Preparations Of Total Flavonoids Chrysanthemum Indicum(TFC)/PLGA Sustained Release Microspheres And Optimization Of Technology

Objective:The reasons of defects in jaw bone are mostly maxillofacial tumor,trauma and inflammation.Effective control affection improves the success rate of surgery,so antibiotics are necessary after the operation.Many experiments study the delivery of local antibiotic medicine,nevertheless drug toxicity should not be ignored,and they also can result in dysbacteriosis and other side effects.TFC is the principal active component with the properties of anti-inflammatory,antiviral and improving blood circulation.It was tested that the chrysanthemum indicum extract was non-poisonous.At present there are few researches about anti-inflammatory effect of chrysanthemum indicum,therefore TFC is made into sustained release microspheres for high concentrations of continuous dosing in local drug delivery and reducing the side effect of antibiotics.PLGA are widely used in medicine and material areas with properties of favorable biocompatibility and film-forming ability.The entrapment efficiency was taken as an index to optimize the conditions such as stirring rate,PVA concentration and rate of charge in order to prepare safer and better anti-inflammatory effect medicine in oral treatment.Methods:(1)The TFC/PLGA microspheres were prepared by using emulsion method.(2)Preparation technology with different single factor conditions were optimized, such as the stirring rate,PVA concentration and rate of charge by observing the evaluation index of entrapment efficiency.The general morphology of the microspheres was observed by microscope,the surface morphology and particle size of the microspheres were observed by SEM.(3)The encapsulation efficiency and in vitro release results of the microspheres were measured by UV spectrophotometer.Results:When stirring rate was 3000r/min,PVA concentration was 3%,and rate of charge was 1:15 under the optimal conditions,the acquired TFC/PLGA microspheres showed well-defined properties,with uniform sphere in appearance,general particles without adhesion,the entrapment efficiency of45.03±1.25% and the mean diameter of 102.20±1.97μm.The results showed that the initial release was 22.07%,the cumulative drug release ratio was 92.32% within 20 d,with significant sustained-release effect.Conclusion:TFC/PLGA microspheres were prepared by the double emulsion solvent evaporation method.TFC/PLGA microspheres with suitable size, uniform dispersion,high encapsulation efficiency and sustained effect of in vitro release can be acquired under the optimized condition.But the bacteriostasis and feasibility of application need to be further researched.