Improving physicochemical characteristics and cytotoxicity of baicalin esters by liposome encapsulation

Abstract

The instability of ester bonds, low water solubility, and increased cytotoxicity of flavonoid glycoside esters significantly limit their application in the food industry. Therefore, the present study attempted to resolve these issues through liposome encapsulation. The results showed that baicalin butyl ester (BEC4) and octyl ester (BEC8) have higher encapsulation and loading efficiencies and lower leakage rate from liposomes than baicalin. FTIR results revealed the location of BEC4 and BEC8 in the hydrophobic layer of liposomes, which was different from baicalin. Additionally, liposome encapsulation improved the water solubility and stability of BEC4 and BEC8 in the digestive system and PBS but significantly reduced their cytotoxicity. Furthermore, the release rate of BEC4 and BEC8 from liposomes was lower than that of baicalin during gastrointestinal digestion. These results indicate that liposome encapsulation alleviated the negative effects of fatty chain introduction into flavonoid glycosides.

Keywords:

• Liposome encapsulation
• flavonoid glycoside esters
• fatty chain
• stability
• cytotoxicity

Authors’ contributions

W. W., M. Z., and X. X. performed the conception and design of the study. W. W., X. X., M. Z., X. L. and W. B. performed experimental design, experiments, acquisition of data, and analysis and interpretation of data. X. X., X. L., and G. Z. discussed the project and provided key resources and supervised the project. W. W. and X. X. wrote the manuscript, and the final manuscript was revised and approved by all the authors.

Disclosure statement

All authors declare that they have no conflict of interest.

Additional information

Funding

This work was supported by the National Natural Science Foundation of China (21978101 and 32101937), GuangDong Basic and Applied Basic Research Foundation (2022A1515011686 and 2022A1515110710), Guangzhou Science and Technology Planning Project (202102020773), and Science and Technology Projects in Guangzhou (2023A04J0745).