The study to reduce the hemolysis side effect of puerarin by a submicron emulsion delivery system.
A safe and effective delivery system with a submicron emulsion for puerarin was studied. Puerarin submicron emulsion was prepared by a novel complex-phase inversion-high press homogenization technology. The mechanism to reduce the hemolysis side effect of puerarin was studied by blood cell counts in rabbits. The average diameter, zeta potential and entrapment efficiency of the emulsion prepared was 198.14+/-8.61 nm, -29.45+/-1.47 mV, 87.32+/-0.34%, respectively. Compared with control group, the red blood cell values, packed cell volume, plasma hemoglobin level, haptoglobin level and osmotic fragility of puerarin i.v. group was significantly different (p<0.05) at 42, 43 d, respectively. The blood cell parameter values of puerarin submicron emulsion group were not significantly different (p>0.05) in contrast to control group. Such observations indicated that the intravascular hemolysis occurred at 42, 43 d in puerarin i.v. group rabbits, the hemolysis did not occur for puerarin emulsion group rabbits. As an explanation for these results, it was proposed that the puerarin was either incorporated into the lipophilic core or intercalated between the phospholipid molecules at the interface. It could be concluded that puerarin submicron emulsions prepared markedly reduced the hemolysis effect of puerarin.
Yue
Peng-Fei
PF
302 Hospital of PLA&PLA Institute of Chinese Materia Medica, Beijing, China.
Hai-Long Yuan
Hai-Long
HL
Zhu
Wei-Feng
WF
Cong
Long-Bo
LB
Xie
Huan
H
Liu
Zhi-Guo
ZG
Wang
Lu-Jun
LJ
Xiao
Xiao-He
XH
D000818:Animals; D016503:Drug Delivery Systems; D004655:Emulsions; D006461:Hemolysis / Q000187:drug effects*; D007529:Isoflavones / Q000008:administration & dosage* / Q000009:adverse effects*; D008297:Male; D046529:Microscopy, Electron, Transmission; D010316:Particle Size; D011817:Rabbits
D004655:Emulsions; D007529:Isoflavones; C033607:puerarin