Combined use of phospholipid complexes and self-emulsifying microemulsions for improving the oral absorption of a BCS class IV compound, baicalin
The aim of this study was to develop a formulation to improve the oral absorption of baicalin (BA) by combining a phospholipid complex (PC) and self-emulsifying microemulsion drug delivery system (SMEDDS), termed BA–PC–SMEDDS. BA–PC was prepared by a solvent evaporation method and evaluated by compl...
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| Format: | Article |
| Language: | English |
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Elsevier
2014-06-01
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| Series: | Acta Pharmaceutica Sinica B |
| Subjects: | |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S221138351400029X |
| _version_ | 1818964449379221504 |
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| author | Huiyi Wu Xiaoying Long Fei Yuan Li Chen Sujing Pan Yunjun Liu Yoshiko Stowell Xiaoling Li |
| author_facet | Huiyi Wu Xiaoying Long Fei Yuan Li Chen Sujing Pan Yunjun Liu Yoshiko Stowell Xiaoling Li |
| author_sort | Huiyi Wu |
| collection | DOAJ |
| description | The aim of this study was to develop a formulation to improve the oral absorption of baicalin (BA) by combining a phospholipid complex (PC) and self-emulsifying microemulsion drug delivery system (SMEDDS), termed BA–PC–SMEDDS. BA–PC was prepared by a solvent evaporation method and evaluated by complexation percentage (CP). The physicochemical properties of BA–PC were determined. The synergistic effect of PC and SMEDDS on permeation of BA was studied in vitro with Caco-2 cells and in situ with a single pass intestinal perfusion model. The improved bioavailability of BA in BA–PC–SMEDDS was confirmed in an in vivo rat model. The CP of BA–PC reached 100% when the molar ratio of drug to phospholipid (PP) was ≥1:1. The solubility of BA–PC increased in both water and octanol, and the log Po/w of BA–PC was increased significantly. BA–PC–SMEDDS could be dispersed more evenly in water, compared to BA and BA–PC. Both the Caco-2 cell uptake and single-pass intestinal perfusion models illustrated that transport of BA in BA–PC was lower than that of free BA, while improved significantly in BA–PC–SMEDDS. The relative bioavailability of BA–PC(1:2)–SMEDDS was 220.37%. The combination system of PC and SMEDDS had a synergistic effect on improving the oral absorption of BA. |
| first_indexed | 2024-12-20T13:01:17Z |
| format | Article |
| id | doaj.art-29762c30578a42b48d5fe1b18cb2e8f6 |
| institution | Directory Open Access Journal |
| issn | 2211-3835 2211-3843 |
| language | English |
| last_indexed | 2024-12-20T13:01:17Z |
| publishDate | 2014-06-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Acta Pharmaceutica Sinica B |
| spelling | doaj.art-29762c30578a42b48d5fe1b18cb2e8f62022-12-21T19:39:54ZengElsevierActa Pharmaceutica Sinica B2211-38352211-38432014-06-014321722610.1016/j.apsb.2014.03.002Combined use of phospholipid complexes and self-emulsifying microemulsions for improving the oral absorption of a BCS class IV compound, baicalinHuiyi Wu0Xiaoying Long1Fei Yuan2Li Chen3Sujing Pan4Yunjun Liu5Yoshiko Stowell6Xiaoling Li7School of Traditional Chinese Medicine, Guangdong Pharmaceutical University, Guangzhou 510006, ChinaSchool of Traditional Chinese Medicine, Guangdong Pharmaceutical University, Guangzhou 510006, ChinaSchool of Traditional Chinese Medicine, Guangdong Pharmaceutical University, Guangzhou 510006, ChinaSchool of Traditional Chinese Medicine, Guangdong Pharmaceutical University, Guangzhou 510006, ChinaSchool of Traditional Chinese Medicine, Guangdong Pharmaceutical University, Guangzhou 510006, ChinaSchool of Traditional Chinese Medicine, Guangdong Pharmaceutical University, Guangzhou 510006, ChinaDepartment of Pharmaceutics, Thomas J Long School of Pharmacy & Health Sciences, University of the Pacific, CA 95211, USADepartment of Pharmaceutics, Thomas J Long School of Pharmacy & Health Sciences, University of the Pacific, CA 95211, USAThe aim of this study was to develop a formulation to improve the oral absorption of baicalin (BA) by combining a phospholipid complex (PC) and self-emulsifying microemulsion drug delivery system (SMEDDS), termed BA–PC–SMEDDS. BA–PC was prepared by a solvent evaporation method and evaluated by complexation percentage (CP). The physicochemical properties of BA–PC were determined. The synergistic effect of PC and SMEDDS on permeation of BA was studied in vitro with Caco-2 cells and in situ with a single pass intestinal perfusion model. The improved bioavailability of BA in BA–PC–SMEDDS was confirmed in an in vivo rat model. The CP of BA–PC reached 100% when the molar ratio of drug to phospholipid (PP) was ≥1:1. The solubility of BA–PC increased in both water and octanol, and the log Po/w of BA–PC was increased significantly. BA–PC–SMEDDS could be dispersed more evenly in water, compared to BA and BA–PC. Both the Caco-2 cell uptake and single-pass intestinal perfusion models illustrated that transport of BA in BA–PC was lower than that of free BA, while improved significantly in BA–PC–SMEDDS. The relative bioavailability of BA–PC(1:2)–SMEDDS was 220.37%. The combination system of PC and SMEDDS had a synergistic effect on improving the oral absorption of BA.http://www.sciencedirect.com/science/article/pii/S221138351400029XBaicalinSMEDDSPhospholipid complexCaco-2 cellSingle-pass intestinal perfusionBioavailability |
| spellingShingle | Huiyi Wu Xiaoying Long Fei Yuan Li Chen Sujing Pan Yunjun Liu Yoshiko Stowell Xiaoling Li Combined use of phospholipid complexes and self-emulsifying microemulsions for improving the oral absorption of a BCS class IV compound, baicalin Acta Pharmaceutica Sinica B Baicalin SMEDDS Phospholipid complex Caco-2 cell Single-pass intestinal perfusion Bioavailability |
| title | Combined use of phospholipid complexes and self-emulsifying microemulsions for improving the oral absorption of a BCS class IV compound, baicalin |
| title_full | Combined use of phospholipid complexes and self-emulsifying microemulsions for improving the oral absorption of a BCS class IV compound, baicalin |
| title_fullStr | Combined use of phospholipid complexes and self-emulsifying microemulsions for improving the oral absorption of a BCS class IV compound, baicalin |
| title_full_unstemmed | Combined use of phospholipid complexes and self-emulsifying microemulsions for improving the oral absorption of a BCS class IV compound, baicalin |
| title_short | Combined use of phospholipid complexes and self-emulsifying microemulsions for improving the oral absorption of a BCS class IV compound, baicalin |
| title_sort | combined use of phospholipid complexes and self emulsifying microemulsions for improving the oral absorption of a bcs class iv compound baicalin |
| topic | Baicalin SMEDDS Phospholipid complex Caco-2 cell Single-pass intestinal perfusion Bioavailability |
| url | http://www.sciencedirect.com/science/article/pii/S221138351400029X |
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