Department of Biochemistry, CSIR-Central Food Technological Research Institute, Mysore, 570020, Karnataka, India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad, 201002, India.
Department of Biochemistry, CSIR-Central Food Technological Research Institute, Mysore, 570020, Karnataka, India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad, 201002, India.
Carbohydr Polym. 2021 Feb 15;254:117409. doi: 10.1016/j.carbpol.2020.117409. Epub 2020 Nov 21.
Aiming to enhance therapeutic efficiency of lutein, lutein loaded chitosan-sodium alginate (CS-SA) based nanocarrier system (LNCs) were prepared and evaluated for lutein bioavailability and pharmacokinetics in diabetic rats in comparison to micellar lutein (control). Further, cytotoxicity, cellular uptake and protective activity against HO induced oxidative stress in ARPE-19 cells were studied. Results revealed that LNCs displayed maximal lutein AUC in plasma, liver and eye respectively in normal (3.1, 2.7 and 5.2 folds) and diabetic (7.3, 3.4 and 2.8 folds) rats. Lutein from LNCs exhibited a higher half-life time, mean residence time and slow clearance from the plasma, indicating prolonged circulation compared to control. In ARPE-19 cells, pre-treatment with LNCs (10 μM) have significantly attenuated HO induced cell death, intracellular ROS and mitochondrial membrane potential compared to control. In conclusion, LNCs improve the lutein bioavailability in conditions like diabetes, diabetic retinopathy and cataract to curtail oxidative stress in retinal cells.
提高叶黄素的治疗效率,将叶黄素负载于壳聚糖-海藻酸钠(CS-SA)纳米载体系统(LNCs)中,并与胶束叶黄素(对照)相比,评估其在糖尿病大鼠中的叶黄素生物利用度和药代动力学。此外,还研究了细胞毒性、细胞摄取以及对 ARPE-19 细胞中 HO 诱导的氧化应激的保护作用。
结果表明,与正常大鼠相比,LNCs 在糖尿病大鼠的血浆、肝脏和眼睛中分别显示出最大的叶黄素 AUC(分别为 3.1、2.7 和 5.2 倍)。与对照相比,LNCs 中的叶黄素半衰期更长,平均滞留时间更长,从血浆中清除速度更慢,表明其循环时间延长。在 ARPE-19 细胞中,与对照相比,LNCs(10 μM)预处理可显著减轻 HO 诱导的细胞死亡、细胞内 ROS 和线粒体膜电位。
总之,LNCs 可提高糖尿病、糖尿病性视网膜病变和白内障等情况下叶黄素的生物利用度,以减少视网膜细胞的氧化应激。