PLoS ONE (Jan 2014)

Brain-targeted delivery of trans-activating transcriptor-conjugated magnetic PLGA/lipid nanoparticles.

  • Xiangru Wen,
  • Kai Wang,
  • Ziming Zhao,
  • Yifang Zhang,
  • Tingting Sun,
  • Fang Zhang,
  • Jian Wu,
  • Yanyan Fu,
  • Yang Du,
  • Lei Zhang,
  • Ying Sun,
  • YongHai Liu,
  • Kai Ma,
  • Hongzhi Liu,
  • Yuanjian Song

DOI
https://doi.org/10.1371/journal.pone.0106652
Journal volume & issue
Vol. 9, no. 9
p. e106652

Abstract

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Magnetic poly (D,L-lactide-co-glycolide) (PLGA)/lipid nanoparticles (MPLs) were fabricated from PLGA, L-α-phosphatidylethanolamine (DOPE), 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-amino (polyethylene glycol) (DSPE-PEG-NH2), and magnetic nanoparticles (NPs), and then conjugated to trans-activating transcriptor (TAT) peptide. The TAT-MPLs were designed to target the brain by magnetic guidance and TAT conjugation. The drugs hesperidin (HES), naringin (NAR), and glutathione (GSH) were encapsulated in MPLs with drug loading capacity (>10%) and drug encapsulation efficiency (>90%). The therapeutic efficacy of the drug-loaded TAT-MPLs in bEnd.3 cells was compared with that of drug-loaded MPLs. The cells accumulated higher levels of TAT-MPLs than MPLs. In addition, the accumulation of QD-loaded fluorescein isothiocyanate (FITC)-labeled TAT-MPLs in bEnd.3 cells was dose and time dependent. Our results show that TAT-conjugated MPLs may function as an effective drug delivery system that crosses the blood brain barrier to the brain.