RETRACTED: 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.

Optimization of Thymoquinone-Loaded Self-Nanoemulsion for Management of Indomethacin-Induced Ulcer

“… 7 Since For hundreds of years, thymoquinone (TQ) has been commonly used for conditions ranging from a simple migraine to illnesses such as obesity, asthma, gastrointestinal problems, menstruation and lactation. 8 , 9 TQ is a member of the Ranunculaceae family, rising on Mediterranean coastal plants. Almond oil (AO) is a colloidal liquid containing proteins, minerals and vitamins.…”

“…It is suggested that oxygen radicals may contribute to the formation of ethanol-induced gastric mucosal lesions, and antioxidants are protective against the damage caused by these oxidants. 7 , 19 …”

Thymoquinone, as a Novel Therapeutic Candidate of Cancers

“…It also showed the ability to suppress the ERK1/2 signaling pathway, which inhibited the migration and invasion of A549 cells [ 66 ]. TQ combined with a developed delivery system (TQ-phytosome) induced apoptosis at 4.31 ± 2.21 µM via the activation of caspase-3 and generation of reactive oxygen species (ROS), in addition to accumulating cells on G2-M and pre-G1 phases in the A549 cell line [ 67 ]. TQ enhanced apoptosis by increasing the Bax/Bcl2 ratio and upregulating the p53 expression in A549 cells [ 11 ] and mice [ 68 ].…”

Optimized Icariin Cubosomes Exhibit Augmented Cytotoxicity against SKOV-3 Ovarian Cancer Cells

“…The analysis of variance (ANOVA) was used to statistically investigate the data to evaluate the significance of the studied variables. Interactions between the independent variables were assessed from the generated contour plots and interaction plots [ 25 ]. The best fitting model was selected based on an adequate precision ratio and the predicted and adjusted determination coefficients for the measured response.…”