Amoxicillin and Clarithromycin Mucoadhesive Delivery System for <i>Helicobacter pylori</i> Infection in a Mouse Model: Characterization, Pharmacokinetics, and Efficacy
<i>Helicobacter pylori</i> 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<sup>®</su...
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| Format: | Article |
| Language: | English |
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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/1999-4923/13/2/153 |
| _version_ | 1797407821135872000 |
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| author | Isabel Villegas María Ángeles Rosillo Catalina Alarcón-de-la-Lastra Victoria Vázquez-Román Maria Llorente Susana Sánchez Ana Gloria Gil Pilar Alcalde Esther González Elisabet Rosell Carles Nieto Francisco Fernandez-Campos |
| author_facet | Isabel Villegas María Ángeles Rosillo Catalina Alarcón-de-la-Lastra Victoria Vázquez-Román Maria Llorente Susana Sánchez Ana Gloria Gil Pilar Alcalde Esther González Elisabet Rosell Carles Nieto Francisco Fernandez-Campos |
| author_sort | Isabel Villegas |
| collection | DOAJ |
| description | <i>Helicobacter pylori</i> 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<sup>®</sup>) loaded with amoxicillin and clarithromycin is proposed to improve the efficacy of treatment against <i>H. pylori</i>. 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 <i>H. pylori</i> also demonstrated the superiority of the antibiotics when administered in Mucolast<sup>®</sup>, 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. |
| first_indexed | 2024-03-09T03:47:13Z |
| format | Article |
| id | doaj.art-37c4f9c80166471b96fe02ced44b77d1 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-09T03:47:13Z |
| publishDate | 2021-01-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-37c4f9c80166471b96fe02ced44b77d12023-12-03T14:31:35ZengMDPI AGPharmaceutics1999-49232021-01-0113215310.3390/pharmaceutics13020153Amoxicillin and Clarithromycin Mucoadhesive Delivery System for <i>Helicobacter pylori</i> Infection in a Mouse Model: Characterization, Pharmacokinetics, and EfficacyIsabel Villegas0María Ángeles Rosillo1Catalina Alarcón-de-la-Lastra2Victoria Vázquez-Román3Maria Llorente4Susana Sánchez5Ana Gloria Gil6Pilar Alcalde7Esther González8Elisabet Rosell9Carles Nieto10Francisco Fernandez-Campos11Department of Pharmacology, Faculty of Pharmacy, University of Seville, Profesor García González Street 2, 41012 Seville, SpainDepartment of Pharmacology, Faculty of Pharmacy, University of Seville, Profesor García González Street 2, 41012 Seville, SpainDepartment of Pharmacology, Faculty of Pharmacy, University of Seville, Profesor García González Street 2, 41012 Seville, SpainDepartment of Normal and Pathological Cytology and Histology, Faculty of Medicine, University of Seville, Avda. Dr. Fedriani, s/n, 41009 Sevilla, SpainBionanoplus. Pol. Mocholí Plaza Cein Nº5, nave B14, 31110 Noáin, SpainBionanoplus. Pol. Mocholí Plaza Cein Nº5, nave B14, 31110 Noáin, SpainToxicology Laboratory, DDUNAV Navarra University, Irunlarrea 1, 31008 Pamplona, SpainReig Jofre Laboratories, Avda dels Flors s/n, 08970 Sant Joan Despi, SpainReig Jofre Laboratories, Rio Jarama 111, 45007 Toledo, SpainReig Jofre Laboratories, Avda dels Flors s/n, 08970 Sant Joan Despi, SpainReig Jofre Laboratories, Avda dels Flors s/n, 08970 Sant Joan Despi, SpainReig Jofre Laboratories, Avda dels Flors s/n, 08970 Sant Joan Despi, Spain<i>Helicobacter pylori</i> 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<sup>®</sup>) loaded with amoxicillin and clarithromycin is proposed to improve the efficacy of treatment against <i>H. pylori</i>. 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 <i>H. pylori</i> also demonstrated the superiority of the antibiotics when administered in Mucolast<sup>®</sup>, 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.https://www.mdpi.com/1999-4923/13/2/153<i>Helicobacter pylori</i>mucoadhesiveclarithromycinamoxicillinmicepharmacokinetics |
| spellingShingle | Isabel Villegas María Ángeles Rosillo Catalina Alarcón-de-la-Lastra Victoria Vázquez-Román Maria Llorente Susana Sánchez Ana Gloria Gil Pilar Alcalde Esther González Elisabet Rosell Carles Nieto Francisco Fernandez-Campos Amoxicillin and Clarithromycin Mucoadhesive Delivery System for <i>Helicobacter pylori</i> Infection in a Mouse Model: Characterization, Pharmacokinetics, and Efficacy Pharmaceutics <i>Helicobacter pylori</i> mucoadhesive clarithromycin amoxicillin mice pharmacokinetics |
| title | Amoxicillin and Clarithromycin Mucoadhesive Delivery System for <i>Helicobacter pylori</i> Infection in a Mouse Model: Characterization, Pharmacokinetics, and Efficacy |
| title_full | Amoxicillin and Clarithromycin Mucoadhesive Delivery System for <i>Helicobacter pylori</i> Infection in a Mouse Model: Characterization, Pharmacokinetics, and Efficacy |
| title_fullStr | Amoxicillin and Clarithromycin Mucoadhesive Delivery System for <i>Helicobacter pylori</i> Infection in a Mouse Model: Characterization, Pharmacokinetics, and Efficacy |
| title_full_unstemmed | Amoxicillin and Clarithromycin Mucoadhesive Delivery System for <i>Helicobacter pylori</i> Infection in a Mouse Model: Characterization, Pharmacokinetics, and Efficacy |
| title_short | Amoxicillin and Clarithromycin Mucoadhesive Delivery System for <i>Helicobacter pylori</i> Infection in a Mouse Model: Characterization, Pharmacokinetics, and Efficacy |
| title_sort | amoxicillin and clarithromycin mucoadhesive delivery system for i helicobacter pylori i infection in a mouse model characterization pharmacokinetics and efficacy |
| topic | <i>Helicobacter pylori</i> mucoadhesive clarithromycin amoxicillin mice pharmacokinetics |
| url | https://www.mdpi.com/1999-4923/13/2/153 |
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