Iordache Teodora-Alexandra, Badea Nicoleta, Mihaila Mirela, Crisan Simona, Pop Anca Lucia, Lacatusu Ioana
Faculty of Applied Chemistry and Materials Science, University POLITEHNICA of Bucharest, Polizu No 1, 011061 Bucharest, Romania.
National Research & Development Institute for Food Bioresources-IBA Bucharest, 6th Dinu Vintila Street, 021102 Bucharest, Romania.
Nanomaterials (Basel). 2021 Nov 12;11(11):3035. doi: 10.3390/nano11113035.
There is ongoing research on various herbal bioactives and delivery systems which indicates that both lipid nanocarriers and herbal medicines will be fine tunned and integrated for future bio-medical applications. The current study was undertaken to systematically develop NLC-DSG-yam extract for the improved efficacy of herbal Diosgenin (DSG) in the management of anti-inflammatory disorders. NLCs were characterized regarding the mean size of the particles, morphological characteristics, physical stability in time, thermal behaviour, and entrapment efficiency of the herbal bioactive. Encapsulation efficiency and in vitro antioxidant activity measured the differences between the individual and dual co-loaded-NLC, the co-loaded one assuring a prolonged controlled release of DSG and a more emphasized ability of capturing short-life reactive oxygen species (ROS). NLCs safety properties were monitored following the in vitro MTS ((3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) tetrazolium reduction assay) and RTCA (Real-Time Cell Analysis) assays. Concentrations less than 50 μg/mL showed no cytotoxic effects during in vitro cytotoxicity assays. Besides, the NLC-DSG-yam extract revealed a great anti-inflammatory effect, as the production of pro-inflammatory cytokines (TNF-alpha, IL-6) was significantly inhibited at 50 μg/mL NLC (e.g., 98.2% ± 1.07 inhibition of TNF-α, while for IL-6 the inhibition percentage was of 62% ± 1.07). Concluding, using appropriate lipid nanocarriers, the most desirable properties of herbal bioactives could be improved.
目前正在对各种草药生物活性成分和递送系统进行研究，这表明脂质纳米载体和草药都将得到优化并整合，以用于未来的生物医学应用。本研究旨在系统地开发NLC-DSG-山药提取物，以提高草药薯蓣皂苷元（DSG）在抗炎疾病管理中的疗效。对NLCs的颗粒平均大小、形态特征、随时间的物理稳定性、热行为以及草药生物活性成分的包封率进行了表征。通过包封效率和体外抗氧化活性来衡量单一负载和双重共负载NLC之间的差异，共负载NLC可确保DSG的延长控释以及更强的捕获短寿命活性氧（ROS）的能力。通过体外MTS（（3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四氮唑溴盐）四氮唑还原试验）和RTCA（实时细胞分析）试验监测NLCs的安全性。在体外细胞毒性试验中，浓度低于50μg/mL时未显示出细胞毒性作用。此外，NLC-DSG-山药提取物显示出很强的抗炎作用，因为在50μg/mL的NLC下，促炎细胞因子（TNF-α、IL-6）的产生受到显著抑制（例如，TNF-α的抑制率为98.2%±1.07，而IL-6的抑制率为62%±1.07）。总之，使用合适的脂质纳米载体，可以改善草药生物活性成分的最理想特性。
