Study On The Mechanism Of Solution And Efficiency Of Baicalin By Nano Sponge Based On β-cyclodextrin

Baicalin(BA)has a wide range of pharmacological effects and has a significant effect in clinical application,but its bioavailability is low when used alone,and it is not easy to be absorbed in the gastrointestinal tract.Nanosponge(NS)not only has a good solubilization effect on insoluble drugs,but also can significantly increase drug efficacy and improve drug bioavailability,which can be widely used in the field of medicine.Based on the cyclodextrin modification technology,our research group has a certain research foundation.Combined with the existing conditions and equipment in the laboratory,BA-NS was prepared for the first time with BA as the research object.The physicochemical properties,safety and antibacterial activity in vitro were discussed.The feasibility of NS as a new drug delivery system for BA was analyzed.Firstly,the research group determined the method of phenol and BA in vitro according to the literature research and the laboratory conditions.The melting method and the stirring freeze-drying method were selected to prepare NS and BA-NS respectively.The preparation process of NS and BA-NS was optimized by BoxBehnken optimization design method.According to the existing instrument conditions in the laboratory,the optimum parameters of NS are: the molar ratio of β-CD and DPC of 1:4,the reaction temperature of 92℃,the reaction time of 4.6 h,the stirring speed of500 rpm,the washing method and times are washed three times with hot ethanol firstly,and then washed 3 times with hot water(60℃).The results showed that the phenol content was 0.21 ± 0.012% and the particle size was 254.4 ± 11.30 nm.The optimum parameters of BA-NS: the ratio of mass of BA and NS of 1:4,the stirring temperature of 60℃,the mixing time of 3 h,and the stirring speed of 454 rpm.The results showed that the loading capacity of BA-NS was 18.02 ± 0.36%,the entrapment rate was 86.64± 0.86%,and the particle size was 389.8 ± 24.0 nm.Under the optimal conditions,the phenol content is in the safe range,the particle size and the multi dispersion index are better,and the loading capacity and the encapsulation rate of BA-NS are higher.The physical appearance of BA changed significantly after NS loading.The results of electron microscopy showed that BA-NS were spherical particles,which accumulated into clumps or flakes.The binding sites of Ba and NS were chimeric and irregular aggregation.The results show that BA in NS does not exist in molecular state,but in amorphous state embedded in NS short network structure.FTIR,XRD and DSC spectra showed that NS and BA-NS were successfully synthesized,which indicated that the preparation method selected in this project was suitable for the synthesis of BA-NS.Solubility test showed that NS could significantly increase the solubility of BA in water.The results of in vitro release experiments showed that the cumulative release of BA in different media is different,but the common point is that the maximum release of BA-NS in different media does not change much,indicating that its performance is relatively stable,and NS can increase the stability of BA in different media.The results of the experiment of influencing factors showed that BA-NS has higher stability in high temperature,high humidity and strong light irradiation environment than that of BA.In this study,zebrafish with liver fluorescence was selected to investigate whether BA-NS and NS have significant effects on their liver,so as to explore the safety of BANS.The results showed that BA-NS and NS had no significant effect on the morphological development of zebrafish and its liver after 72 h of cultivation.In vitro,BA-NS and NS had no obvious antibacterial activity to Escheria coli and Candida albicans,and had different inhibition effects on Bacillus subtilis,Staphylococcus aureus and Aspergillus niger.