Preparation and in vivo pharmacokinetics study of baicalin encapsulated glycyrrhizaprotein nanoparticles
OBJECTIVE To prepare baicalin encapsulated glycyrrhiza protein nanoparticles and explore their in vivo pharma-cokinetics.METHODS Baicalin encapsulated glycyrrhiza protein nanoparticles were prepared by pH-agglomeration method.Taking the dosage of baicalin and glycyrrhiza protein,as well as pH value as influencing factors,encapsulation efficiency of baicalin and size of nanoparticle as evaluation parameters,the preparation of baicalin encapsulated glycyrrhiza protein nanoparticles was optimized with Box-Behnken design.After optimization,morphology,encapsulation efficiency,drug loading,particle size distribution and polydispersity of nanoparticles were determined.Then in vivo pharmacokinetics of baicalin encapsulated glycyr rhiza protein nanoparticles were examined.Briefly,free baicalin and nanoparticles were given to rats orally and the plasma concen-trations of baicalin in rats at different timepoints were determined by high performance liquid chromatography-tandem mass spec-trometry(HPLC-MS).RESULTS The baicalin encapsulated glycyrrhiza protein nanoparticles prepared by the optimal prescrip-tion were spherical with a particle size of 212.3 nm.The nanoparticles were uniform with an excellent dispersibility and drug load-ing capacity and encapsulation efficiency were 9.1％and 81.8％respectively.For in vivo pharmacokinetics studies,both nanopar ticles and free baicalin conformed to the pharmacokinetic two-chamber model in rats.As compared with free baicalin,Cmaxand AUC0-t of nanoparticles rose obviously.CL declined(P＜0.01)and oral bioavailability spiked to 2.36 folds.CONCLUSION The preparation process of glycyrrhiza protein nanoparticles is simple with a high drug loading capacity.As a novel drug delivery system,it improves oral absorption efficiency of baicalin.
baicalinglycyrrhiza protein nanoparticlespH-agglomeration methodin vivo pharmacokinetics
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