Preparation, Physical Characterization, Pharmacokinetics and Anti-Hyperglycemic Activity of Esculetin-Loaded Mixed Micelles.

Abstract

Despite its low water solubility, esculetin (EC) have been described to demonstrate various health benefits. Thus, we sought to develop esculetin-loaded mixed micelles (EC-M) delivery system to purposively improve biological availability and anti-hyperglycemia activity of EC. Thin-film hydration method was employed to fabricate EC-M, amid characterization with transmission electron microscopic analysis (TEM), coupled with physical properties such as particle size (PS), poly-dispersity index (PDI), zeta-potential (ZP) and stability testing. We analyzed in-vitro release and studied EC-M pharmacokinetics in rats. The hyperglycemic mice model was established with streptozotocin (STZ) to evaluate anti-hyperglycemic activity of EC-M. The PS, PDI and ZP of EC-M were 47.97 ± 0.41 nm, 0.189 ± 0.005 and -25.55 ± 0.28 mV, respectively. The release rate of EC-M increased comparable to free EC in the three media. The oral biological availability and half-life of EC-M increased respectively by 3.06 and 1.45 folds compared to free EC. Besides, we observed 46.21% decrease in blood glucose of mice in EC-M group comparable to the model control, wherein, the anti-hyperglycemic effect of EC-M was better compared to free EC. Conclusively, EC-M may ideally serve as a novel approach to enhance biological availability and increased anti-hyperglycemic activity of EC.

• Authors: Xiaoxiao Li, Xiaoli Xia, Jian Zhang, Michael Adu-Frimpong, Xinyi Shen, Wenxiong Yin, Qing He, Wanjing Rong, Feng Shi, Xia Cao, Hao Ji, Elmurat Toreniyazov, Qilong Wang, Jiangnan Yu, Ximing Xu
• Journal: Journal of pharmaceutical sciences (J Pharm Sci) Vol. 112 Issue 1 Pg. 148-157 (01 2023) ISSN: 1520-6017 [Electronic] United States
• PMID: 35780820 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2022 American Pharmacists Association. Published by Elsevier Inc. All rights reserved.

Chemical References

• Micelles
• esculetin
• Umbelliferones
• Hypoglycemic Agents
• Drug Carriers

Topics

• Rats
• Animals
• Mice
• Micelles
• Administration, Oral
• Umbelliferones
• Solubility
• Biological Availability
• Particle Size
• Hypoglycemic Agents (pharmacology, therapeutic use)
• Drug Carriers