Preparation and evaluation of dexamethasone palmitate submicron emulsion injection
Objective To prepare a dexamethasone palmitate(DMP)submicron emulsion injection and to investigate its physicochemical properties and safety.Methods The DMP submicron emulsion was prepared by high pressure homogenization method.The formulation amounts of oil phase(LCT:MCT=1∶1),egg yolk lecithin and poloxamer 188 were optimized by the response surface methodology with the particle size and entrapment efficiency as the indicators.And then the particle size,polydispersity index(PDI),Zeta potential,pH value,drug loading,entrapment efficiency,osmotic pressure,free fatty acid value,hemolysis,stability and in vitro release were evaluated respectively.Results The results showed that the optimal formulation should be composed of 5%soybean oil,5%MCT,1.2%egg yolk lecithin and 0.3%Poloxamer 188.The mean particle size,PDI,Zeta potential and pH value of DMP submicron emulsion were(188.1±2.5)nm,0.093±0.025,(-38.4±0.643)mV and 7.12±0.13.The drug loading,encapsulation efficiency and osmotic pressure were(3.96±0.05)mg·mL-1,(97.91±0.28)%and(294±1)mOsmol·kg-1,respectively.The free fatty acid value meets the quality requirements.The results of stability test showed that the product could maintain stable for 12 months at(4±2)℃under light-resistant conditions.The maximum hemolysis rate was 1.83%.The release result of DMP submicron emulsion was followed the first release equations.Conclusion The DMP submicron emulsion prepared in this study is stable,safe and have a sustained release effect.
万方数据
维普
