Preparation and Evaluation of Curcumin Derivatives Nanoemulsion Based on Turmeric Extract and Its Antidepressant Effect

姜黄素 药代动力学 生物利用度 药理学 姜黄 化学 抗坏血酸 抗抑郁药 抗氧化剂 医学 传统医学 食品科学 生物化学 海马体 内分泌学
作者
Lin Sheng,Yumeng Wei,Chao Pi,Cheng Ju,Zhilian Su,Yuan Yuan Wang,Tao Chen,Jie Wen,Yuxun Wei,Jingwen Ma,Jia Tang,Huiyang Liu,Zerong Liu,Hongping Shen,Ying Zuo,Wenwu Zheng,Ling Zhao
出处
期刊:International Journal of Nanomedicine [Dove Medical Press]
卷期号:Volume 18: 7965-7983 被引量:3
标识
DOI:10.2147/ijn.s430769
摘要

Purpose: The early stage of this study verified that a turmeric extract (TUR) including 59% curcumin (CU), 22% demethoxycurcumin (DMC), and 18% bisdemethoxycurcumin (BDMC), could enhance the stability of CU and had greater antidepressant potential in vitro. The objective of the study was to develop a nano-delivery system containing TUR (TUR-NE) to improve the pharmacokinetic behavior of TUR and enhance its antidepressant effect. Methods: The antidepressant potential of TUR was explored using ABTS, oxidative stress-induced cell injury, and a high-throughput screening model. TUR-NE was fabricated, optimized and characterized. The pharmacokinetic behaviors of TUR-NE were evaluated following oral administration to normal rats. The antidepressant effect of TUR-NE was assessed within chronic unpredictable mild stress model (CUMS) mice. The behavioral and biochemical indexes of mice were conducted. Results: The results depicted that TUR had 3.18 and 1.62 times higher antioxidant capacity than ascorbic acid and CU, respectively. The inhibition effect of TUR on ASP+ transport was significantly enhanced compared with fluoxetine and CU. TUR-NE displayed a particle size of 116.0 ± 0.31 nm, polydispersity index value of 0.121 ± 0.007, an encapsulation rate of 98.45%, and good release and stability in cold storage. The results of pharmacokinetics indicated the AUC (0-t) of TUR-NE was 8.436 and 4.495 times higher than that of CU and TUR, while the C max was 9.012 and 5.452 times higher than that of CU and TUR, respectively. The pharmacodynamic study confirmed that the superior antidepressant effect of TUR-NE by significantly improving the depressant-like behaviors and elevating the content of 5-hydroxytryptamine in plasma and brain in CUMS mice. TUR-NE showed good safety with repeated administration. Conclusion: TUR-NE, which had small and uniform particle size, enhanced the bioavailability and antidepressant effect of TUR. It could be a promising novel oral preparation against depression. Keywords: turmeric extract, curcuminoids, nanoemulsion, stability, antidepressant effect, 5-hydroxytryptamine
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