Journal
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
Volume 59, Issue -, Pages -Publisher
ELSEVIER
DOI: 10.1016/j.jddst.2020.101842
Keywords
6-shogaol; TPGS; Liposome; Oral bioavailability; Tissue distribution
Categories
Funding
- National Natural Science Foundation of China [81473172, 81720108030, 81773695]
- Innovation Team in Colleges and Universities of Jiangsu Province [SJK-2015-4]
- National Key Research and Development Program of China [2018YFE0208600]
- Natural Science Foundation of the Jiangsu Higher Education Institution of China [19KJB350008]
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6-Shogaol is one component of ginger, which has been described to possess various health-promoting effects including anticancer, antiinflammatory, antioxidant and antiathemgenic. 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-vitro dissolution 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 t(1/)(2), MRT, C-max, AUC(0)(-t) and T-max. 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.
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