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Improved oral bioavailability and target delivery of 6-shogaol via vitamin E TPGS-modified liposomes: Preparation, in-vitroand in-vivocharacterizations

Authors :
Bao, Rui
Wang, Qi-Long
Li, Ran
Adu-Frimpong, Michael
Toreniyazov, Elmurat
Ji, Hao
Xu, Xi-Ming
Yu, Jiang-Nan
Source :
Journal of Drug Delivery Science and Technology; October 2020, Vol. 59 Issue: 1
Publication Year :
2020

Abstract

6-Shogaol is one component of ginger, which has been described to possess various health-promoting effects including anticancer, antiinflammatory, antioxidant and antiatherogenic. However, poor water solubility has limited the aforementioned health benefits and clinical applications of the drug. Herein, the aforementioned drawback was circumvented by the preparation of 6-shogaol-loaded liposome through thin-film dispersion method with TPGS as the carrier, in comparison with 6-shogaol liposome and free 6-shogaol. Appropriate indices were used for the characterization of the developed liposomes viz., particle size (PS), zeta potential (Z-potential), polydispersity index (PDI), entrapment efficiency (EE) and loading capacity (LC) while their morphologies were observed under the transmission electron microscopy (TEM). In-vitrodissolution investigation showed a substantial improvement in the accumulative release rates of liposomes comparable to the free 6-shogaol. The TPGS-modified 6-shogaol and 6-shogaol liposomes had oral relative bioavailability (RBA) of 580.04% and 281.55%, respectively, with improved t1/2, MRT, Cmax, AUC0-tand Tmax. Pertinently, the TPGS coated 6-shogaol liposome may enhance the targeting of the drug to the brain. Therefore, the TPGS coated 6-shogaol liposome could potentially improve oral bioavailability of lipophilic drug in-vivo. More importantly, the results of tissue distribution investigation suggest that TPGS coated 6-shogaol liposome may act as promising carrier for brain delivery in future.

Details

Language :
English
ISSN :
17732247
Volume :
59
Issue :
1
Database :
Supplemental Index
Journal :
Journal of Drug Delivery Science and Technology
Publication Type :
Periodical
Accession number :
ejs53671838
Full Text :
https://doi.org/10.1016/j.jddst.2020.101842