Research On Garcinia Glycosides Nanoemulsion

Garcinia Glycosides is to gambogic acid as lead compounds,it is a state first class anti-tumor drug of NCEs by Structure modification.Many researches show that gambogic acid has wide chart sex to fight tumor active,but its toxicity is bigger, with LD50is79.94mg/kg,95%confidence interval is62.65-98.49mg/kg,The use of the drug is restricted.The toxicity of Garcinia Glycosides is much lower than gambogic acid and its water solubility is enhanced significantly with bioavailability increased.Pharmacodynamic data displays that Garcinia Glycosides has strong inhibitory activity to human tumor cell SMMC-7721and xenograftsHL-60with nude mice.Nanoemulsion is aimed atimproving the drug targeting,slowing releasing action, increasing the efficacy and reducing drug toxic reaction.In this project, the study before formulation designing were firstly investigated,we established a complete analysis method of standards for the quality of medicines,the result of the oil-water participate coefficient was presented to demonstrate the feassibility of Garcinia Glycosides nanoemulsion.The prescription was optimized by orthofonal experiment and the best craft produce was investigated by single factor.In the stduy of Garcinia Glycosides nanoemulsion quality assessment and stability factor,we studied its content determination (0.297±0.012mg/mL),deter-mination of encapsulation percentage (98.64±0.74%),size distribution (151.0±15nm),viscosity (6.50-6.55mPa-s),pH(7-7.5),Zeta potential(-38.1±3.8mV), etc. And the stability of the nanoemulsion was evaluated by stress test,accelerated test and long-term test.Its appearance,related sub stances, content determination and size were no significant change.The safety of Garcinia Glycosides nanoemulsion was investigated by irritability test,hemolysis test and stimulation test.Conclusion: Garcinia Glycosides nanoemulsion was safe.In the pharmacokinetic experiment and tissue distribubion test,the concentration-time curves,pharmacokinetic parameters and content determination in tissues were obtained, Conclusion:Garcinia Glycosides nanoemulsion had liver,spleen,lung and kidney targeting properties,providing a reference for the further study.