Artesunate Dry Emulsion Formulation Combined with Antibiotics for Treatment of <i>Helicobacter pylori</i> Infections: In Vitro/In Vivo Evaluation
<i>Helicobacter pylori</i> is the primary pathogen responsible for causing gastroduodenal ulcers and stomach cancer. The standard treatment for <i>H. pylori</i> typically involves a combination of antibiotics and acid-reducing medications. However, the recurrence of ulcers is...
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| Format: | Article |
| Language: | English |
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MDPI AG
2023-07-01
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| Series: | International Journal of Molecular Sciences |
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| Online Access: | https://www.mdpi.com/1422-0067/24/13/11008 |
| _version_ | 1797591504024240128 |
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| author | Canh Le-Tien Lindsay Blemur Dennis Baltzis |
| author_facet | Canh Le-Tien Lindsay Blemur Dennis Baltzis |
| author_sort | Canh Le-Tien |
| collection | DOAJ |
| description | <i>Helicobacter pylori</i> is the primary pathogen responsible for causing gastroduodenal ulcers and stomach cancer. The standard treatment for <i>H. pylori</i> typically involves a combination of antibiotics and acid-reducing medications. However, the recurrence of ulcers is closely linked to the emergence of antibiotic resistance in <i>H. pylori</i>, necessitating the development of alternative drugs. This report focuses on the investigation of artesunate as a potential alternative to reduce antibiotic use and enhance effectiveness against <i>H. pylori</i>. Unfortunately, commercial artesunate is available in an acid form, which has poor solubility, especially in gastric acid fluid. The aim of this study is to utilize a water-soluble formulation of artesunate called dry emulsion formulation (ADEF) and combine it with amoxicillin to eradicate <i>H. pylori</i>. In vitro studies were conducted to evaluate the activity of ADEF against <i>H. pylori</i> and determine its inhibitory concentrations. In addition, pharmacokinetic parameters of orally administered ADEF and native artesunate were investigated in rats for in vivo studies. The results showed that when combined with amoxicillin and pantoprazole, ADEF exhibited effectiveness against <i>H. pylori</i>. It is worth noting that the solubility of ADEF in gastric acid appears to be a critical factor for achieving successful treatment. Consequently, ADEF could be considered a promising candidate for <i>H. pylori</i> therapy. |
| first_indexed | 2024-03-11T01:39:20Z |
| format | Article |
| id | doaj.art-b754e420c2dc4e6faa1d4d648d46701f |
| institution | Directory Open Access Journal |
| issn | 1661-6596 1422-0067 |
| language | English |
| last_indexed | 2024-03-11T01:39:20Z |
| publishDate | 2023-07-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | International Journal of Molecular Sciences |
| spelling | doaj.art-b754e420c2dc4e6faa1d4d648d46701f2023-11-18T16:46:45ZengMDPI AGInternational Journal of Molecular Sciences1661-65961422-00672023-07-0124131100810.3390/ijms241311008Artesunate Dry Emulsion Formulation Combined with Antibiotics for Treatment of <i>Helicobacter pylori</i> Infections: In Vitro/In Vivo EvaluationCanh Le-Tien0Lindsay Blemur1Dennis Baltzis2Solstar Pharma, Department of Chemistry, 237-43 Boulevard Samson, Laval, QC H7X 3R8, CanadaSolstar Pharma, Department of Chemistry, 237-43 Boulevard Samson, Laval, QC H7X 3R8, CanadaSolstar Pharma, Department of Chemistry, 237-43 Boulevard Samson, Laval, QC H7X 3R8, Canada<i>Helicobacter pylori</i> is the primary pathogen responsible for causing gastroduodenal ulcers and stomach cancer. The standard treatment for <i>H. pylori</i> typically involves a combination of antibiotics and acid-reducing medications. However, the recurrence of ulcers is closely linked to the emergence of antibiotic resistance in <i>H. pylori</i>, necessitating the development of alternative drugs. This report focuses on the investigation of artesunate as a potential alternative to reduce antibiotic use and enhance effectiveness against <i>H. pylori</i>. Unfortunately, commercial artesunate is available in an acid form, which has poor solubility, especially in gastric acid fluid. The aim of this study is to utilize a water-soluble formulation of artesunate called dry emulsion formulation (ADEF) and combine it with amoxicillin to eradicate <i>H. pylori</i>. In vitro studies were conducted to evaluate the activity of ADEF against <i>H. pylori</i> and determine its inhibitory concentrations. In addition, pharmacokinetic parameters of orally administered ADEF and native artesunate were investigated in rats for in vivo studies. The results showed that when combined with amoxicillin and pantoprazole, ADEF exhibited effectiveness against <i>H. pylori</i>. It is worth noting that the solubility of ADEF in gastric acid appears to be a critical factor for achieving successful treatment. Consequently, ADEF could be considered a promising candidate for <i>H. pylori</i> therapy.https://www.mdpi.com/1422-0067/24/13/11008<i>Helicobacter pylori</i>gastroduodenal ulcersstomach cancerantibiotic resistanceartesunateartesunate dry emulsion formulation |
| spellingShingle | Canh Le-Tien Lindsay Blemur Dennis Baltzis Artesunate Dry Emulsion Formulation Combined with Antibiotics for Treatment of <i>Helicobacter pylori</i> Infections: In Vitro/In Vivo Evaluation International Journal of Molecular Sciences <i>Helicobacter pylori</i> gastroduodenal ulcers stomach cancer antibiotic resistance artesunate artesunate dry emulsion formulation |
| title | Artesunate Dry Emulsion Formulation Combined with Antibiotics for Treatment of <i>Helicobacter pylori</i> Infections: In Vitro/In Vivo Evaluation |
| title_full | Artesunate Dry Emulsion Formulation Combined with Antibiotics for Treatment of <i>Helicobacter pylori</i> Infections: In Vitro/In Vivo Evaluation |
| title_fullStr | Artesunate Dry Emulsion Formulation Combined with Antibiotics for Treatment of <i>Helicobacter pylori</i> Infections: In Vitro/In Vivo Evaluation |
| title_full_unstemmed | Artesunate Dry Emulsion Formulation Combined with Antibiotics for Treatment of <i>Helicobacter pylori</i> Infections: In Vitro/In Vivo Evaluation |
| title_short | Artesunate Dry Emulsion Formulation Combined with Antibiotics for Treatment of <i>Helicobacter pylori</i> Infections: In Vitro/In Vivo Evaluation |
| title_sort | artesunate dry emulsion formulation combined with antibiotics for treatment of i helicobacter pylori i infections in vitro in vivo evaluation |
| topic | <i>Helicobacter pylori</i> gastroduodenal ulcers stomach cancer antibiotic resistance artesunate artesunate dry emulsion formulation |
| url | https://www.mdpi.com/1422-0067/24/13/11008 |
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