Preparation Of Baicalin-sanguinarine Ion-pair Nanoparticles

Baicalin, sanguinarine both has strong antibacterial activities, we synthesis those two into baicalin-sanguinarine ion-pair, not only hope to improve the deficiencies, but also improve the antibacterial activity. But consider poor water solubility of BSI, we prepared it to nanoparticles firstly, which can improve the bioavailability and prepare for further study of the pharmacological effect of the BSI.According to the papers, we select the polylactic acid, lecithin, cyclodextrins, chitosan as the carrier and Entrapment Efficiency, Drug Loading, zeta potential, uniform grading and stability as the index for synthesis of Baicalin-sanguinarine ion-pair nanoparticles (BSI-NPs). We also compare advantage and disadvantages of various carriers for synthesis of BSI-NPs. The development of the optimized technology in single factor and orthogonal test selection of the carriers can gain the good indexes of BSI-NPs. Finally describe the properties of the BSI-NPs, and study the in vitro release and bioavailability.By comparing the various indexes, chitosan nanoparticles loading baicalin-sanguinarine ion-pair (BSI-CS-NPs) synthesized by ionotropic gelation method are suitable for the preparation of BSI-NPs, because it has the ideal Entrapment Efficiency, Drug Loading, particle size and better stability. Moreover, single factor and orthogonal test shows that the content of chitosan and TPP, the quantity of BSI and the value of pH have huge influence on the various indexes of preparation during the process. The suitable condition is the content of chitosan100mg, TPP20mg, dose of drug15mg,the value of pH4. BSI-CS-NPs synthesized by better process have good look, uniform size distribution of particles. The mean particle size was found to be326.4nm with a narrow particles distribution of polydispersity index. The Zeta potential of the optimized method-loaded chitosan nanoparticles was45.7mV, the drug entrapment efficiency was65.68%, and the loading rate was36.43%. we respectively investigate the use of the four protective solutes and find that the10%of sucrose solutions is the best protective solute for BSI-CS-NPs. It not only has good look and bright colour, shorter time of distribution, compared with the original BSI drug,but also the drug release degree of BSI-CS-NPs decreased about36.51%in2h compared with BSI solution and the total drug release degree in12h was92.29%with the sustained releasing behaviorlonotropic gelation method by the carrier of citosan is suitable for the synthesis of the BSI-CS-NPs. The Optimized proces of BSI-CS-NPs is simple and relable, low cost and stable method. The experiment proved that BSI-CS-NPs have the release property, the enhancement of the relative bioavailability and better effect.