Self-assembled micelles enhance the oral delivery of curcumin for the management of alcohol-induced tissue injury

作者：Sha Bao, Yanqin Zhang, Jing Ye, Yujin Zhu, Rui Li, Xiaohong Xu, Quan Zhang · 发表于：Pharmaceutical Development and Technology · 年份：2021 · DOI：10.1080/10837450.2021.1950185 · 被引用次数：17 · 研究领域：Curcumin's Biomedical Applications、Alcohol Consumption and Health Effects、Phytochemicals and Antioxidant Activities

Curcumin (CUR) shows great potential in the management of alcohol-use disorders. However, the hydrophobicity and poor oral bioavailability result in the limited therapeutic efficacy of CUR against alcohol-induced tissue injury. Here, self-assembled Soluplus® micelles (Ms) were developed for the enhanced oral delivery of CUR. CUR-loaded Soluplus® micelles (CUR-Ms) were prepared using a thin-film hydration method and these micelles displayed nearly spherical shape with an average size of 62.80 ± 1.29 nm. CUR in micelles showed the greater stability, solubility and dissolution than free CUR. With the increased water solubility of CUR-Ms and P glycoprotein inhibition of Soluplus®, the absorption rate constant (Ka) and apparent permeability coefficient (Papp) of CUR-Ms in intestines was respectively 3.50 and 4.10 times higher than that of free CUR. Pharmacokinetic studies showed that CUR-Ms significantly improved the oral bioavailability of CUR. Specifically, the AUC0–∞ and Cmax of CUR-Ms were increased by 9.45 and 47.38 folds compared to free CUR, respectively. In mice with alcohol-induced tissue injury, the oral administration of CUR-Ms greatly reduced oxidative stress, and significantly defended liver and gastric mucosa from alcoholic damages. The results demonstrated CUR-Ms with good oral bioavailability could represent a promising strategy for the management of alcohol-induced tissue injury.