Mechanism of enhanced oral absorption of Akebia saponin D by a self-nanoemulsifying drug delivery system loaded with phospholipid complex
Authors
Wang, Yuhui
Shen, Jinyang
Yang, Xiaolin
Jin, Ye
Yang, Zhonglin
Wang, Rufeng
Zhang, Fuming
Linhardt, Robert J.
ORCID
https://orcid.org/0000-0003-2219-5833
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Other Contributors
Issue Date
2019-01-02
Keywords
Biology , Chemistry and chemical biology , Chemical and biological engineering , Biomedical engineering
Degree
Terms of Use
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Full Citation
Mechanism of enhanced oral absorption of Akebia saponin D by a self-nanoemulsifying drug delivery system loaded with phospholipid complex, Y. Wang, J. Shen, X. Yang, Y. Jin, Z. Yang, R. Wang, F. Zhang, R.J. Linhardt, Drug Development and Industrial Pharmacy, 45, 124-129, 2019.
Abstract
Akebia saponin D (ASD) exhibits a variety of pharmacological activities, such as anti-osteoporosis, neuroprotection, hepatoprotection, but has poor oral bioavailability. A self-nanoemulsifying drug delivery system loaded with akebia saponin D - phospholipid complex (APC-SNEDDS) (composition: Peceol: Cremophor® EL: Transcutol HP: ASD: phospholipid; ratio: 10:45:45:51:12.3, w:w:w:w:w) was first developed to improve the oral absorption of saponins and it was found to significantly enhance ASD's oral bioavailability by 4.3 - fold (p < .01). This study was conducted to elucidate the mechanism of enhanced oral absorption of ASD by the drug delivery system of APC-SNEDDS. The aggregation morphology and particle size of ASD and APC-SNEDDS prepared in aqueous solutions were determined by transmission electron microscope and particle size analyzer, respectively. Stability of ASD and APC-SNEDDS in gastrointestinal luminal contents and mucosa homogenates were also explored. The differences of in situ intestinal permeability of ASD and APC-SNEDDS were compared. APC-SNEDDS reduced the aggregation size from 389 ± 7 nm (ASD) to 148 ± 3 nm (APC-SNEDDS). APC-SNEDDS increased the remaining drug in large intestine luminal contents from 47 ± 1% (ASD) to 83 ± 1% (APC-SNEDDS) during 4 h incubation. APC-SNEDDS provided an 11-fold increase in Ka value and an 11-fold increase in Peff value compared to ASD. In summary, APC-SNEDDS improved ASD's oral bioavailability mainly by increasing membrane permeability, destroying self-micelles and inhibiting the intestinal metabolism.
Description
Drug Development and Industrial Pharmacy, 45, 124-129
Note : if this item contains full text it may be a preprint, author manuscript, or a Gold OA copy that permits redistribution with a license such as CC BY. The final version is available through the publisher’s platform.
Note : if this item contains full text it may be a preprint, author manuscript, or a Gold OA copy that permits redistribution with a license such as CC BY. The final version is available through the publisher’s platform.
Department
The Linhardt Research Labs.
The Shirley Ann Jackson, Ph.D. Center for Biotechnology and Interdisciplinary Studies (CBIS)
The Shirley Ann Jackson, Ph.D. Center for Biotechnology and Interdisciplinary Studies (CBIS)
Publisher
Relationships
The Linhardt Research Labs Online Collection
Rensselaer Polytechnic Institute, Troy, NY
Drug Development and Industrial Pharmacy
https://harc.rpi.edu/
Rensselaer Polytechnic Institute, Troy, NY
Drug Development and Industrial Pharmacy
https://harc.rpi.edu/
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https://login.libproxy.rpi.edu/login?url=https://doi.org/10.1080/03639045.2018.1526183