In vitro and in vivo evaluation of puerarin-loaded PEGylated mesoporous silica nanoparticles.
Puerarin, which is extracted from Chinese medicine, is widely used in China and mainly used as a therapeutic agent for the treatment of cardiovascular diseases. Owing to its short elimination half-life in human beings, frequently intravenous administration of high doses of puerarin may be needed, which possibly leads to severe and acute side effects. The development of an effective sustained-release drug delivery system is urgently needed. In this study, PEGylated mesoporous silica nanoparticles (PEG-MSNs) had become a preferred way to prolong the half-life and improve the bioavailability of drugs. The release of puerarin from PEG-MSNs was pH dependent, and the release rate was much faster at lower pH than that at higher pH. Moreover, the PEG-MSNs exhibited improved blood compatibility over the MSNs in terms of low hemolysis, and it could also reduce the side effect of hemolysis induced by PUE. Compared with puerarin, PUE-loaded PEG-MSNs showed a 2.3-fold increase in half-life of puerarin and a 1.47-fold increase in bioavailability. Thus, the PEG-MSNs hold the substantial potential to be further developed as an effective sustained-release drug delivery system.
a Department of Pharmacy , The Second Xiangya Hospital of Central South University , Changsha , PR China ;|b Institution of Clinical Pharmacy of Central South University , Changsha , PR China ;
Xinyi
X
Liu
b Institution of Clinical Pharmacy of Central South University , Changsha , PR China ;
Yuxiang
Y
Ding
c School of Pharmaceutical Sciences , Central South University , Changsha , PR China ;
Bingjie
B
Zhao
d Hunan Testing Institute for Medical Devices and Pharmaceutical Packaging Material , Changsha , PR China.
Yuanyuan
Y
Liu
a Department of Pharmacy , The Second Xiangya Hospital of Central South University , Changsha , PR China ;|b Institution of Clinical Pharmacy of Central South University , Changsha , PR China ;
Shilin
S
Luo
a Department of Pharmacy , The Second Xiangya Hospital of Central South University , Changsha , PR China ;|c School of Pharmaceutical Sciences , Central South University , Changsha , PR China ;
Junyong
J
Wu
a Department of Pharmacy , The Second Xiangya Hospital of Central South University , Changsha , PR China ;|b Institution of Clinical Pharmacy of Central South University , Changsha , PR China ;
Jianhe
J
Li
a Department of Pharmacy , The Second Xiangya Hospital of Central South University , Changsha , PR China ;|b Institution of Clinical Pharmacy of Central South University , Changsha , PR China ;
Daxiong
D
Xiang
Hemolysis; PEGylated mesoporous silica nanoparticles; pharmacokinetics; puerarin; sustained-release drug delivery system