Studies On Supramolecular Extract Of Andrographis- Loaded Micelles

Andrographis is one of commonly used cleaning heat and detoxificating Chinese herbal medicine. Modern research shows that Andrographis has significant anti-tumor effect. It's major active ingredient is andrographolide,dehydroandrographolide and 14-deoxyandrographolide. andrographolide and dehydroandrographolide are important indicators of the quality inspection in the 2010 edition Chinese Pharmacopoeia.By using supermolecule techniques to enrich ethanol extract of Andrographis paniculata, Han Guang obtained supramolecular extract of Andrographis (SEA), which contained more than 50% of andrographolides.The topic was based on SEA to prepare micelles,which used modern targeting drug delivery system technology,and took poloxamer 188 as carrier material. The SEA-loaded micelles were prepared by thin-film hydration method.The entrapment efficiency was taken as the index to evaluate the effects of the amount of SEA,volume of water phase,temperature of rotary evaporation,and pH of water phase on the characteristics of micelles.Chosing the most influential three factors: the amount of SEA,volume of water phase,temperature of rotary evaporation,to design Orthogonal experiment, the final optimized formulation was 15mg of Andrographis supramolecular extract,120mg ploxamer 188 and 8mL of water phase.The optimized supramolecular micelles solution was uniform and clear : arerage particle size was 198nm;entrapment efficiency was (85.7±2.1)% ;drug loading was (3.9±0.1)% . Compared with SEA solution,in vitro release results of SEA-loaded micelles indicated that the drug release slowly from micelles.Using the original extract as the control group, giving tail vein injection, measuring the concentration of andrographolide and dehydroandrographolide in the organization at different time an d comparing it with the original drug to evaluate the tissue distribution characteristics. The results showed that the relative increase in the concentration of liver and lung was more significant compared with the PEG original drug, so it was beneficial to the treatment of liver cancer and lung cancer.The results showed that poloxamer188 micelle as the carrier of insoluble drugs can improve the targeting of specific tissues.