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姜黄素羟丙基甲基纤维素固体分散体提高生物利用度及其肝保护活性。

A Hydroxypropyl Methylcellulose-Based Solid Dispersion of Curcumin with Enhanced Bioavailability and its Hepatoprotective Activity.

机构信息

College of Korean Medicine, Gachon University, Seongnam 13120, Korea.

Institute of Pharmaceutical Science and Technology and College of Pharmacy, Hanyang University, Ansan 15588, Korea.

出版信息

Biomolecules. 2019 Jul 15;9(7):281. doi: 10.3390/biom9070281.

Abstract

Curcumin is a polyphenol compound derived from the rhizomes of that exhibits antioxidant, anti-inflammatory, anticancer, and antimicrobial properties. However, its low solubility in aqueous solutions, low absorption following oral administration, and rapid degradation limit its use as a functional food material. In this study, a hydroxypropyl methylcellulose-based solid dispersion of curcumin (DW-CUR 20) was prepared and its bioavailability was evaluated. In addition, its therapeutic efficacy as a hepatoprotective agent was investigated using the model of tert-butyl hydroperoxide (t-BHP)-induced hepatocyte damage. The rat plasma pharmacokinetic study showed that the oral curcumin bioavailability of DW-CUR 20 significantly increased compared to that of non-formulated curcumin. DW-CUR 20 showed a concentration-dependent hepatocyte protective effect on t-BHP-induced HepG2 cells. DW-CUR 20 inhibited the release of lactate dehydrogenase and decreased apoptosis-related proteins such as Poly (ADP-ribose) polymerase, cleaved caspase-7 and cleaved caspase-8 on t-BHP-treated HepG2 cells. These findings suggest that DW-CUR 20 could be a promising formulation for enhancing the therapeutic efficiency of curcumin and for improving the safety.

摘要

姜黄素是一种源自 的多酚化合物,具有抗氧化、抗炎、抗癌和抗菌特性。然而,其在水溶液中的低溶解度、口服后吸收低以及快速降解限制了其作为功能性食品材料的应用。在本研究中,制备了一种基于羟丙基甲基纤维素的姜黄素固体分散体(DW-CUR 20),并评估了其生物利用度。此外,还使用叔丁基过氧化氢(t-BHP)诱导的肝细胞损伤模型研究了其作为肝保护剂的治疗效果。大鼠血浆药代动力学研究表明,DW-CUR 20 的口服姜黄素生物利用度明显高于未制剂化的姜黄素。DW-CUR 20 对 t-BHP 诱导的 HepG2 细胞具有浓度依赖性的肝细胞保护作用。DW-CUR 20 抑制 t-BHP 处理的 HepG2 细胞中乳酸脱氢酶的释放,并降低多聚(ADP-核糖)聚合酶、裂解 caspase-7 和裂解 caspase-8 等凋亡相关蛋白。这些发现表明,DW-CUR 20 可能是一种有前途的制剂,可提高姜黄素的治疗效率并提高安全性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6d53/6681311/587a21503e4e/biomolecules-09-00281-g001.jpg

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