Development of Stable Liposomal Drug Delivery System of Thymoquinone and Its In Vitro Anticancer Studies Using Breast Cancer and Cervical Cancer Cell Lines

Abstract

Thymoquinone, a well-known phytoconstituent derived from the seeds of Nigella sativa, exhibits unique pharmacological activities However, despite the various medicinal properties of thymoquinone, its administration in vivo remains challenging due to poor aqueous solubility, bioavailability, and stability. Therefore, an advanced drugdelivery system is required to improve the therapeutic outcome of thymoquinone by enhancing its solubility and stability in biological systems. Therefore, this study is mainly focused on preparing thymoquinone-loaded liposomes to improve its physicochemical stability in gastric media and its performance in different cancer cell line studies. Liposomes were prepared using phospholipid extracted from egg yolk. The liposomal nano preparations were evaluated in terms of hydrodynamic diameter, zeta potential, microscopic analysis, and entrapment efficiency. Cell-viability measurements were conducted using breast and cervical cancer cell lines. Optimized liposomal preparation exhibited polygonal, globule-like shape with a hydrodynamic diameter of less than 260 nm, PDI of 0.6, and zeta potential values of −23.0 mV. Solid-state characterizations performed using DSC and XRPD showed that the freeze-dried liposomal preparations were amorphous in nature. Gastric pH stability data showed no physical changes (precipitation, degradation) or significant growth in the average size of blank and thymoquinone-loaded liposomes after 24 h. Cell line studies exhibited better performance for thymoquinone-loaded liposomal drug delivery system compared with the thymoquinone-only solution; this finding can play a critical role in improving breast and cervical cancer treatment management.

Self-micellizing solid dispersion of thymoquinone with enhanced biopharmaceutical and nephroprotective effects

“…It was hypothesized that the apparent absorption rate of TQM in the orally-dosed SMSD-TQM group was faster with a shorter T max , possibly due to the rapid dissolution of TQM via the SMSD approach. Since TQM has high membrane permeability (Shariare et al., 2022 ), the improved dissolution and sufficiently high supersaturation of TQM could contribute to the quick absorption that can prevent the precipitation or degradation of TQM in the GI tract. However, further investigation into the absorption mechanism of micellar TQM is required before a plausible hypothesis can be proposed (Morgen et al., 2012 ).…”

Inhibitory effects evaluation of Thymoquinone and Nanoliposome formulation against Candida parapsilosis isolates

“…Hence, to increase the activity of TQ, a liposomal formulation was investigated. Because of the low solubility in water, encapsulation of TQ not only solves this problem but also improves the e ciency of TQ due to its gradual release from the nanoliposomal structure [24]. On the other hand, the development of biosynthesized NPs can signi cantly reduce drug-resistant attribute to infectious of candidiasis, which have been shown in various studies.…”

Current development of theragnostic nanoparticles for women’s cancer treatment

“…The stability study data demonstrate that the liposomal preparation of thymoquinone is physico-chemically stable in both water and gastric pH 1.2. Therefore, this study suggests that developing liposomal preparations of hydrophobic, poorly soluble, and unstable ingredients like thymoquinone can enhance their in vivo performance and physicochemical stability to treat cervical cancer and other similar conditions (Shariare et al 2022).…”