Challenges in Coopted Hydrophilic and Lipophilic Herbal Bioactives in the Same Nanostructured Carriers for Effective Bioavailability and Anti-Inflammatory Action.

ABSTRACT

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.