Nanoparticles of Thiolated Xanthan Gum for the Oral Delivery of Miconazole Nitrate: In Vitro and In Vivo Evaluation
The objective of this research was to develop a mucoadhesive delivery system that improves permeation for the administration of poorly absorbed oral medications. Thiolation of xanthan gum (XGM) was carried out by esterification with mercaptobutyric acid. Fourier-transformed infrared spectroscopy was...
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MDPI AG
2024-02-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/16/2/225 |
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| author | Nader I. Namazi Hamad Alrbyawi Abdulkareem Ali Alanezi Afaf F Almuqati Anwar Shams Hany S. M. Ali |
| author_facet | Nader I. Namazi Hamad Alrbyawi Abdulkareem Ali Alanezi Afaf F Almuqati Anwar Shams Hany S. M. Ali |
| author_sort | Nader I. Namazi |
| collection | DOAJ |
| description | The objective of this research was to develop a mucoadhesive delivery system that improves permeation for the administration of poorly absorbed oral medications. Thiolation of xanthan gum (XGM) was carried out by esterification with mercaptobutyric acid. Fourier-transformed infrared spectroscopy was used to confirm thiol-derivatization. Using Ellman’s technique, it was revealed that the xanthan-mercaptobutyric acid conjugate had 4.7 mM of thiol groups in 2 mg/mL of polymeric solution. Using mucosa of sheep intestine, the mucoadhesive properties of XGM and thiolated xanthan gum (TXGM) nanoparticles were investigated and we found that TXGM had a longer bioadhesion time than XGM. The disulfide link that forms between mucus and thiolated XGM explains why it has better mucoadhesive properties than XGM. A study on in vitro miconazole (MCZ) release using phosphate buffer (pH 6.8) found that TXGM nanoparticles released MCZ more steadily than MCZ dispersion did. A 1-fold increase in the permeation of MCZ was observed from nanoparticles using albino rat intestine compared to MCZ. Albino rats were used to test the pharmacokinetics of MCZ, and the results showed a 4.5-fold increase in bioavailability. In conclusion, the thiolation of XGM enhances its bioavailability, controlled release of MCZ for a long period of time, and mucoadhesive activity. |
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| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-07T22:17:54Z |
| publishDate | 2024-02-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-6a539e5632b64006ad025f77848d63b12024-02-23T15:31:09ZengMDPI AGPharmaceutics1999-49232024-02-0116222510.3390/pharmaceutics16020225Nanoparticles of Thiolated Xanthan Gum for the Oral Delivery of Miconazole Nitrate: In Vitro and In Vivo EvaluationNader I. Namazi0Hamad Alrbyawi1Abdulkareem Ali Alanezi2Afaf F Almuqati3Anwar Shams4Hany S. M. Ali5Department of Pharmaceutics and Pharmaceutical Industries, College of Pharmacy, Taibah University, Madinah 41477, Saudi ArabiaDepartment of Pharmaceutics and Pharmaceutical Industries, College of Pharmacy, Taibah University, Madinah 41477, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, University of Hafr Al-Batin, Hafr Al-Batin 31991, Saudi ArabiaDepartment of Pharmaceutical Chemistry, College of Pharmacy, University of Hafr Al-Batin, Hafr Al-Batin 31991, Saudi ArabiaDepartment of Pharmacology, College of Medicine, Taif University, Taif 21944, Saudi ArabiaDepartment of Pharmaceutics and Pharmaceutical Industries, College of Pharmacy, Taibah University, Madinah 41477, Saudi ArabiaThe objective of this research was to develop a mucoadhesive delivery system that improves permeation for the administration of poorly absorbed oral medications. Thiolation of xanthan gum (XGM) was carried out by esterification with mercaptobutyric acid. Fourier-transformed infrared spectroscopy was used to confirm thiol-derivatization. Using Ellman’s technique, it was revealed that the xanthan-mercaptobutyric acid conjugate had 4.7 mM of thiol groups in 2 mg/mL of polymeric solution. Using mucosa of sheep intestine, the mucoadhesive properties of XGM and thiolated xanthan gum (TXGM) nanoparticles were investigated and we found that TXGM had a longer bioadhesion time than XGM. The disulfide link that forms between mucus and thiolated XGM explains why it has better mucoadhesive properties than XGM. A study on in vitro miconazole (MCZ) release using phosphate buffer (pH 6.8) found that TXGM nanoparticles released MCZ more steadily than MCZ dispersion did. A 1-fold increase in the permeation of MCZ was observed from nanoparticles using albino rat intestine compared to MCZ. Albino rats were used to test the pharmacokinetics of MCZ, and the results showed a 4.5-fold increase in bioavailability. In conclusion, the thiolation of XGM enhances its bioavailability, controlled release of MCZ for a long period of time, and mucoadhesive activity.https://www.mdpi.com/1999-4923/16/2/225xanthan gumthiolationnanoparticlesantifungal activitypharmacokinetics |
| spellingShingle | Nader I. Namazi Hamad Alrbyawi Abdulkareem Ali Alanezi Afaf F Almuqati Anwar Shams Hany S. M. Ali Nanoparticles of Thiolated Xanthan Gum for the Oral Delivery of Miconazole Nitrate: In Vitro and In Vivo Evaluation Pharmaceutics xanthan gum thiolation nanoparticles antifungal activity pharmacokinetics |
| title | Nanoparticles of Thiolated Xanthan Gum for the Oral Delivery of Miconazole Nitrate: In Vitro and In Vivo Evaluation |
| title_full | Nanoparticles of Thiolated Xanthan Gum for the Oral Delivery of Miconazole Nitrate: In Vitro and In Vivo Evaluation |
| title_fullStr | Nanoparticles of Thiolated Xanthan Gum for the Oral Delivery of Miconazole Nitrate: In Vitro and In Vivo Evaluation |
| title_full_unstemmed | Nanoparticles of Thiolated Xanthan Gum for the Oral Delivery of Miconazole Nitrate: In Vitro and In Vivo Evaluation |
| title_short | Nanoparticles of Thiolated Xanthan Gum for the Oral Delivery of Miconazole Nitrate: In Vitro and In Vivo Evaluation |
| title_sort | nanoparticles of thiolated xanthan gum for the oral delivery of miconazole nitrate in vitro and in vivo evaluation |
| topic | xanthan gum thiolation nanoparticles antifungal activity pharmacokinetics |
| url | https://www.mdpi.com/1999-4923/16/2/225 |
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