Depressant effect of resveratrol nanoemulsion on human heptoma line HepG2 cells
April 11, 2012Hepatocellular carcinoma is one of the most common and most malignant tumor diseases. It ranks 5th among the global incidence of malignant tumors. In Chinese cancer mortality, it ranks 2nd. Side effects of chemical medicine and radiotherapy large restrict its clinical applications. Using the natural anti-cancer agents to observe the anti-tumor effect and explore their possible anti-cancer mechanisms has become a research hotspot in recent years. It has broad application prospects.
Resveratrol is a phytoalexin existing widely in plants such as polygonum cuspidatum, grapes, peanuts and peanut. It is a plants filling when the plant in face of fungal infections, ultraviolet radiation and other adverse conditions. Because of the role of anti-platelet aggregation, antioxidant has long been used in the treatment of cardiovascular disease. Recent studies have found that resveratrol can inhibit the proliferation of liver cancer, breast cancer, prostate cancer, skin cancer, colon and leukemia cancer cells, induction of apoptosis, and selective for tumor cells in the carcinogenic effects The three main stages of chemical anti-cancer activity. However, resveratrol is insoluble in water, the short half-life, low bioavailability, limiting its application.
The nanoemulsion is an ideal drug delivery system, which is characterized by dispersion, soluble the drug which is insoluble in water. It can help absorb, increase bioavailability of the drug, extend the duration of drugs action. It has great potential and broad prospects for development. Resveratrol preparation nanoemulsion on cultured human hepatoma cell line HepG2 growth inhibition, anti-cancer research foundation for the nanoemulsion.
According to the nanoemulsion formation mechanism, when the surfactant hydrophilic lipophilic’s balance value is equal or close to the HLB value that oil required, it is easy to form nanoemulsion with stable physical and chemical properties. There are relatively small toxicity based on this principle and there are less vulnerable to the electrolyte, the inorganic salts and acid-base and good compatibility with other surfactants glutathione non-ionic surfactant polyoxyethylene hydrogenated castor oil. Choice of cosurfactant to adjust the HLB value of surfactant, the surfactant and the oil is easier to form a nanoemulsion cosurfactant not only used to adjust the HLB value, and resveratrol in a good solvent, so that white veratryl alcohol in the nanoemulsion of the solubility is greatly increased.
After resveratrol nanoemulsion and resveratrol bulk drugs respectively play roles in HepG2, MTT, morphological observation, HE staining and growth curve results showed that the cells showed significant apoptosis, cells became round condensed cytoplasm and nuclei condensation and apoptotic bodies; when resveratrol concentration of 4mg / L, resveratrol nanoemulsion group on the cell inhibitory rate was significantly higher than resveratrol bulk drugs group, there was significant differences. Studies have shown that resveratrol nanoemulsion inhibition of HepG2 cells was significantly, which may be due to the small particle size nanoemulsion large specific surface area, strong adsorption, adsorption on the cell surface. As the surfactant is amphiphilic molecules with hydrophilic and hydrophobic and biofilm structure very similar to the nanoemulsion is adsorbed on the cell surface and cell membrane fusion, drug release in the cell, the nanoemulsion as a drug carrier to assist white veratryl alcohol across the cell membrane, the relative drug chia seed concentration increased in the cells, thereby greatly enhancing the utilization of drugs and increasing the efficacy.
Resveratrol nanoemulsion has transparent appearance with small viscosity. The technology is feasible and reliable with good reproducibility. Small particle size and uniform distribution of the nanoemulsion will significantly inhibit the growth of human hepatoma cell line HepG2 in vitro and induce apoptosis. Its function on HepG2 growth inhibition was significantly superior to resveratrol bulk drugs.Source:http://www.cospcn.com
Posted by tracy ma. Posted In : pharmaceutical raw materials