The State Key Laboratory of Functions and Applications of Medicinal Plants, School of Pharmaceutical Sciences, Guizhou Medical University, Guiyang 550025, China; The High Efficacy Application of Natural Medicinal Resources Engineering Center of Guizhou Province, School of Pharmaceutical Sciences, Guizhou Medical University, Guiyang 550025, China.
The First People's Hospital of Guiyang, Guiyang 550002, China.
Int J Biol Macromol. 2023 Sep 30;249:125918. doi: 10.1016/j.ijbiomac.2023.125918. Epub 2023 Jul 24.
The injury of vascular endothelial cells caused by high glucose (HG) is one of the driving factors of vascular complications of diabetes. Oral administration is the most common route of administration for the treatment of diabetes and its vascular complications. Essential oil extracts from Chinese medicine possess potential therapeutic effects on vascular endothelial injury. However, low solubility and volatility of essential oils generally result in poor oral absorption. Development of nanocarriers for essential oils is a promising strategy to overcome the physiological barriers of oral absorption. In this study, a nanoemulsion composed of bovine serum albumin (BSA)-dextran sulfate (DS) conjugate and sodium deoxycholate (SD) was constructed. The nanoemulsions were verified with promoted oral absorption and prolonged circulation time. After the primary evaluation of the nanoemulsion, essential oil from Alpinia zerumbet Fructus (EOFAZ)-loaded nanoemulsion (denoted as EOFAZ@BD/S) was prepared and characterized. Compared to the free EOFAZ, EOFAZ@BD/S increased the protective effects on HG-induced HUVEC injury in vitro and ameliorative effects on the vascular endothelium disorder and tunica media fibroelastosis in a TDM mouse model. Collectively, this study provides a nanoemulsion for the oral delivery of essential oils, which holds strong promise in the treatment of diabetes-induced vascular endothelial injury.
高血糖（HG）引起的血管内皮细胞损伤是糖尿病血管并发症的驱动因素之一。口服给药是治疗糖尿病及其血管并发症最常见的给药途径。中药精油提取物对血管内皮损伤具有潜在的治疗作用。然而，精油的低溶解度和挥发性通常导致口服吸收不良。开发精油的纳米载体是克服口服吸收生理障碍的有前途的策略。在这项研究中，构建了由牛血清白蛋白（BSA）-葡聚糖硫酸酯（DS）缀合物和脱氧胆酸钠（SD）组成的纳米乳液。纳米乳液经促进口服吸收和延长循环时间得到验证。在对纳米乳液进行初步评价后，制备并表征了姜科植物益智仁精油（EOFAZ）负载的纳米乳液（表示为 EOFAZ@BD/S）。与游离 EOFAZ 相比，EOFAZ@BD/S 增加了体外对 HG 诱导的 HUVEC 损伤的保护作用，并改善了 TDM 小鼠模型中的血管内皮功能障碍和中膜纤维化。总之，本研究为精油的口服递送提供了一种纳米乳液，在治疗糖尿病诱导的血管内皮损伤方面具有很大的应用前景。
