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已发表论文
对心肌梗死模型的保护作用：使用基质金属蛋白酶敏感的肽修饰聚乙二醇化脂质纳米颗粒递送五味子乙素
Authors Shao M, Yang W, Han G
Received 10 May 2017
Accepted for publication 8 August 2017
Published 26 September 2017 Volume 2017:12 Pages 7121—7130
DOI https://doi.org/10.2147/IJN.S141549
Checked for plagiarism Yes
Review by Single-blind
Peer reviewers approved by Dr Akshita Wason
Peer reviewer comments 4
Editor who approved publication: Dr Linlin Sun
Purpose: Schisandrin B
(Sch B) is clinically applied for the treatment of hepatitis and ischemic
disease. However, its clinical efficacy is limited due to the poor solubility
and low bioavailability. This study aimed to develop matrix metalloproteinase
(MMP)-sensitive peptide-modified, polyethylene glycol (PEG)-modified
(PEGylated) solid lipid nanoparticles (SLNs) for loading Sch B (MMP-Sch B
SLNs), and to evaluate the therapeutic effect in the myocardial infarction
model.
Methods: PEG lipid and MMP-targeting peptide conjugate were synthesized. MMP-Sch B SLNs were prepared by solvent displacement technique. The physicochemical properties and pharmacokinetics of SLNs were investigated. In vivo effects on infarct size was evaluated in rats.
Results: The successful synthesis of lipid-peptide conjugate was confirmed. MMP-Sch B SLNs had a particle size of 130 nm, a zeta potential of 18.3 mV, and a sustained-release behavior. Higher heart drug concentration and longer blood circulation times were achieved by Sch B loaded SLNs than the drug solution according to the pharmacokinetic and biodistribution results. The best therapeutic efficacy was exhibited by MMP-Sch B SLNs by reducing the infarction size to the greatest extent.
Conclusion: The modified SLNs may be a good choice for delivery of Sch B for the treatment of myocardial infarction.
Keywords: cardiovascular diseases, CVDs, schisandrin B, matrix metalloproteinase, lipid nanoparticles
Methods: PEG lipid and MMP-targeting peptide conjugate were synthesized. MMP-Sch B SLNs were prepared by solvent displacement technique. The physicochemical properties and pharmacokinetics of SLNs were investigated. In vivo effects on infarct size was evaluated in rats.
Results: The successful synthesis of lipid-peptide conjugate was confirmed. MMP-Sch B SLNs had a particle size of 130 nm, a zeta potential of 18.3 mV, and a sustained-release behavior. Higher heart drug concentration and longer blood circulation times were achieved by Sch B loaded SLNs than the drug solution according to the pharmacokinetic and biodistribution results. The best therapeutic efficacy was exhibited by MMP-Sch B SLNs by reducing the infarction size to the greatest extent.
Conclusion: The modified SLNs may be a good choice for delivery of Sch B for the treatment of myocardial infarction.
Keywords: cardiovascular diseases, CVDs, schisandrin B, matrix metalloproteinase, lipid nanoparticles
