Self-micellizing solid dispersion of thymoquinone with enhanced biopharmaceutical and nephroprotective effects
AbstractThe present study was designed to develop a self-micellizing solid dispersion (SMSD) containing Thymoquinone (TQM), a phytonutrient obtained from Nigella sativa seeds, aiming to improve its biopharmaceutical and nephroprotective functions. The apparent solubility of TQM in polymer solutions...
| Main Authors: | , , , , , , , |
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| Format: | Article |
| Language: | English |
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Taylor & Francis Group
2024-12-01
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| Series: | Drug Delivery |
| Subjects: | |
| Online Access: | https://www.tandfonline.com/doi/10.1080/10717544.2024.2337423 |
| _version_ | 1797216999672119296 |
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| author | Shimul Halder Sanjida Afrose Manik Chandra Shill Nahid Sharmin Patricia Prova Mollick Madhabi Lata Shuma Md. Abdul Muhit S. M. Abdur Rahman |
| author_facet | Shimul Halder Sanjida Afrose Manik Chandra Shill Nahid Sharmin Patricia Prova Mollick Madhabi Lata Shuma Md. Abdul Muhit S. M. Abdur Rahman |
| author_sort | Shimul Halder |
| collection | DOAJ |
| description | AbstractThe present study was designed to develop a self-micellizing solid dispersion (SMSD) containing Thymoquinone (TQM), a phytonutrient obtained from Nigella sativa seeds, aiming to improve its biopharmaceutical and nephroprotective functions. The apparent solubility of TQM in polymer solutions was used to choose an appropriate amphiphilic polymer that could be used to make an SMSD system. Based on the apparent solubility, Soluplus® was selected as an appropriate carrier, and mixing with TQM, SMSD-TQM with different loadings of TQM (5–15%) was made by solvent evaporation and freeze-drying techniques, respectively, and the formulations were optimized. The optimized SMSD-TQM was evaluated in terms of particle size distribution, morphology, release characteristics, pharmacokinetic behavior, and nephroprotective effects in a rat model of acute kidney injury. SMSD-TQM significantly improved the dissolution characteristics (97.8%) of TQM in water within 60 min. Oral administration of SMSD-TQM in rats exhibited a 4.9-fold higher systemic exposure than crystalline TQM. In a cisplatin-induced (6 mg/kg, i.p.) acute kidney-damaged rat model, oral SMSD-TQM (10 mg/kg) improved the nephroprotective effects of TQM based on the results of kidney biomarkers and histological abnormalities. These findings suggest that SMSD-TQM might be efficacious in enhancing the nephroprotective effect of TQM by overcoming biopharmaceutical limitations. |
| first_indexed | 2024-04-24T11:54:53Z |
| format | Article |
| id | doaj.art-d7d3a4d290ab4c5e903dfb753b062fee |
| institution | Directory Open Access Journal |
| issn | 1071-7544 1521-0464 |
| language | English |
| last_indexed | 2024-04-24T11:54:53Z |
| publishDate | 2024-12-01 |
| publisher | Taylor & Francis Group |
| record_format | Article |
| series | Drug Delivery |
| spelling | doaj.art-d7d3a4d290ab4c5e903dfb753b062fee2024-04-09T05:41:45ZengTaylor & Francis GroupDrug Delivery1071-75441521-04642024-12-0131110.1080/10717544.2024.2337423Self-micellizing solid dispersion of thymoquinone with enhanced biopharmaceutical and nephroprotective effectsShimul Halder0Sanjida Afrose1Manik Chandra Shill2Nahid Sharmin3Patricia Prova Mollick4Madhabi Lata Shuma5Md. Abdul Muhit6S. M. Abdur Rahman7Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Dhaka, Dhaka, BangladeshDepartment of Pharmaceutical Technology, Faculty of Pharmacy, University of Dhaka, Dhaka, BangladeshDepartment of Pharmaceutical Sciences, North South University, Dhaka, BangladeshDepartment of Pharmaceutical Technology, Faculty of Pharmacy, University of Dhaka, Dhaka, BangladeshDepartment of Pharmaceutical Sciences, North South University, Dhaka, BangladeshDepartment of Pharmacy, School of Pharmacy and Public Health, Independent University Bangladesh, Dhaka, BangladeshDepartment of Clinical Pharmacy and Pharmacology, Faculty of Pharmacy, University of Dhaka, Dhaka, BangladeshDepartment of Clinical Pharmacy and Pharmacology, Faculty of Pharmacy, University of Dhaka, Dhaka, BangladeshAbstractThe present study was designed to develop a self-micellizing solid dispersion (SMSD) containing Thymoquinone (TQM), a phytonutrient obtained from Nigella sativa seeds, aiming to improve its biopharmaceutical and nephroprotective functions. The apparent solubility of TQM in polymer solutions was used to choose an appropriate amphiphilic polymer that could be used to make an SMSD system. Based on the apparent solubility, Soluplus® was selected as an appropriate carrier, and mixing with TQM, SMSD-TQM with different loadings of TQM (5–15%) was made by solvent evaporation and freeze-drying techniques, respectively, and the formulations were optimized. The optimized SMSD-TQM was evaluated in terms of particle size distribution, morphology, release characteristics, pharmacokinetic behavior, and nephroprotective effects in a rat model of acute kidney injury. SMSD-TQM significantly improved the dissolution characteristics (97.8%) of TQM in water within 60 min. Oral administration of SMSD-TQM in rats exhibited a 4.9-fold higher systemic exposure than crystalline TQM. In a cisplatin-induced (6 mg/kg, i.p.) acute kidney-damaged rat model, oral SMSD-TQM (10 mg/kg) improved the nephroprotective effects of TQM based on the results of kidney biomarkers and histological abnormalities. These findings suggest that SMSD-TQM might be efficacious in enhancing the nephroprotective effect of TQM by overcoming biopharmaceutical limitations.https://www.tandfonline.com/doi/10.1080/10717544.2024.2337423Biopharmaceuticalnephroprotectiveoral absorptionself-micellizing solid dispersionthymoquinone |
| spellingShingle | Shimul Halder Sanjida Afrose Manik Chandra Shill Nahid Sharmin Patricia Prova Mollick Madhabi Lata Shuma Md. Abdul Muhit S. M. Abdur Rahman Self-micellizing solid dispersion of thymoquinone with enhanced biopharmaceutical and nephroprotective effects Drug Delivery Biopharmaceutical nephroprotective oral absorption self-micellizing solid dispersion thymoquinone |
| title | Self-micellizing solid dispersion of thymoquinone with enhanced biopharmaceutical and nephroprotective effects |
| title_full | Self-micellizing solid dispersion of thymoquinone with enhanced biopharmaceutical and nephroprotective effects |
| title_fullStr | Self-micellizing solid dispersion of thymoquinone with enhanced biopharmaceutical and nephroprotective effects |
| title_full_unstemmed | Self-micellizing solid dispersion of thymoquinone with enhanced biopharmaceutical and nephroprotective effects |
| title_short | Self-micellizing solid dispersion of thymoquinone with enhanced biopharmaceutical and nephroprotective effects |
| title_sort | self micellizing solid dispersion of thymoquinone with enhanced biopharmaceutical and nephroprotective effects |
| topic | Biopharmaceutical nephroprotective oral absorption self-micellizing solid dispersion thymoquinone |
| url | https://www.tandfonline.com/doi/10.1080/10717544.2024.2337423 |
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