Francisco
author_role author
author2 Rosillo Ramírez, María de los Ángeles
Alarcón de la Lastra Romero, Catalina
Vázquez Román, María Victoria
Llorente, María
Sánchez, Susana
Fernández Campos, Francisco
author2_role author
author
author
author
author
author
dc.contributor.none.fl_str_mv Farmacología
Citología e Histología Normal y Patológica
Ministerio de Ciencia e Innovación (MICIN). España
dc.subject.none.fl_str_mv Helicobacter pylori
mucoadhesive
clarithromycin
amoxicillin
mice
pharmacokinetics
Mucolast®
topic Helicobacter pylori
mucoadhesive
clarithromycin
amoxicillin
mice
pharmacokinetics
Mucolast®
description Helicobacter pylori is the main pathogen responsible for gastric ulcers and a predisposing factor of stomach cancer. Although current treatment is usually successful, it requires high doses and frequent administration. An innovative mucoadhesive system (Mucolast®) loaded with amoxicillin and clarithromycin is proposed to improve the efficacy of treatment against H. pylori. The drug product was optimized based on its viscoelastic properties to obtain long-term stability of the vehicle. The drug release mechanisms were different for both antibiotics based on their solubilization status. A systemic and stomach pharmacokinetic profile was obtained after three different doses were administered to mice, obtaining similar systemic exposure levels but an increase in drug concentration in the stomach. The efficacy results in mice infected with H. pylori also demonstrated the superiority of the antibiotics when administered in Mucolast®, as shown by the bacterial count in stomach tissue and under histopathological and biochemical evaluation. The proposed treatment was efficacious and safe and is presented as a realistic alternative to current treatment options to improve patient compliance and to reduce bacterial resistance.
publishDate 2021
dc.date.none.fl_str_mv 2021
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
format article
status_str publishedVersion
dc.identifier.none.fl_str_mv https://hdl.handle.net/11441/104881
https://doi.org/10.3390/pharmaceutics13020153
url https://hdl.handle.net/11441/104881
https://doi.org/10.3390/pharmaceutics13020153
dc.language.none.fl_str_mv Inglés
language_invalid_str_mv Inglés
dc.relation.none.fl_str_mv Pharmaceutics, 13 (2), 153.
RTC-2015-4437-1
https://doi.org/10.3390/pharmaceutics13020153
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
application/pdf
dc.publisher.none.fl_str_mv MDPI
publisher.none.fl_str_mv MDPI
dc.source.none.fl_str_mv reponame:idUS. Depósito de Investigación de la Universidad de Sevilla
instname:Universidad de Sevilla (US)
instname_str Universidad de Sevilla (US)
reponame_str idUS. Depósito de Investigación de la Universidad de Sevilla
collection idUS. Depósito de Investigación de la Universidad de Sevilla
repository.name.fl_str_mv
repository.mail.fl_str_mv
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