Improved oral bioavailability and target delivery of 6-Shogaol via Vitamin E TPGS-modified liposomes: Preparation, in-vitro and in-vivo characterizations

6-Shogaol is one component of ginger, which has been described to possess various health-promoting effects including anticancer, anti-inflammatory, 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-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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Rui Bao, Qi-Long Wang, Ran Li, Michael Adu-Frimpong, Elmurat Toreniyazov, Hao Ji, Xi-Ming Xu, Jiang-Nan Yu
Journal of Drug Delivery Science and Technology,  1 July 2020, 101842

Keywords: 6-Shogaol, TPGS, Liposome, Oral bioavailability, Tissue distribution