Investigating the Phospholipid Effect on the Bioaccessibility of Rosmarinic Acid-Phospholipid Complex through a Dynamic Gastrointestinal in Vitro Model
Phyto-phospholipid complexes have been developed as a common way of improving the oral bioavailability of poorly absorbable phyto-pharmaceuticals; however, the complexation with phospholipids can induce positive or negative effects on the bioaccessibility of such plant-derived active ingredients in...
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| Format: | Article |
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MDPI AG
2019-04-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/11/4/156 |
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| author | Jiahao Huang Peter X. Chen Michael A. Rogers Shawn D. Wettig |
| author_facet | Jiahao Huang Peter X. Chen Michael A. Rogers Shawn D. Wettig |
| author_sort | Jiahao Huang |
| collection | DOAJ |
| description | Phyto-phospholipid complexes have been developed as a common way of improving the oral bioavailability of poorly absorbable phyto-pharmaceuticals; however, the complexation with phospholipids can induce positive or negative effects on the bioaccessibility of such plant-derived active ingredients in different parts of the gastrointestinal tract (GIT). The purpose of this study was to investigate the effects of phospholipid complexation on the bioaccessibility of a rosmarinic acid-phospholipid complex (RA-PLC) using the TNO dynamic intestinal model-1 (TIM-1). Preparation of RA-PLC was confirmed using X-ray diffraction, Fourier-transform infrared spectroscopy, partition coefficient measurement, and Caco-2 monolayer permeation test. Bioaccessibility parameters in different GIT compartments were investigated. Complexation by phospholipids reduced the bioaccessibility of RA in jejunum compartment, while maintaining the ileum bioaccessibility. The overall bioaccessibility of RA-PLC was lower than the unformulated drug, suggesting that the improved oral absorption from a previous animal study could be considered as a net result of decreased bioaccessibility overwhelmed by enhanced intestinal permeability. This study provides insights into the effects of phospholipid on the bioaccessibility of hydrophilic compounds, and analyzes them based on the relationship between bioaccessibility, membrane permeability, and bioavailability. Additionally, TIM-1 shows promise in the evaluation of dosage forms containing materials with complicated effects on bioaccessibility. |
| first_indexed | 2024-04-13T06:18:02Z |
| format | Article |
| id | doaj.art-67738ff656774a2783e624d80239eeb4 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-04-13T06:18:02Z |
| publishDate | 2019-04-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-67738ff656774a2783e624d80239eeb42022-12-22T02:58:44ZengMDPI AGPharmaceutics1999-49232019-04-0111415610.3390/pharmaceutics11040156pharmaceutics11040156Investigating the Phospholipid Effect on the Bioaccessibility of Rosmarinic Acid-Phospholipid Complex through a Dynamic Gastrointestinal in Vitro ModelJiahao Huang0Peter X. Chen1Michael A. Rogers2Shawn D. Wettig3School of Pharmacy, University of Waterloo, Waterloo, ON N2L3G1, CanadaSchool of Pharmacy, University of Waterloo, Waterloo, ON N2L3G1, CanadaDepartment of Food Science, University of Guelph, Guelph, ON N1G2W1, CanadaSchool of Pharmacy, University of Waterloo, Waterloo, ON N2L3G1, CanadaPhyto-phospholipid complexes have been developed as a common way of improving the oral bioavailability of poorly absorbable phyto-pharmaceuticals; however, the complexation with phospholipids can induce positive or negative effects on the bioaccessibility of such plant-derived active ingredients in different parts of the gastrointestinal tract (GIT). The purpose of this study was to investigate the effects of phospholipid complexation on the bioaccessibility of a rosmarinic acid-phospholipid complex (RA-PLC) using the TNO dynamic intestinal model-1 (TIM-1). Preparation of RA-PLC was confirmed using X-ray diffraction, Fourier-transform infrared spectroscopy, partition coefficient measurement, and Caco-2 monolayer permeation test. Bioaccessibility parameters in different GIT compartments were investigated. Complexation by phospholipids reduced the bioaccessibility of RA in jejunum compartment, while maintaining the ileum bioaccessibility. The overall bioaccessibility of RA-PLC was lower than the unformulated drug, suggesting that the improved oral absorption from a previous animal study could be considered as a net result of decreased bioaccessibility overwhelmed by enhanced intestinal permeability. This study provides insights into the effects of phospholipid on the bioaccessibility of hydrophilic compounds, and analyzes them based on the relationship between bioaccessibility, membrane permeability, and bioavailability. Additionally, TIM-1 shows promise in the evaluation of dosage forms containing materials with complicated effects on bioaccessibility.https://www.mdpi.com/1999-4923/11/4/156phospholipid complexrosmarinic acidbioaccessibilitydissolutionTNO gastrointestinal modelgastrointestinal simulator |
| spellingShingle | Jiahao Huang Peter X. Chen Michael A. Rogers Shawn D. Wettig Investigating the Phospholipid Effect on the Bioaccessibility of Rosmarinic Acid-Phospholipid Complex through a Dynamic Gastrointestinal in Vitro Model Pharmaceutics phospholipid complex rosmarinic acid bioaccessibility dissolution TNO gastrointestinal model gastrointestinal simulator |
| title | Investigating the Phospholipid Effect on the Bioaccessibility of Rosmarinic Acid-Phospholipid Complex through a Dynamic Gastrointestinal in Vitro Model |
| title_full | Investigating the Phospholipid Effect on the Bioaccessibility of Rosmarinic Acid-Phospholipid Complex through a Dynamic Gastrointestinal in Vitro Model |
| title_fullStr | Investigating the Phospholipid Effect on the Bioaccessibility of Rosmarinic Acid-Phospholipid Complex through a Dynamic Gastrointestinal in Vitro Model |
| title_full_unstemmed | Investigating the Phospholipid Effect on the Bioaccessibility of Rosmarinic Acid-Phospholipid Complex through a Dynamic Gastrointestinal in Vitro Model |
| title_short | Investigating the Phospholipid Effect on the Bioaccessibility of Rosmarinic Acid-Phospholipid Complex through a Dynamic Gastrointestinal in Vitro Model |
| title_sort | investigating the phospholipid effect on the bioaccessibility of rosmarinic acid phospholipid complex through a dynamic gastrointestinal in vitro model |
| topic | phospholipid complex rosmarinic acid bioaccessibility dissolution TNO gastrointestinal model gastrointestinal simulator |
| url | https://www.mdpi.com/1999-4923/11/4/156 |
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