Effect of drug loading on the formation of insulin-contained W/O microemulsion
The advantages of microemulsion as an oral insulin carrier are its high dispersibility and reten-tion of insulin biological activity,which benefit insulin intestinal absorption.Traditional formulation screening method of insulin-contained microemulsion(ICME)usually based on the addition of insulin to the insulin-free microemulsion(IFME)after IFME formulation is determined by pseudo-ternary phase di-agram.However,as a biomacromolecule,insulin has effect on oil-water interface tension and structure,which means the pseudo-ternary phase diagram will change after adding insulin.In such situation,the stability of ICME will be impacted.In this study,pseudo-ternary phase diagrams of IFME and ICME were compared and the optimized formulation of ICME was determined.Results showed that the addition of insulin changed the microemulsion area in pseudo-ternary phase diagram and the maximum range is 56.1％.Based on ICME pseudo-ternary phase diagram,the optimal formulation of ICME was determined as Span-80 22.6％,Tween-80 9.7％,ethanol 8.1％,isopropyl myristate(IPM)40.4％and aqueous phase 19.2％(mass fraction),with a diameter of 84.25 nm.The result in this experiment is valuable for the formulation screening of drug-contained microemulsion.
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