Core-shell hybrid liposomal vesicles loaded with panax notoginsenoside: preparation, characterization and protective effects on global cerebral ischemia/reperfusion injury and acute myocardial ischemia in rats.
OBJECTIVE
Novel panax notoginsenoside-loaded core-shell hybrid liposomal vesicles (PNS-HLV) were developed to resolve the restricted bioavailability of PNS and to enhance its protective effects in vivo on oral administration.


METHODS
Physicochemical characterizations of PNS-HLV included assessment of morphology, particle size and zeta potential, encapsulation efficiency (EE%), stability and in vitro release study. In addition, to evaluate its oral treatment potential, we compared the effect of PNS-HLV on global cerebral ischemia/reperfusion and acute myocardial ischemia injury with those of PNS solution, conventional PNS-loaded nanoparticles, and liposomes.


RESULTS
In comparison with PNS solution, conventional PNS-loaded nanoparticles and liposomes, PNS-HLV was stable for at least 12 months at 4°C. Satisfactory improvements in the EE% of notoginsenoside R1, ginsenoside Rb1, and ginsenoside Rg1 were shown with the differences in EE% shortened and the greater controlled drug release profiles were exhibited from PNS-HLV. The improvements in the physicochemical properties of HLV contributed to the results that PNS-HLV was able to significantly inhibit the edema of brain and reduce the infarct volume, while it could markedly inhibit H(2)O(2), modified Dixon agar, and serum lactate dehydrogenase, and increase superoxide dismutase (P < 0.05).


CONCLUSIONS
The results of the present study imply that HLV has promising prospects for improving free drug bioactivity on oral administration.
Key Laboratory of Modern Preparation of TCM, Ministry of Education, Jiangxi University of Traditional Chinese Medicine, Nanchang 330004, China.
Jing
J
Zhang
Xizhen
X
Han
Xiang
X
Li
Yun
Y
Luo
Haiping
H
Zhao
Ming
M
Yang
Bin
B
Ni
Zhenggen
Z
Liao
D000704:Analysis of Variance; D000818:Animals; D000975:Antioxidants / Q000378:metabolism; D001923:Brain Chemistry / Q000187:drug effects; D020520:Brain Infarction / Q000473:pathology; D002545:Brain Ischemia / Q000378:metabolism / Q000517:prevention & control*; D002316:Cardiotonic Agents / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D004355:Drug Stability; D004365:Drugs, Chinese Herbal / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D036145:Ginsenosides / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D007770:L-Lactate Dehydrogenase / Q000378:metabolism; D008081:Liposomes / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D008297:Male; D017202:Myocardial Ischemia / Q000378:metabolism* / Q000517:prevention & control*; D051381:Rats; D017207:Rats, Sprague-Dawley; D015427:Reperfusion Injury / Q000378:metabolism / Q000517:prevention & control*; D014867:Water / Q000378:metabolism
D000975:Antioxidants; D002316:Cardiotonic Agents; D004365:Drugs, Chinese Herbal; D036145:Ginsenosides; D008081:Liposomes; D014867:Water; D007770:L-Lactate Dehydrogenase