Thymoquinone (TQ), a phytochemical compound found in Carum carvil seeds (C. carvil), has a lot of applications in medical especially cancer therapy. However, TQ has a hydrophobic nature, and because of that, its solubility, permeability and its bioavailability in biological mediums are poor. To diminish these drawbacks, we have designed a herbal carrier composed of Ergosterol (herbal lipid), Carum carvil extract (Carum) and nonionic surfactants for herbal cancer treatment. C. carvil was extracted and characterized by GC/Mass. Two different formulations containing TQ and Carum were encapsulated into niosomes (Nio/TQ and Nio/Carum, respectively) and their properties were compared together. Morphology, size, zeta potential, encapsulation efficiency (EE%), profile release rate, in vitro cytotoxicity, flow cytometric, DNA fragmentation and cell migration assay of formulations were evaluated. Results show that both loaded formulations have a spherical morphology, nanometric size and negative zeta potential. EE% of TQ and Carum loaded niosomes was about 92.32% ± 2.32 and 86.25% ± 1.85, respectively. Both loaded formulations provided a controlled release compared with free TQ. MTT assay showed that loaded niosomes have more anti-cancer activity compared with Free TQ and free Carum against MCF-7 cancer cell line and these results were confirmed by flow cytometric analysis. Cell cycle analysis showed G2/M arrest in TQ, Nio/TQ and Nio/Carum formulations. TQ, Nio/TQ and Nio/Carum decreased the migration of MCF7 cells remarkedly. These results show that the TQ and Carum loaded niosomes are novel carriers with high efficiency for encapsulation of low soluble phytochemicals and also would be favourable systems for breast cancer treatment.
27 May 2019 in DARU Journal of Pharmaceutical Sciences
An efficient gene delivery system has some critical factors that enhance the efficiency of nanocarrier. These factors are low production cost, high bioavailability, high encapsulation efficiency, controllable release, and targeting ability. Niosome (the nonionic surfactant vesicles) was considered as a promising gene delivery system. Niosome can increase stability and uptake of active agents. We used all mentioned factors in one optimized formulation entitled plasmid-loaded magnetic niosomes (PMN). To increase the bioavailability of niosomes, we used ergosterol (a natural lipid) instead of cholesterol in structure of niosome. Also, cetyl trimethyl ammonium bromide (CTAB) in different concentrations was used to improve encapsulation of plasmid and compared to niosomes that did not have CTAB (negative niosome). Afterward, magnetic nanoparticle (Fe3O4@SiO2) was synthesized and loaded into niosome to obtain targeting ability. Prepared formulations were evaluated regarding size, zeta potential, morphology, encapsulation of magnetic nanoparticles and plasmid (Pm-cherry-N1), release rate, and transfection efficiency. Results demonstrated that optimum formulation (Nio/CTAB3%/Fe/P) has a nanometric size (118 +/- 2.31 nm, positive zeta potential (+25 +/- 0.67 mV), high loading of plasmid (72%), and good gene expression (35%). Interestingly, after applying a magnetic field below the cell plate, we obtained ac increased gene expression from 35% to 42%. These results showed that this new formulation would have a promising future and also can be used for delivering the other drugs and active agents.