title: Baicalin-loaded PEGylated lipid nanoparticles: characterization, pharmacokinetics, and protective effects on acute myocardial ischemia in rats.
abstract: BACKGROUND
  Baicalin has many pharmacological activities, including protective function against myocardial ischemia by antioxidant effects and free radical scavenging activity. However, its rapid elimination half-life in plasma and poor water solubility limits its clinical efficacy.
  
  
  OBJECTIVE
  Novel baicalin-loaded PEGylated nanostructured lipid carriers (BN-PEG-NLC) were developed to improve bioavailability of BN, to prolong retention time in vivo and to enhance its protective effect.
  
  
  METHODS
  In this study, BN-PEG-NLC were prepared by the emulsion-evaporation and low temperature-solidification method using a mixture of glycerol monostearate and polyethylene glycol monostearate as solid lipids, and oleic acid as the liquid lipid. The physicochemical properties of NLC were characterized. The pharmacokinetic and pharmacodynamic behaviors of BN-PEG-NLC or BN-NLC were evaluated in acute MI rats.
  
  
  CONCLUSIONS
  The particle size, zeta potential, and entrapment efficiency for BN-PEG-NLC were observed as 83.9 nm, -32.1 mV, and 83.5%, respectively. The release profiles of BN from both BN-PEG-NLC and BN-NLC were fitted to the Ritger-Peppas modal, which presented burst release initially and prolonged release afterwards. Pharmacokinetics results indicated that BN-PEG-NLC exhibited a 7.2-fold increase in AUC in comparison to BN solution, while a 3-fold increase in comparison to BN-NLC. Biodistribution results revealed that BN-PEG-NLC exhibited higher heart drug concentration compared with BN-NLC as well as BN solution. In the present study, BN-PEG-NLC significantly ameliorated infarct size.
  
  
  CONCLUSIONS
  The results of the present study imply that PEG-NLC could be the biocompatible carriers for heart-targeted drug delivery to improve myocardial ischemia.
authors.affiliation: a Department of Cardiology , Linyi People's Hospital , Linyi , P. R. China.
authors.forename: Shouwen
authors.initials: S
authors.lastname: Zhang
authors.affiliation: a Department of Cardiology , Linyi People's Hospital , Linyi , P. R. China.
authors.forename: Jie
authors.initials: J
authors.lastname: Wang
authors.affiliation: a Department of Cardiology , Linyi People's Hospital , Linyi , P. R. China.
authors.forename: Jin
authors.initials: J
authors.lastname: Pan
mesh_terms: D000818:Animals; D001682:Biological Availability; D003692:Delayed-Action Preparations / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems / Q000379:methods; D004655:Emulsions / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism; D005419:Flavonoids / Q000008:administration & dosage* / Q000737:chemistry* / Q000378:metabolism; D006207:Half-Life; D008055:Lipids / Q000737:chemistry*; D008297:Male; D017202:Myocardial Ischemia / Q000188:drug therapy*; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry*; D010316:Particle Size; D011092:Polyethylene Glycols / Q000008:administration & dosage / Q000737:chemistry*; D020011:Protective Agents / Q000008:administration & dosage / Q000737:chemistry* / Q000378:metabolism; D051381:Rats; D017207:Rats, Sprague-Dawley; D012995:Solubility; D014018:Tissue Distribution
chemical_list: D003692:Delayed-Action Preparations; D004337:Drug Carriers; D004655:Emulsions; D005419:Flavonoids; D008055:Lipids; D020011:Protective Agents; C038044:baicalin; D011092:Polyethylene Glycols; C009314:polyethylene glycol monostearate
keywords: Myocardial infarction; baicalin; long circulation; nanoparticles; nanostructured lipid carriers