The characterisation, pharmacokinetic and tissue distribution studies of TPGS modified myricetrin mixed micelles in rats

Abstract

This study was designed to investigate the bioavailability and targeting of myricetrin-loaded ternary micelles modified with and without TPGS. The particle diameters of myricetrin-loaded micelles and myricetrin-loaded-TPGS micelle were 30.93 ± 1.34 nm and 26.42 ± 0.89 nm, respectively, while their respective encapsulation efficiencies (m/m, %) were 83.3 ± 1.08 and 93.8 ± 1.18. The release rate of myricetrin in the micellar system clearly exceeded the free myricetrin in the three media (pH 6.8 phosphate buffer, pH 1.2 HCl solution and double distilled water). In vivo studies displayed that the bioavailability of myricetrin mixed micelles was remarkably improved than the free drug after oral administration. Moreover, the results of tissue distribution showed that myricetrin-loaded-TPGS micelles accumulated well in the liver tissue. Based on these results, it was speculated that myricetrin-loaded-TPGS micelles might act as a promising carrier for liver targeting with improved hepatic concentration of myricetrin compared with the myricetrin-loaded micelles.

Keywords:

• Myricetrin mixed micelles
• TPGS
• in vitro release
• oral bioavailability
• tissue distribution

Acknowledgements

We appreciate the University Ethics Committee for playing crucial role in the approval of the instructions for the animal experiments.

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

This work was funded by National Natural Science Foundation of China (81473172, 81503025), National ‘Twelfth Five-Year’ Plan for Science & Technology Support (Grant 2013BAD16B07-1), and a project financed by the Priority Academic Programme Development of Jiangsu Higher Education Institutions. This study was also supported by Funding for Key Lab of Drug Delivery and Tissue Regeneration (SS2018004).