Enhancement of the oral bioavailability of isopropoxy benzene guanidine though complexation with hydroxypropyl-β-cyclodextrin
Isopropoxy benzene guanidine (IBG) is a novel substituted benzene guanidine analogue with antibacterial activity against multidrug-resistant bacteria. However, the bioavailability of IBG is not optimal due to its finite aqueous solubility, thus hampering its potential therapeutic exploitation. In th...
| Main Authors: | , , , , , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
Taylor & Francis Group
2022-12-01
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| Series: | Drug Delivery |
| Subjects: | |
| Online Access: | https://www.tandfonline.com/doi/10.1080/10717544.2022.2118400 |
| _version_ | 1798036627582353408 |
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| author | Yixing Lu Liuye Yang Wanying Zhang Shiting Xie Feifei Zhao Xianfeng Peng Zonghua Qin Dongping Zeng Zhenling Zeng |
| author_facet | Yixing Lu Liuye Yang Wanying Zhang Shiting Xie Feifei Zhao Xianfeng Peng Zonghua Qin Dongping Zeng Zhenling Zeng |
| author_sort | Yixing Lu |
| collection | DOAJ |
| description | Isopropoxy benzene guanidine (IBG) is a novel substituted benzene guanidine analogue with antibacterial activity against multidrug-resistant bacteria. However, the bioavailability of IBG is not optimal due to its finite aqueous solubility, thus hampering its potential therapeutic exploitation. In this study, we prepared IBG/hydroxypropyl-β-CD (IBG/HP-β-CD) complex, and characterized it by differential scanning calorimetry, Fourier transform infrared spectroscopy, powder X-ray diffraction, and scanning electron microscopy. Physicochemical characterization indicated that the crystal morphology of IBG transformed into an amorphous state, thus forming IBG/HP-β-CD inclusion complexes. Complexation with HP-β-CD significantly improve the aqueous solubility, pharmaceutical properties, absorption, and bioavailability of IBG. |
| first_indexed | 2024-04-11T21:15:32Z |
| format | Article |
| id | doaj.art-1e7c918289a148abbf762031c2191605 |
| institution | Directory Open Access Journal |
| issn | 1071-7544 1521-0464 |
| language | English |
| last_indexed | 2024-04-11T21:15:32Z |
| publishDate | 2022-12-01 |
| publisher | Taylor & Francis Group |
| record_format | Article |
| series | Drug Delivery |
| spelling | doaj.art-1e7c918289a148abbf762031c21916052022-12-22T04:02:50ZengTaylor & Francis GroupDrug Delivery1071-75441521-04642022-12-012912824283010.1080/10717544.2022.2118400Enhancement of the oral bioavailability of isopropoxy benzene guanidine though complexation with hydroxypropyl-β-cyclodextrinYixing Lu0Liuye Yang1Wanying Zhang2Shiting Xie3Feifei Zhao4Xianfeng Peng5Zonghua Qin6Dongping Zeng7Zhenling Zeng8Guangdong Provincial Key Laboratory of Veterinary Pharmaceutics Development and Safety Evaluation, National Risk Assessment Laboratory for Antimicrobial Resistance of Animal Original Bacteria, College of Veterinary Medicine, South China Agricultural University, Guangzhou, ChinaGuangdong Provincial Key Laboratory of Veterinary Pharmaceutics Development and Safety Evaluation, National Risk Assessment Laboratory for Antimicrobial Resistance of Animal Original Bacteria, College of Veterinary Medicine, South China Agricultural University, Guangzhou, ChinaGuangdong Provincial Key Laboratory of Veterinary Pharmaceutics Development and Safety Evaluation, National Risk Assessment Laboratory for Antimicrobial Resistance of Animal Original Bacteria, College of Veterinary Medicine, South China Agricultural University, Guangzhou, ChinaGuangdong Provincial Key Laboratory of Veterinary Pharmaceutics Development and Safety Evaluation, National Risk Assessment Laboratory for Antimicrobial Resistance of Animal Original Bacteria, College of Veterinary Medicine, South China Agricultural University, Guangzhou, ChinaGuangdong Provincial Key Laboratory of Veterinary Pharmaceutics Development and Safety Evaluation, National Risk Assessment Laboratory for Antimicrobial Resistance of Animal Original Bacteria, College of Veterinary Medicine, South China Agricultural University, Guangzhou, ChinaGuangzhou Insighter Biotechnology Co., Ltd, Guangzhou, ChinaGuangzhou Insighter Biotechnology Co., Ltd, Guangzhou, ChinaGuangdong Provincial Key Laboratory of Veterinary Pharmaceutics Development and Safety Evaluation, National Risk Assessment Laboratory for Antimicrobial Resistance of Animal Original Bacteria, College of Veterinary Medicine, South China Agricultural University, Guangzhou, ChinaGuangdong Provincial Key Laboratory of Veterinary Pharmaceutics Development and Safety Evaluation, National Risk Assessment Laboratory for Antimicrobial Resistance of Animal Original Bacteria, College of Veterinary Medicine, South China Agricultural University, Guangzhou, ChinaIsopropoxy benzene guanidine (IBG) is a novel substituted benzene guanidine analogue with antibacterial activity against multidrug-resistant bacteria. However, the bioavailability of IBG is not optimal due to its finite aqueous solubility, thus hampering its potential therapeutic exploitation. In this study, we prepared IBG/hydroxypropyl-β-CD (IBG/HP-β-CD) complex, and characterized it by differential scanning calorimetry, Fourier transform infrared spectroscopy, powder X-ray diffraction, and scanning electron microscopy. Physicochemical characterization indicated that the crystal morphology of IBG transformed into an amorphous state, thus forming IBG/HP-β-CD inclusion complexes. Complexation with HP-β-CD significantly improve the aqueous solubility, pharmaceutical properties, absorption, and bioavailability of IBG.https://www.tandfonline.com/doi/10.1080/10717544.2022.2118400Isopropoxy benzene guanidinehydroxypropyl-β-cyclodextrindissolutionbioavailabilitypharmacokinetics |
| spellingShingle | Yixing Lu Liuye Yang Wanying Zhang Shiting Xie Feifei Zhao Xianfeng Peng Zonghua Qin Dongping Zeng Zhenling Zeng Enhancement of the oral bioavailability of isopropoxy benzene guanidine though complexation with hydroxypropyl-β-cyclodextrin Drug Delivery Isopropoxy benzene guanidine hydroxypropyl-β-cyclodextrin dissolution bioavailability pharmacokinetics |
| title | Enhancement of the oral bioavailability of isopropoxy benzene guanidine though complexation with hydroxypropyl-β-cyclodextrin |
| title_full | Enhancement of the oral bioavailability of isopropoxy benzene guanidine though complexation with hydroxypropyl-β-cyclodextrin |
| title_fullStr | Enhancement of the oral bioavailability of isopropoxy benzene guanidine though complexation with hydroxypropyl-β-cyclodextrin |
| title_full_unstemmed | Enhancement of the oral bioavailability of isopropoxy benzene guanidine though complexation with hydroxypropyl-β-cyclodextrin |
| title_short | Enhancement of the oral bioavailability of isopropoxy benzene guanidine though complexation with hydroxypropyl-β-cyclodextrin |
| title_sort | enhancement of the oral bioavailability of isopropoxy benzene guanidine though complexation with hydroxypropyl β cyclodextrin |
| topic | Isopropoxy benzene guanidine hydroxypropyl-β-cyclodextrin dissolution bioavailability pharmacokinetics |
| url | https://www.tandfonline.com/doi/10.1080/10717544.2022.2118400 |
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