Chitosan-coated mangifer in liposomes:preparation,characterization and oral pharmacokinetic evaluations
OBJECTIVE To prepare chitosan-coated mangiferin liposomes(CS-MF-Lips)and explore its drug release in vitro and pharmacokinetic behaviors.METHODS Entrapment efficiency,drug loading and particle size were selected as param-eters.Box-Behnken response surface design method was employed for examining the optimal prescriptions of CS-MF-Lips.Lyophilized powder of CS-MF-Lips was prepared and then characterized.Sprague-Dawley(SD)rats were administered intragas-trically of mangiferin and CS-MF-Lips and plasma concentration was determined.RESULTS Optimal prescriptions for CS-MF-Lips:ratio of lipid-to-drug was 15.9∶1,ratio of phospholipid-to-cholesterol 9.9∶1 and concentration of chitosan 0.18％.Aver-age entrapment efficiency of CS-MF-Lips was(85.92±1.48)％,drug loading(4.04±0.16)％,particle size(196.74±10.37)nm and Zeta potential(14.13±0.49)mV.Micro-morphology of CS-MF-Lips was elliptical and mangiferin existed as an amor-phous state in CS-MF-Lips lyophilized powder.Sustained release characteristics of CS-MF-Lips in vitro were obvious and solu-bility rose to 8.41 folds.tmax,t1/2,MRT,Cmax,AUC0-t and CL of CS-MF-Lips altered significantly when comparing with mangif-erin(P＜0.05 or P＜0.01).Oral bioavailability spiked to 420.48％.CONCLUSION CS-MF-Lips may effectively promote oral absorption.It offers rationales for pharmacodynamic evaluations.
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