Optimized solubility and bioavailability of genistein based on cocrystal engineering
Abstract With various potential health-promoting bioactivities, genistein has great prospects in treatment of a series of complex diseases and metabolic syndromes such as cancer, diabetes, cardiovascular diseases, menopausal symptoms and so on. However, poor solubility and unsatisfactory bioavailabi...
| Main Authors: | , , , , , , , , , , |
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| Format: | Article |
| Language: | English |
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SpringerOpen
2023-09-01
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| Series: | Natural Products and Bioprospecting |
| Subjects: | |
| Online Access: | https://doi.org/10.1007/s13659-023-00397-w |
| _version_ | 1827707678149836800 |
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| author | Zhipeng Wang Qi Li Qi An Lixiang Gong Shiying Yang Baoxi Zhang Bin Su Dezhi Yang Li Zhang Yang Lu Guanhua Du |
| author_facet | Zhipeng Wang Qi Li Qi An Lixiang Gong Shiying Yang Baoxi Zhang Bin Su Dezhi Yang Li Zhang Yang Lu Guanhua Du |
| author_sort | Zhipeng Wang |
| collection | DOAJ |
| description | Abstract With various potential health-promoting bioactivities, genistein has great prospects in treatment of a series of complex diseases and metabolic syndromes such as cancer, diabetes, cardiovascular diseases, menopausal symptoms and so on. However, poor solubility and unsatisfactory bioavailability seriously limits its clinical application and market development. To optimize the solubility and bioavailability of genistein, the cocrystal of genistein and piperazine was prepared by grinding assisted with solvent based on the concept of cocrystal engineering. Using a series of analytical techniques including single-crystal X-ray diffraction, powder X-ray diffraction, Fourier transform infrared spectroscopy, differential scanning calorimetry and thermogravimetric analysis, the cocrystal was characterized and confirmed. Then, structure analysis on the basis of theoretical calculation and a series of evaluation on the stability, dissolution and bioavailability were carried out. The results indicated that the cocrystal of genistein and piperazine improved the solubility and bioavailability of genistein. Compared with the previous studies on the cocrystal of genistein, this is a systematic and comprehensive investigation from the aspects of preparation, characterization, structural analysis, stability, solubility and bioavailability evaluation. As a simple, efficient and green approach, cocrystal engineering can pave a new path to optimize the pharmaceutical properties of natural products for successful drug formulation and delivery. Graphical Abstract |
| first_indexed | 2024-03-10T16:50:51Z |
| format | Article |
| id | doaj.art-81ba1ca4e0d847b2aa6525e1d3b7c3e1 |
| institution | Directory Open Access Journal |
| issn | 2192-2195 2192-2209 |
| language | English |
| last_indexed | 2024-03-10T16:50:51Z |
| publishDate | 2023-09-01 |
| publisher | SpringerOpen |
| record_format | Article |
| series | Natural Products and Bioprospecting |
| spelling | doaj.art-81ba1ca4e0d847b2aa6525e1d3b7c3e12023-11-20T11:17:55ZengSpringerOpenNatural Products and Bioprospecting2192-21952192-22092023-09-0113111410.1007/s13659-023-00397-wOptimized solubility and bioavailability of genistein based on cocrystal engineeringZhipeng Wang0Qi Li1Qi An2Lixiang Gong3Shiying Yang4Baoxi Zhang5Bin Su6Dezhi Yang7Li Zhang8Yang Lu9Guanhua Du10Beijing City Key Laboratory of Polymorphic Drugs, Center of Pharmaceutical Polymorphs, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical CollegeBeijing City Key Laboratory of Polymorphic Drugs, Center of Pharmaceutical Polymorphs, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical CollegeBeijing City Key Laboratory of Polymorphic Drugs, Center of Pharmaceutical Polymorphs, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical CollegeBeijing City Key Laboratory of Polymorphic Drugs, Center of Pharmaceutical Polymorphs, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical CollegeBeijing City Key Laboratory of Polymorphic Drugs, Center of Pharmaceutical Polymorphs, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical CollegeBeijing City Key Laboratory of Polymorphic Drugs, Center of Pharmaceutical Polymorphs, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical CollegeShandong Soteria Pharmaceutical Co., Ltd.Beijing City Key Laboratory of Polymorphic Drugs, Center of Pharmaceutical Polymorphs, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical CollegeBeijing City Key Laboratory of Polymorphic Drugs, Center of Pharmaceutical Polymorphs, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical CollegeBeijing City Key Laboratory of Polymorphic Drugs, Center of Pharmaceutical Polymorphs, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical CollegeBeijing City Key Laboratory of Drug Target and Screening Research, National Center for Pharmaceutical Screening, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical CollegeAbstract With various potential health-promoting bioactivities, genistein has great prospects in treatment of a series of complex diseases and metabolic syndromes such as cancer, diabetes, cardiovascular diseases, menopausal symptoms and so on. However, poor solubility and unsatisfactory bioavailability seriously limits its clinical application and market development. To optimize the solubility and bioavailability of genistein, the cocrystal of genistein and piperazine was prepared by grinding assisted with solvent based on the concept of cocrystal engineering. Using a series of analytical techniques including single-crystal X-ray diffraction, powder X-ray diffraction, Fourier transform infrared spectroscopy, differential scanning calorimetry and thermogravimetric analysis, the cocrystal was characterized and confirmed. Then, structure analysis on the basis of theoretical calculation and a series of evaluation on the stability, dissolution and bioavailability were carried out. The results indicated that the cocrystal of genistein and piperazine improved the solubility and bioavailability of genistein. Compared with the previous studies on the cocrystal of genistein, this is a systematic and comprehensive investigation from the aspects of preparation, characterization, structural analysis, stability, solubility and bioavailability evaluation. As a simple, efficient and green approach, cocrystal engineering can pave a new path to optimize the pharmaceutical properties of natural products for successful drug formulation and delivery. Graphical Abstracthttps://doi.org/10.1007/s13659-023-00397-wGenisteinPiperazineCocrystalSolubilityBioavailability |
| spellingShingle | Zhipeng Wang Qi Li Qi An Lixiang Gong Shiying Yang Baoxi Zhang Bin Su Dezhi Yang Li Zhang Yang Lu Guanhua Du Optimized solubility and bioavailability of genistein based on cocrystal engineering Natural Products and Bioprospecting Genistein Piperazine Cocrystal Solubility Bioavailability |
| title | Optimized solubility and bioavailability of genistein based on cocrystal engineering |
| title_full | Optimized solubility and bioavailability of genistein based on cocrystal engineering |
| title_fullStr | Optimized solubility and bioavailability of genistein based on cocrystal engineering |
| title_full_unstemmed | Optimized solubility and bioavailability of genistein based on cocrystal engineering |
| title_short | Optimized solubility and bioavailability of genistein based on cocrystal engineering |
| title_sort | optimized solubility and bioavailability of genistein based on cocrystal engineering |
| topic | Genistein Piperazine Cocrystal Solubility Bioavailability |
| url | https://doi.org/10.1007/s13659-023-00397-w |
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