Encapsulation of gingerol into nanoliposomes: Evaluation of in vitro anti-inflammatory and anti-cancer activity.

Nanoliposomes (NLs) are ideal carriers for delivering complex molecules and phytochemical products, but ginger by-products, despite their therapeutic benefits, have poor bioavailability due to their low water solubility and stability. Crude ginger extracts (CGEs) and 6-gingerol were individually encapsulated within NLs for in vitro activity assessment. In vitro evaluation of anti-proliferative and anti-inflammatory properties of encapsulated 6-gingerol and CGE was performed on healthy human periodontal ligament (PDL) fibroblasts and MDA-MB-231 breast cancer cells. Encapsulation efficiency and loading capacity of 6-gingerol reached 25.23% and 2.5%, respectively. NLs were found stable for up to 30 days at 4°C with a gradual load loss of up to 20%. In vitro cytotoxic effect of encapsulated 6-gingerol exceeded 70% in the MDA-MB-231 cell line, in a comparable manner with non-encapsulated 6-gingerol and CGE. The effect of CGE with an IC50 of 3.11 ± 0.39, 7.14 ± 0.80, and 0.82 ± 0.55 µM and encapsulated 6-gingerol on inhibiting IL-8 was evident, indicating its potential anti-inflammatory activity. Encapsulating 6-gingerol within NLs enhanced its stability and facilitated its biological activity. All compounds, including vitamin C, were equivalent at concentrations below 2 mg/mL, with a slight difference in antioxidant activity. The concentrations capable of inhibiting 50% of 2,2-diphenyl-1-picrylhydrazyl (DPPH) substrate were comparable.

Preparation, Characterization, Wound Healing, and Cytotoxicity Assay of PEGylated Nanophytosomes Loaded with 6-Gingerol.

BACKGROUND: Nutrients are widely used for treating illnesses in traditional medicine. Ginger has long been used in folk medicine to treat motion sickness and other minor health disorders. Chronic non-healing wounds might elicit an inflammation response and cancerous mutation. Few clinical studies have investigated 6-gingerol's wound-healing activity due to its poor pharmacokinetic properties. However, nanotechnology can deliver 6-gingerol while possibly enhancing these properties. Our study aimed to develop a nanophytosome system loaded with 6-gingerol molecules to investigate the delivery system's influence on wound healing and anti-cancer activities. METHODS: We adopted the thin-film hydration method to synthesize nanophytosomes. We used lipids in a ratio of 70:25:5 for DOPC(dioleoyl-sn-glycero-3-phosphocholine): cholesterol: DSPE/PEG2000, respectively. We loaded the 6-gingerol molecules in a concentration of 1.67 mg/mL and achieved size reduction via the extrusion technique. We determined cytotoxicity using lung, breast, and pancreatic cancer cell lines. We performed gene expression of inflammation markers and cytokines according to international protocols. RESULTS: The synthesized nanophytosome particle sizes were 150.16 ± 1.65, the total charge was -13.36 ± 1.266, and the polydispersity index was 0.060 ± 0.050. Transmission electron microscopy determined the synthesized particles' spherical shape and uniform size. The encapsulation efficiency was 34.54% ± 0.035. Our biological tests showed that 6-gingerol nanophytosomes displayed selective antiproliferative activity, considerable downregulation of inflammatory markers and cytokines, and an enhanced wound-healing process. CONCLUSIONS: Our results confirm the anti-cancer activity of PEGylated nanophytosome 6-gingerol, with superior activity exhibited in accelerating wound healing.

High risk of drug toxicity in social isolation stress due to liver dysfunction: Role of oxidative stress and inflammation.

BACKGROUND: Previous studies have shown that social isolation stress (SIS) could associate with several systemic diseases; however, the role of SIS on liver dysfunction has yet to be established. This study aimed to investigate the effect of SIS on liver function and possible drug toxicity through liver inflammation and oxidative stress. METHODS: Male Naval Medical Research Institute mice in two groups of SIS and control were treated with typical anti-depressant and anxiolytic agents including fluoxetine, norfluoxetine, desipramine, and imipramine in both groups. Then blood concentrations (or their active metabolites) of these drugs were assessed. Liver function test, including aspartate transaminase (AST), alanine aminotransferase (ALT), total bilirubin, and conjugated bilirubin), oxidative activity, inflammatory cytokines, and the gene expression of cytochrome P450 enzymes were assessed. RESULTS: We observed that the liver enzymes including AST and ALT was slightly higher in SIS animals. The blood concentrations of fluoxetine, norfluoxetine, desipramine, and imipramine were significantly higher in SIS animals. The gene expression of CYP1A2, CYP2A6, CYP2C9, CYP2C29, and CYP2D were significantly decreased in SIS animals. Our results showed that SIS animals had significantly higher level of tumor necrosis factor-α, interleukin-1ß, and interleukin-6. SIS could significantly decrease the activity of antioxidant agent (Glutathione). CONCLUSION: We hypothesized that SIS could induce liver dysfunction and decrease the rate of drug clearance through liver inflammation and oxidative stress; therefore, the blood concentration of anti-depressant/anxiolytic agents should closely monitor in SIS due to the high toxicity of these agents.

SARS-CoV-2; What We Know so far.

A recent outbreak of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has affected more than 1100000 (April 5, 2020) individuals worldwide and is spreading rapidly. The virus is reported to be derived from bats and the infection was first reported in China. Similar to the severe acute respiratory syndrome and the Middle East respiratory syndrome coronaviruses, it is responsible for respiratory tract infection. Real time polymerase chain reaction and radiography are the two main diagnostic methods. Guidelines from the Center for Disease Control and Prevention and the World Health Organization (WHO) should be followed for diagnostic and precautionary measures. Treatment of the infection is still not available; however, antivirals are under clinical trials.