title: Polysorbate 80-coated PLGA nanoparticles improve the permeability of acetylpuerarin and enhance its brain-protective effects in rats.
abstract: OBJECTIVE
  Acetylpuerarin (AP) is an acetylated derivative of puerarin (PUE). The study aimed to prepare polysorbate 80-coated poly(lactic-co-glycolic acid) (PLGA) nanoparticles to improve the permeability of AP across the blood-brain barrier (BBB) and enhance its brain-protective effects.
  
  
  METHODS
  AP-loaded PLGA nanoparticles (AP-PLGA-NPs) were prepared using a solvent diffusion methodology. The NPs were characterized. The pharmacokinetics, tissue distributions and brain-protective effects of AP-PLGA-NPs were evaluated in animals.
  
  
  RESULTS
  AP-PLGA-NPs were successfully prepared with a mean particle size of 145.0 nm and a zeta potential of -14.81 mV. The in-vitro release of AP from the PLGA-NPs showed a biphasic release profile. AP was metabolized into PUE in rats. The AUC0-∞ values of AP and PUE for AP-PLGA-NPs were 2.90- and 2.29-fold as great as those for AP solution, respectively. The values of the relative targeting efficiency in the brain were 2.40 and 2.58 for AP and PUE, and the ratios of peak concentration were 1.91 and 1.89 for AP and PUE, respectively. Compared with the crude drug, AP-PLGA-NPs showed better brain-protective effects in rats.
  
  
  CONCLUSIONS
  Polysorbate 80-coated PLGA-NPs can improve the permeability of AP cross the BBB and enhance its brain-protective effects in rats.
authors.affiliation: Department of Pharmacy, Second Hospital of Shandong University, Jinan, China.
authors.forename: Deqing
authors.initials: D
authors.lastname: Sun
authors.affiliation: Department of Cardiology, Second Hospital of Shandong University, Jinan, China.
authors.forename: Aiying
authors.initials: A
authors.lastname: Xue
authors.affiliation: Department of Pharmacy, Second Hospital of Shandong University, Jinan, China.
authors.forename: Bin
authors.initials: B
authors.lastname: Zhang
authors.affiliation: Department of Pharmacology, School of Medicine and Shandong University, Jinan, China.
authors.forename: Haiyan
authors.initials: H
authors.lastname: Lou
authors.affiliation: Department of Pharmacology, School of Medicine and Shandong University, Jinan, China.
authors.forename: Huanying
authors.initials: H
authors.lastname: Shi
authors.affiliation: Department of Pharmacology, School of Medicine and Shandong University, Jinan, China.
authors.forename: Xiumei
authors.initials: X
authors.lastname: Zhang
mesh_terms: D000818:Animals; D017209:Apoptosis / Q000187:drug effects; D019540:Area Under Curve; D001711:Biotransformation; D001812:Blood-Brain Barrier / Q000378:metabolism; D001921:Brain / Q000187:drug effects* / Q000378:metabolism / Q000473:pathology; D001930:Brain Injuries / Q000378:metabolism / Q000473:pathology / Q000517:prevention & control*; D002199:Capillary Permeability; D002626:Chemistry, Pharmaceutical; D004195:Disease Models, Animal; D004337:Drug Carriers; D007275:Injections, Intravenous; D007529:Isoflavones / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D019344:Lactic Acid / Q000737:chemistry*; D008297:Male; D051379:Mice; D050997:Nanomedicine / Q000379:methods; D053758:Nanoparticles; D018696:Neuroprotective Agents / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D010316:Particle Size; D010539:Permeability; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011136:Polysorbates / Q000737:chemistry*; D017208:Rats, Wistar; D015427:Reperfusion Injury / Q000378:metabolism / Q000473:pathology / Q000517:prevention & control*; D012995:Solubility; D014018:Tissue Distribution
chemical_list: D004337:Drug Carriers; D007529:Isoflavones; D018696:Neuroprotective Agents; D011136:Polysorbates; C521069:acetylpuerarin; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid
keywords: acetylpuerarin; brain-targeting; nanoparticles; poly(lactic-co-glycolic acid); polysorbate 80