Preparation of baicalin nanocrystal pellets and preliminary study on its pharmacokinetics

Objective: To prepare baicalin nanocrystal(BC-NC) and evaluate its pharmacokinetics in rats.Method: Baicalin nanosuspensions(BC-NS) were prepared by the high pressure homogenization technology combined with ultrasonic,and then BC-NS were solidificated into BC-NC pellets by removing the water through fluid-bed drying.Its morphology,mean diameter and Zeta-potential were determined.An HPLC method was employed to determine the concentration of baicalin in plasma,and the bioavailability of the nanocrystal was compared with the reference group by oral administration in Wistar rats.Result: The nanocrystals observed by scanning electron microscopy were irregular granulated,and the mean particle sizes of BC-NC were(248 ± 6) nm.Its polydispersity index(PI) and zeta-potential were(0.181±0.065),(-32.3±1.8) mV,respectively.The pharmacokinetic parameters showed that the Cmax was(16.54±1.73) mg·L-1 and the AUC0-24 h was(206.96±21.23) mg·L-1·h,which were significantly enhanced compared with the baicalin bulk and baicalin physical mixture(BC-PM) formulation,respectively(P0.01).Conclusion: Baicalin nanocrystal can significantly improve the bioavailability of baicalin.