College of Korean Medicine, Gachon University, Seongnam 13120, Korea.
Institute of Pharmaceutical Science and Technology and College of Pharmacy, Hanyang University, Ansan 15588, Korea.
Biomolecules. 2019 Jul 15;9(7):281. doi: 10.3390/biom9070281.
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.
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。