The Reach Of Preparation, Characterization And Bioavailability Of Two High Water-Soluble Apigenin Powders

Apigenin is a kind of flavonoids compounds with many bioactivities and pharmacological activities.However,its poor solubility and low bioavailability are a major obscale for biomedical application,so the experiments are designed to prepare inclusion complex of apigenin(AP)-hydroxypropyl-β-cyclodextrin(HP-β-CD)via supercritical antisolvent(SAS)method combined with inclusion technique and to prepare apigenin-mesoporous silica nanoparticles(AP-MSN)solid dispersion by solid dispersion techniques to improve apigenin bioavailability.In this paper,the main researches and results were as follows:This article,selecting HP-β-CD as inclusion materials,applies supercritical antisolvent(SAS)method combined with inclusion technique to prepare inclusion complex of AP-HP-β-CD.The characterizations of inclusion complex of AP-β-HP-βk-CD were detected and its bioavailability was valued.The main researches and results were as follows.Firstly,the mole ratio of AP and HP-β-CD(1:1)was established by phase solubility equilibrium experiment.Secondly,combining supercritical antisolvent(SAS)method with inclusion technique and using DMF as solvent and supercritical C02 as antisolvent,the single-factor experiments were designed to investigate the precipitation pressure,precipitation temperature and concentration of AP for the influence of the load efficiency and encapsulation efficiency of the AP-HP-β-CD inclusion complex as well as its particle size.Then,the optimal conditions were obtained;these conditions included precipitation pressure of 22.5 MPa,precipitation temperature of 50 ℃ and AP concentration of 20 mg/mL.The load efficiency and encapsulation efficiency of the AP-HP-(3-CD inclusion complex,with a mean particle size of 392.13 ±7.56 nm,were 13.97%±0.17%and 93.22%±1.17%,respectively,under the optimal conditions.FTIR,1H NMR,SEM,XRD,DSC,and TG analyses were also conducted for determination of inclusion complex of AP-HP-β-CD.The results demonstrated that the inclusion complex of AP-HP-β-CD was formed in a kind of amorphous type.In addition,the DMF residue,solubility,dissolution and bioavailability were conducted,then,the experiment results showed that DMF residue in inclusion complex of AP-HP-β-CD was lower than the ICH limit(0.088%).The solubility and dissolution of inclusion complex of AP-HP-β-CD were about 152.43 times and 7.6 times of raw AP,respectively.The oral relative bioavailability of the inclusion complex increased by 6.45 times compared with that of the raw AP.In this study,the apigenin-mesoporous silica nanoparticles(AP-MSN)solid dispersion was prepared by solid dispersion technique.Based on solubility,the loading efficiency(LE)and encapsulation efficiency(EE),the experiment use the absortion of MSN and its huge specific surface area to prepare AP-MSN solid dispersion.The results showed that the AP-MSN solid dispersion was prepared at the weight ratio of 1:1 to obtain the optimum solubility.And the loading efficiency(LE),encapsulation efficiency(EE)and solubility of AP-MSN solid dispersion were 29.71%,42.27%and 25.11μg/mL,respectively.The solubility of AP-MSN solid dispersion was 5.96 times higher than that of raw AP.The characteristics of the AP-MSN solid dispersion were analyzed using SEM,TEM,BET,FTIR,XRD,DSC and TG The results of SEM and TEM showed that the AP-MSN solid dispersion was regular sphere.The analysis of FTIR,XRD,DSC and TG demonstrated that AP was almost absorbed into the pore of MSN and formed in amorphous type.In addition,the experiment of DMF residue in AP-MSN solid dispersion,dissolution and bioavailability were also carried out.The results showed that DMF residue in AP-MSN solid dispersion meet the ICH limit(0.088%).The dissolution experiment result implied that the AP-MSN solid dispersion have effect on control release of AP.And the oral relative bioavailability of AP-MSN solid dispersion increased by 8.32 times compared with that of the raw AP.In addition,in this paper,the two kinds of AP powders were compared and analyzed in purity,solubility and oral relative bioavailability.It is concluded that the solubility of AP-MSN solid dispersion was lower than that of inclusion complex of AP-HP-β-CD,but its purity and oral relative bioavailability were superior to inclusion complex of AP-HP-β-CD.So,they have their own advantages and both of them have better reference value and application value.