[Preparation of baicalin nanocrystal pellets and preliminary study on its pharmacokinetics].
OBJECTIVE
To prepare baicalin nanocrystal (BC-NC) and evaluate its pharmacokinetics in rats.


METHODS
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.


RESULTS
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 C(max) was (16.54 +/- 1.73) mg x L(-1) and the AUC(0-24 h) was (206.96 +/- 21.23) mg x L(-1) x h, which were significantly enhanced compared with the baicalin bulk and baicalin physical mixture (BC-PM) formulation, respectively (P < 0.01).


CONCLUSIONS
Baicalin nanocrystal can significantly improve the bioavailability of baicalin.
School of Pharmaceutical Sciences, Chengdu University of Traditional Chinese Medicine, Chengdu 611730, China. jsypharm@126.com
Shi-Ying
SY
Jin
Hai-Long
HL
Yuan
Shi-Xiao
SX
Jin
Qing-Yuan
QY
Lv
Jin-Xia
JX
Bai
Jin
J
Han
D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D002851:Chromatography, High Pressure Liquid; D005419:Flavonoids / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics*; D008297:Male; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D010316:Particle Size; D051381:Rats
D005419:Flavonoids; C038044:baicalin