In vitro and in vivo evaluation of puerarin-loaded PEGylated mesoporous silica nanoparticles |
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Authors: | Xinyi Liu Yuxiang Ding Bingjie Zhao Yuanyuan Liu Shilin Luo Junyong Wu |
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Affiliation: | 1. Department of Pharmacy, The Second Xiangya Hospital of Central South University, Changsha, PR China;2. Institution of Clinical Pharmacy of Central South University, Changsha, PR China;3. Institution of Clinical Pharmacy of Central South University, Changsha, PR China;4. School of Pharmaceutical Sciences, Central South University, Changsha, PR China;5. Hunan Testing Institute for Medical Devices and Pharmaceutical Packaging Material, Changsha, PR China;6. School of Pharmaceutical Sciences, Central South University, Changsha, PR China |
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Abstract: | 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. |
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Keywords: | Hemolysis PEGylated mesoporous silica nanoparticles pharmacokinetics puerarin sustained-release drug delivery system |
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