Kaempferol-Phospholipid Complex: Formulation, and Evaluation of Improved Solubility, In Vivo Bioavailability, and Antioxidant Potential of Kaempferol
The current work describes the formulation and evaluation of a phospholipid complex of kaempferol to enhance the latter’s aqueous solubility, in vitro dissolution rate, in vivo antioxidant and hepatoprotective activities, and oral bioavailability. The kaempferol-phospholipid complex was synthesized...
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| Format: | Article |
| Language: | English |
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International Pharmaceutical Excipients Council
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| Series: | Journal of Excipients and Food Chemicals |
| Online Access: | http://jefc.scholasticahq.com/article/1174-kaempferol-phospholipid-complex-formulation-and-evaluation-of-improved-solubility-in-vivo-bioavailability-and-antioxidant-potential-of-kaempferol.pdf |
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| author | Darshan R. Telange Arun T. Patil Anil M. Pethe Amol A. Tatode Sridhar Anand Vivek S. Dave |
| author_facet | Darshan R. Telange Arun T. Patil Anil M. Pethe Amol A. Tatode Sridhar Anand Vivek S. Dave |
| author_sort | Darshan R. Telange |
| collection | DOAJ |
| description | The current work describes the formulation and evaluation of a phospholipid complex of kaempferol to enhance the latter’s aqueous solubility, in vitro dissolution rate, in vivo antioxidant and hepatoprotective activities, and oral bioavailability. The kaempferol-phospholipid complex was synthesized using a freeze-drying method with the formulation being optimized using a full factorial design (32) approach. Our results include the validation of the mathematical model in order to ascertain the role of specific formulation and process variables that contribute favorably to the formulation’s development. The final product was characterized and confirmed by Differential Scanning Calorimetry (DSC), Fourier Transform Infrared Spectroscopy (FTIR), Proton Nuclear Magnetic Resonance Spectroscopy (1H-NMR), and Powder X-ray Diffraction (PXRD) analysis. The aqueous solubility and the in vitro dissolution rate were enhanced compared to that of pure kaempferol. The in vivo antioxidant properties of the kaempferol-phospholipid complex were evaluated by measuring its impact on carbon tetrachloride (CCl4)-intoxicated rats. The optimized phospholipid complex improved the liver function test parameters to a significant level by restoration of all elevated liver marker enzymes in CCl4-intoxicated rats. The complex also enhanced the in vivo antioxidant potential by increasing levels of GSH (reduced glutathione), SOD (superoxide dismutase), catalase and decreasing lipid peroxidation, compared to that of pure kaempferol. The final optimized phospholipid complex also demonstrated a significant improvement in oral bioavailability demonstrated by improvements to key pharmacokinetic parameters, compared to that of pure kaempferol. |
| first_indexed | 2024-12-10T06:23:59Z |
| format | Article |
| id | doaj.art-09eb5229952f4e748297a824227706e9 |
| institution | Directory Open Access Journal |
| issn | 2150-2668 |
| language | English |
| last_indexed | 2024-12-10T06:23:59Z |
| publisher | International Pharmaceutical Excipients Council |
| record_format | Article |
| series | Journal of Excipients and Food Chemicals |
| spelling | doaj.art-09eb5229952f4e748297a824227706e92022-12-22T01:59:15ZengInternational Pharmaceutical Excipients CouncilJournal of Excipients and Food Chemicals2150-2668Kaempferol-Phospholipid Complex: Formulation, and Evaluation of Improved Solubility, In Vivo Bioavailability, and Antioxidant Potential of KaempferolDarshan R. TelangeArun T. PatilAnil M. PetheAmol A. TatodeSridhar AnandVivek S. DaveThe current work describes the formulation and evaluation of a phospholipid complex of kaempferol to enhance the latter’s aqueous solubility, in vitro dissolution rate, in vivo antioxidant and hepatoprotective activities, and oral bioavailability. The kaempferol-phospholipid complex was synthesized using a freeze-drying method with the formulation being optimized using a full factorial design (32) approach. Our results include the validation of the mathematical model in order to ascertain the role of specific formulation and process variables that contribute favorably to the formulation’s development. The final product was characterized and confirmed by Differential Scanning Calorimetry (DSC), Fourier Transform Infrared Spectroscopy (FTIR), Proton Nuclear Magnetic Resonance Spectroscopy (1H-NMR), and Powder X-ray Diffraction (PXRD) analysis. The aqueous solubility and the in vitro dissolution rate were enhanced compared to that of pure kaempferol. The in vivo antioxidant properties of the kaempferol-phospholipid complex were evaluated by measuring its impact on carbon tetrachloride (CCl4)-intoxicated rats. The optimized phospholipid complex improved the liver function test parameters to a significant level by restoration of all elevated liver marker enzymes in CCl4-intoxicated rats. The complex also enhanced the in vivo antioxidant potential by increasing levels of GSH (reduced glutathione), SOD (superoxide dismutase), catalase and decreasing lipid peroxidation, compared to that of pure kaempferol. The final optimized phospholipid complex also demonstrated a significant improvement in oral bioavailability demonstrated by improvements to key pharmacokinetic parameters, compared to that of pure kaempferol.http://jefc.scholasticahq.com/article/1174-kaempferol-phospholipid-complex-formulation-and-evaluation-of-improved-solubility-in-vivo-bioavailability-and-antioxidant-potential-of-kaempferol.pdf |
| spellingShingle | Darshan R. Telange Arun T. Patil Anil M. Pethe Amol A. Tatode Sridhar Anand Vivek S. Dave Kaempferol-Phospholipid Complex: Formulation, and Evaluation of Improved Solubility, In Vivo Bioavailability, and Antioxidant Potential of Kaempferol Journal of Excipients and Food Chemicals |
| title | Kaempferol-Phospholipid Complex: Formulation, and Evaluation of Improved Solubility, In Vivo Bioavailability, and Antioxidant Potential of Kaempferol |
| title_full | Kaempferol-Phospholipid Complex: Formulation, and Evaluation of Improved Solubility, In Vivo Bioavailability, and Antioxidant Potential of Kaempferol |
| title_fullStr | Kaempferol-Phospholipid Complex: Formulation, and Evaluation of Improved Solubility, In Vivo Bioavailability, and Antioxidant Potential of Kaempferol |
| title_full_unstemmed | Kaempferol-Phospholipid Complex: Formulation, and Evaluation of Improved Solubility, In Vivo Bioavailability, and Antioxidant Potential of Kaempferol |
| title_short | Kaempferol-Phospholipid Complex: Formulation, and Evaluation of Improved Solubility, In Vivo Bioavailability, and Antioxidant Potential of Kaempferol |
| title_sort | kaempferol phospholipid complex formulation and evaluation of improved solubility in vivo bioavailability and antioxidant potential of kaempferol |
| url | http://jefc.scholasticahq.com/article/1174-kaempferol-phospholipid-complex-formulation-and-evaluation-of-improved-solubility-in-vivo-bioavailability-and-antioxidant-potential-of-kaempferol.pdf |
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