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Background: Plant flavonoids such as quercetin are useful for both the therapeutic and preventive care of a variety of illnesses. Nevertheless, their antitumor efficacy against KON oral cancer is still unknown. Therefore, the aim of this investigation was to examine quercetin's anti-growth, anti-migrative, and anti-invasive characteristics. The cell cycle arrest property and mitochondrial function disruption of quercetin were also investigated. Additionally, the cellular mechanism responsible for inducing apoptosis and the anti-metastasis mechanism were identified. Methods: KON cells were treated with quercetin in order to test the anticancer activity of this compound. The MTT colorimetric assay was used to examine the cell viability of the treated cells in comparison to MRC-5 fibroblast cells. After being exposed to the detrimental effects of quercetin, the morphology of the KON cells was examined using DAPI and FDA double staining, as well as Hoechst 33,258 and AO double staining. Annexin V-FITC with a flow cytometer and DCFDA labeling were used to detect apoptosis induction and the ROS production associated with cell death. Quercetin's ability to stop the cell cycle was evaluated via PI staining and the flow cytometer. The examination included anti-proliferative, anti-migration, and anti-invasion activities. Values for the transepithelial electrical resistance, or TEER, were measured. Ultimately, the mechanisms of action of the apoptotic markers and genes implicated in the metastatic process were clarified. Results: Quercetin treatment reduced the vitality of KON cells and had minimal effect on MRC cells. Following quercetin treatment, the characterization of apoptosis and cell death in KON cells was observed. When quercetin was applied to KON cells, the generation of ROS increased. Furthermore, it was discovered that quercetin increased the percentage of dead cells and cell cycle arrests in the S and G2/M phases. Moreover, quercetin inhibited KON cells' capacity for migration and invasion in addition to their effects on cell stability and structure. As a result of identifying the mechanism responsible for inducing apoptosis and preventing metastasis, quercetin was found to downregulate the expression of BCL-2/BCL-XL while increasing the expression of BAX. TIMP-1 expression was upregulated while MMP-2 and MMP-9 were downregulated. Quercetin's anticancer properties and specific mechanisms of action in relation to KON cells were clarified. Conclusion: Quercetin is greatly cytotoxic in oral cancer cells, triggering cells undergoing apoptosis and ROS-mediated cell death, possessing S and G2/M cell cycle arrest properties, and exhibiting anti-metastatic activities. Finally, this discovery opens up a wide range of possibilities for developing an anti-oral cancer drug and further investigating its effectiveness in vivo and in clinical trials as an alternative cancer treatment. [ABSTRACT FROM AUTHOR]

Solvent exchange-induced in situ-forming gel (isg) and in situ-forming microparticles (ism) have been currently applied as drug delivery approaches for periodontitis treatment. Doxycycline hyclate-loaded Eudragit RS-based isg and ism were prepared in this study. The basic properties such as density, pH, surface/interfacial tension of their solvents including dimethyl sulfoxide (DMSO), N-methyl pyrrolidone (NMP), and 2-pyrrolidone (PYR) in Eudragit RS solution and oils (olive oil and camellia oil) were assessed. This research also tested for apparent viscosity of solvent and drug-free and doxycycline hyclate-loaded ERS-based isg and ism, and their phase transformation rates. Density of PYR was higher than that of DMSO whereas these solvents exhibited the less wettability than oils on glass slide. All fabricated doxycycline hyclate-loaded Eudragit RS-based ism formulations showed good emulsion physical stability with no phase separation for 1 hour. The apparent viscosity of ism was significantly less than that of isg. DMSO-based isg and ism exhibited a significantly less viscosity than that of PYR-based formulations. Rapid phase inversion was evident after isg and ism exposure to agarose gel indicating fast solvent exchange. The loose barrier of camellia oil from its less viscosity facilitated a water diffusion inward Eudragit RS-based ism easier than using viscous olive oil. Solvent exchange-induced doxycycline hyclate-loaded Eudragit RS-based ism using DMSO as the solvent and camellia oil as the continuous phase exhibited various appropriate physicochemical characteristics for applying as drug delivery system for periodontitis treatment. [ABSTRACT FROM AUTHOR]

An injectable in situ-forming gel (ISG) is a promising approach as a drug delivery system. In this study, natural resins including aloe, benzoin and propolis dissolved in N-methyl pyrrolidone (NMP) and dimethyl sulfoxide (DMSO) were investigated as ISG systems for their ability to form matrices in phosphate buffer. Regarding their functions as ISG, their pH values, viscosities, flow behaviours, surface tensions and injectabilities were tested. Benzoin and propolis exhibited greater matrix formation than aloe, owing to their higher resin contents. Benzoin and propolis in DMSO formed matrices with a faster solvent exchange rate compared with those in NMP. The former had a higher viscosity than the latter, but both of them exhibited similar densities and surface tensions. The 35% and 40% w/w benzoin in DMSO exhibited dominant matrix formations with acceptable injectability via syringe. The 35% w/w benzoin and propolis ISG in DMSO efficiently inhibited the growth of Staphylococcus aureus strains, and the propolis ISG also exhibited a clear inhibition zone against Porphyromonas gingivalis, whereas aloe did not. From the cell viability assay, propolis exhibited a higher toxicity against HCT116 colon cancer cells (IC50=95 μg/ml) compared with benzoin (IC50=400 μg/ml), whereas the resin from aloe showed no toxic effect on this cell. Due to their rapid insoluble matrix formation after contacting aqueous fluid as well as their antibacterial and cytotoxic activities against colon cancer cell, the 35% w/w benzoin and propolis in DMSO have the potential for use as a matrix former for ISGs. [ABSTRACT FROM AUTHOR]