Self-microemulsifying drug delivery system for improving the bioavailability of huperzine A by lymphatic uptake
Huperzine A (Hup-A) is a poorly water-soluble drug with low oral bioavailability. A self-microemulsifying drug delivery system (SMEDDS) was used to enhance the oral bioavailability and lymphatic uptake and transport of Hup-A. A single-pass intestinal perfusion (SPIP) technique and a chylomicron flow...
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| Format: | Article |
| Language: | English |
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Elsevier
2017-05-01
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| Series: | Acta Pharmaceutica Sinica B |
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| Online Access: | http://www.sciencedirect.com/science/article/pii/S2211383516303471 |
| _version_ | 1818911227682750464 |
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| author | Fang Li Rongfeng Hu Bin Wang Yun Gui Gang Cheng Song Gao Lei Ye Jihui Tang |
| author_facet | Fang Li Rongfeng Hu Bin Wang Yun Gui Gang Cheng Song Gao Lei Ye Jihui Tang |
| author_sort | Fang Li |
| collection | DOAJ |
| description | Huperzine A (Hup-A) is a poorly water-soluble drug with low oral bioavailability. A self-microemulsifying drug delivery system (SMEDDS) was used to enhance the oral bioavailability and lymphatic uptake and transport of Hup-A. A single-pass intestinal perfusion (SPIP) technique and a chylomicron flow-blocking approach were used to study its intestinal absorption, mesenteric lymph node distribution and intestinal lymphatic uptake. The value of the area under the plasma concentration–time curve (AUC) of Hup-A SMEDDS was significantly higher than that of a Hup-A suspension (P<0.01). The absorption rate constant (Ka) and the apparent permeability coefficient (Papp) for Hup-A in different parts of the intestine suggested a passive transport mechanism, and the values of Ka and Papp of Hup-A SMEDDS in the ileum were much higher than those in other intestinal segments. The determination of Hup-A concentration in mesenteric lymph nodes can be used to explain the intestinal lymphatic absorption of Hup-A SMEDDS. For Hup-A SMEDDS, the values of AUC and maximum plasma concentration (Cmax) of the blocking model were significantly lower than those of the control model (P<0.05). The proportion of lymphatic transport of Hup-A SMEDDS and Hup-A suspension were about 40% and 5%, respectively, suggesting that SMEDDS can significantly improve the intestinal lymphatic uptake and transport of Hup-A. |
| first_indexed | 2024-12-19T22:55:21Z |
| format | Article |
| id | doaj.art-2bffe9039e234c659486ab0395802694 |
| institution | Directory Open Access Journal |
| issn | 2211-3835 2211-3843 |
| language | English |
| last_indexed | 2024-12-19T22:55:21Z |
| publishDate | 2017-05-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Acta Pharmaceutica Sinica B |
| spelling | doaj.art-2bffe9039e234c659486ab03958026942022-12-21T20:02:39ZengElsevierActa Pharmaceutica Sinica B2211-38352211-38432017-05-017335336010.1016/j.apsb.2017.02.002Self-microemulsifying drug delivery system for improving the bioavailability of huperzine A by lymphatic uptakeFang Li0Rongfeng Hu1Bin Wang2Yun Gui3Gang Cheng4Song Gao5Lei Ye6Jihui Tang7Anhui University of Chinese Medicine, Hefei 230038, ChinaAnhui University of Chinese Medicine, Hefei 230038, ChinaAnhui University of Chinese Medicine, Hefei 230038, ChinaAnhui University of Chinese Medicine, Hefei 230038, ChinaAnhui University of Chinese Medicine, Hefei 230038, ChinaAnhui University of Chinese Medicine, Hefei 230038, ChinaAnhui University of Chinese Medicine, Hefei 230038, ChinaSchool of Pharmacy, Anhui Medical University, Hefei 230022, ChinaHuperzine A (Hup-A) is a poorly water-soluble drug with low oral bioavailability. A self-microemulsifying drug delivery system (SMEDDS) was used to enhance the oral bioavailability and lymphatic uptake and transport of Hup-A. A single-pass intestinal perfusion (SPIP) technique and a chylomicron flow-blocking approach were used to study its intestinal absorption, mesenteric lymph node distribution and intestinal lymphatic uptake. The value of the area under the plasma concentration–time curve (AUC) of Hup-A SMEDDS was significantly higher than that of a Hup-A suspension (P<0.01). The absorption rate constant (Ka) and the apparent permeability coefficient (Papp) for Hup-A in different parts of the intestine suggested a passive transport mechanism, and the values of Ka and Papp of Hup-A SMEDDS in the ileum were much higher than those in other intestinal segments. The determination of Hup-A concentration in mesenteric lymph nodes can be used to explain the intestinal lymphatic absorption of Hup-A SMEDDS. For Hup-A SMEDDS, the values of AUC and maximum plasma concentration (Cmax) of the blocking model were significantly lower than those of the control model (P<0.05). The proportion of lymphatic transport of Hup-A SMEDDS and Hup-A suspension were about 40% and 5%, respectively, suggesting that SMEDDS can significantly improve the intestinal lymphatic uptake and transport of Hup-A.http://www.sciencedirect.com/science/article/pii/S2211383516303471Huperzine ASelf-microemulsionDrug delivery systemsSMEDDSBioavailabilitySingle-pass intestinal perfusionLymphatic transport |
| spellingShingle | Fang Li Rongfeng Hu Bin Wang Yun Gui Gang Cheng Song Gao Lei Ye Jihui Tang Self-microemulsifying drug delivery system for improving the bioavailability of huperzine A by lymphatic uptake Acta Pharmaceutica Sinica B Huperzine A Self-microemulsion Drug delivery systems SMEDDS Bioavailability Single-pass intestinal perfusion Lymphatic transport |
| title | Self-microemulsifying drug delivery system for improving the bioavailability of huperzine A by lymphatic uptake |
| title_full | Self-microemulsifying drug delivery system for improving the bioavailability of huperzine A by lymphatic uptake |
| title_fullStr | Self-microemulsifying drug delivery system for improving the bioavailability of huperzine A by lymphatic uptake |
| title_full_unstemmed | Self-microemulsifying drug delivery system for improving the bioavailability of huperzine A by lymphatic uptake |
| title_short | Self-microemulsifying drug delivery system for improving the bioavailability of huperzine A by lymphatic uptake |
| title_sort | self microemulsifying drug delivery system for improving the bioavailability of huperzine a by lymphatic uptake |
| topic | Huperzine A Self-microemulsion Drug delivery systems SMEDDS Bioavailability Single-pass intestinal perfusion Lymphatic transport |
| url | http://www.sciencedirect.com/science/article/pii/S2211383516303471 |
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