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Thymoquinone-Loaded Soy-Phospholipid-Based Phytosomes Exhibit Anticancer Potential against Human Lung Cancer Cells.

ABSTRACT: Thymoquinone (TQ), a natural polyphenol, has been associated with various pharmacological responses; however, low bioavailability of TQ limits its clinical application. Thus, a novel phytosomal delivery system of TQ-Phospholipon® 90H complex (TQ-phytosome) was developed by refluxing combined with anti-solvent precipitation. This TQ delivery system was optimized by a three-factor, three-level Box-Behnken design. The optimized TQ-phytosome size was (45.59 ± 1.82 nm) and the vesicle size was confirmed by transmission electron microscopy. The in vitro release pattern of the formulation indicated a biphasic release pattern, where an initial burst release was observed within 2 h, followed by a prolonged release. A remarkable increase in dose-dependent cytotoxicity was evident from the significant decrease in IC50 value of TQ-phytosomes (4.31 ± 2.21 µM) against the A549 cell line. The differential effect of TQ-phytosomes in cell cycle analysis was observed, where cancer cells were accumulated on G2-M and pre-G1 phases. Furthermore, increased apoptotic induction and cell necrosis of TQ-phytosomes were revealed with the annexin V staining technique via activation of caspase-3. In reactive oxygen species (ROS) analysis, TQ-phytosomes acted to significantly increase ROS generation in A549 cells. In conclusion, the sustained release profile with significantly-improved anticancer potential could be obtained with TQ by this phytosomal nanocarrier platform.

SUBMITTER: Alhakamy NA

PROVIDER: S-EPMC7463966 | biostudies-literature | 2020 Aug

REPOSITORIES: biostudies-literature

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Thymoquinone-Loaded Soy-Phospholipid-Based Phytosomes Exhibit Anticancer Potential against Human Lung Cancer Cells.

Alhakamy Nabil A NA Badr-Eldin Shaimaa M SM A Fahmy Usama U Alruwaili Nabil K NK Awan Zuhier A ZA Caruso Giuseppe G Alfaleh Mohamed A MA Alaofi Ahmed L AL Arif Faris O FO Ahmed Osama A A OAA Alghaith Adel F AF

Pharmaceutics 20200812 8

Thymoquinone (TQ), a natural polyphenol, has been associated with various pharmacological responses; however, low bioavailability of TQ limits its clinical application. Thus, a novel phytosomal delivery system of TQ-Phospholipon<sup>®</sup> 90H complex (TQ-phytosome) was developed by refluxing combined with anti-solvent precipitation. This TQ delivery system was optimized by a three-factor, three-level Box-Behnken design. The optimized TQ-phytosome size was (45.59 ± 1.82 nm) and the vesicle size ...[more]

PMID: 32806507

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Project description:Phytochemical nanoemulsions, such as thymoquinone nanoemulsions (TQN), are regarded as innovative alternatives to antimicrobials that significantly improve the performance, digestion, antioxidant potential and immunity of rabbits. Thus, the potential effects of TQN on growth, digestibility, antioxidant potential, immunity and resistance against Pasteurella multocida (P. multocida) in rabbits were assessed. Herein, 240 rabbits were offered either a basal diet or diets fortified with three TQN-graded concentrations. At 60 days of age, rabbits were challenged with multidrug-resistant (MDR) virulent P. multocida strain. Our outcomes described that dietary inclusion of TQN, especially at higher concentrations, significantly enhanced the growth performance of rabbits, which was supported by increasing the levels of jejunal lipase, amylase and trypsin enzymes. Of note, the levels of muscle and jejunal antioxidant enzymes [superoxide dismutase (SOD), glutathione peroxidase (GPX), catalase (CAT) and total antioxidant capacity (T-AOC)], serum immunological markers (IgG, IgG, IgM and total Igs) and blood phagocytic percentage were significantly provoked after TQN fortification; meanwhile, the levels of muscle and jejunal MDA, serum biochemical parameters (total cholesterol, TG and LDL), abdominal fat percentage, breast and thigh cholesterol were significantly decreased following TQN supplementations. Our findings showed that TQN protected rabbits against P. multocida experimental challenge as evidenced by reducing P. multocida counts in rabbits' lungs, downregulating the transcription levels of P. multocida virulence-related genes (ptfA, toxA and nanB) at 48 and 96 h post-infection and ameliorating the expression levels of cytokines-related genes (IL-1β, IL-10, IL-8, IL-6, DEFB1, TNF-α, TLR-4 and TLR-2) at 96 h post-infection. Our findings suggest the utilization of TQN in rabbits' diets due to their stimulating effects on digestibility as well as their growth-promoting, anti-inflammatory, antioxidant, antibacterial, anti-virulence and immunostimulant properties, which enhance the rabbits' P. multocida resistance.

Dataset Information

Thymoquinone-Loaded Soy-Phospholipid-Based Phytosomes Exhibit Anticancer Potential against Human Lung Cancer Cells.

Publications

Thymoquinone-Loaded Soy-Phospholipid-Based Phytosomes Exhibit Anticancer Potential against Human Lung Cancer Cells.

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