Preparation And Characterization Of ASA-β-cyclodextrin Inclusion Complexes-loaded PLGA Microspheres For Sustainde Release

Objective:Choosing antipyretic analgesics-Acetylsalicylic acid(ASA) as target drug,to prepare ASA- β-cyclodextrin inclusion complexes firstly,PLGA as the carrier to prepare ASA-β-cyclodextrin inclusion complexes microspheres.And then to determinate the surface morphology,particle size,preparation condition,and in vitro release in vitro.In order to extend ASA releasa time in oral local chronic inflammatory milieu. Methods:(1)β-cyclodex trin as the carrier to prepare ASA-β-cyclodextrin inclusion complexes.(2)Prepare ASA-β-cyclodextrin inclusion complexes microspheres by emulsion-solvent evaporation method.(3)The encapsulation efficiency evaluated and studied for the optimization of condition,including stirring rate,PVA concentration, PVA volume,and rate of charge.(4)The encapsulation efficiency,particle size and surface morphology of microspheres was studied by ultraviolet-visible spectrometer and scanning electron microscope(SEM). Results:Optimum conditions:stirring speed 4000r/min, PVA concentration 3%, PVA volume 30 ml,feed ratio 1:10.By light and electron microscopy,release microspheres obtained under optimum conditions combination are round,regular and well dispersed.Some micro-holes can be seen on the surface of drug-loaded microspheres.The diameter of drug-loaded microspheres are 0.5-127.5μm.Entrapment efficiency of the microspheres is 40.08±1.05%.The results showed that the initial release was 15.25%,the cumulative drug release ratio was85.52% within 4 weeks,and sustained release obviously. Conclusion:In this study,the ASA-βCD-PLGA microspheres were prepared by emulsion-solvent evaporation method.With smooth surface, microporous structure,high encapsulation efficiency, and sustained effect of in vitro release by the optimal conditions.The method is simple.The microspheres are stable dosage of ASA.