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

Abstract

Purpose

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 H₂O₂, modified Dixon agar, and serum lactate dehydrogenase, and increase superoxide dismutase (P < 0.05).

Conclusion

The results of the present study imply that HLV has promising prospects for improving free drug bioactivity on oral administration.

Keywords:

• liposomes
• nanoparticles
• panax notoginsenoside
• physicochemical properties
• in vivo animal models

Acknowledgements

The study was supported by the Science and Technology Support Program of Jiangxi Province (20111BBG70004-1), the Scientific Research Foundation of Traditional Chinese Medicine of Jiangxi Provincial Health Department (2011A132) and the Technology Platform for Novel Drug Delivery System of TCM (2009ZX09310-005).

Disclosure

The authors report no conflicts of interest in this work.