Novel Carbon Dots Derived from Moutan Cortex Significantly Improve the Solubility and Bioavailability of Mangiferin

Abstract

Background

Mangiferin (MA), a bioactive C-glucosyl xanthone with a wide range of interesting therapeutic properties, has recently attracted considerable attention. However, its application in biomedicine is limited by poor solubility and bioavailability. Carbon dots (CDs), novel nanomaterials, have immense promise as carriers for improving the biopharmaceutical properties of active components because of their outstanding characteristics.

Methods

In this study, a novel water-soluble carbon dot (MC-CDs) was prepared for the first time from an aqueous extract of Moutan Cortex Carbonisata, and characterized by various spectroscopies, zeta potential and high-resolution transmission electron microscopy (HRTEM). The toxicity effect was investigated using the CCK-8 assay in vitro. In addition, the potential of MC-CDs as carriers for improving the pharmacokinetic parameters was evaluated in vivo.

Results

The results indicated that MC-CDs with a uniform spherical particle size of 1–5 nm were successfully prepared, which significantly increased the solubility of MA in water. The MC-CDs exhibited low toxicity in HT-22 cells. Most importantly, the MC-CDs effectively affected the pharmacokinetic parameters of MA in normal rats. UPLC-MS analysis indicated that the area under the maximum blood concentration of MA from mangiferin-MC-CDs (MA-MC-CDs) was 1.6-fold higher than that from the MA suspension liquid (MA control) after oral administration at a dose of 20 mg/kg.

Conclusion

Moutan Cortex-derived novel CDs exhibited superior performance in improving the solubility and bioavailability of MA. This study not only opens new possibilities for the future clinical application of MA but also provides evidence for the development of green biological carbon dots as a drug delivery system to improve the biopharmaceutical properties of insoluble drugs.

Graphical Abstract

Keywords:

• Moutan Cortex
• carbon dots
• mangiferin
• solubility
• bioavailability

Data Sharing Statement

The data supporting the findings of this study are available upon request from the corresponding author.

Ethics Approval

All experiments and procedures were performed according to the animal study protocol approved by the Animal Care Ethics Committee of Anhui University of Chinese Medicine. All experiments were performed in accordance with the Guidelines for Ethical Conduct in the Care and Use of Animals.

Acknowledgments

We acknowledge the support from the Department of Material Science and Information Technology, Anhui University.

Disclosure

The authors declare that they have no conflicts of interest in this work.

Additional information

Funding

This work was supported by the Natural Science Foundation of Anhui Province (2308085MH304), the National Natural Science Foundation of China (82304324), the Research Foundation of Education Bureau of Anhui Province (2022AH050472, 2023AH040101), and the High-level Talents Support Project of Anhui University of Chinese Medicine (2022rczd011).