Epigallocatechin-3-gallate loaded PEGylated-PLGA nanoparticles: A new anti-seizure strategy for temporal lobe epilepsy

Nanomedicine. 2018 Jun;14(4):1073-1085. doi: 10.1016/j.nano.2018.01.019. Epub 2018 Feb 15.

Abstract

Temporal lobe epilepsy is the most common type of pharmacoresistant epilepsy in adults. Epigallocatechin-3-gallate has aroused much interest because of its multiple therapeutic effects, but its instability compromises the potential effectiveness. PEGylated-PLGA nanoparticles of Epigallocatechin-3-gallate were designed to protect the drug and to increase the brain delivery. Nanoparticles were prepared by the double emulsion method and cytotoxicity, behavioral, Fluoro-Jade C, Iba1 and GFAP immunohistochemistry studies were carried out to determine their effectiveness. Nanoparticles showed an average size of 169 nm, monodisperse population, negative surface charge, encapsulation efficiency of 95% and sustained release profile. Cytotoxicity assays exhibited that these nanocarriers were non-toxic. Behavioral test showed that nanoparticles reduced most than free drug the number of epileptic episodes and their intensity. Neurotoxicity and immunohistochemistry studies confirmed a decrease in neuronal death and neuroinflammation. In conclusion, Epigallocatechin-3-gallate PEGylated-PLGA nanoparticles could be a suitable strategy for the treatment of temporal lobe epilepsy.

Keywords: Epigallocatechin-3-gallate; Epilepsy; PLGA-PEG; Polymeric nanoparticles.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Catechin / analogs & derivatives*
  • Catechin / chemistry
  • Catechin / therapeutic use
  • Drug Carriers / chemistry
  • Emulsions
  • Epilepsy, Temporal Lobe / drug therapy*
  • Epilepsy, Temporal Lobe / metabolism
  • Mice
  • Mice, Inbred C57BL
  • Nanoparticles / chemistry*
  • PC12 Cells
  • Particle Size
  • Polyethylene Glycols / chemistry*
  • Polylactic Acid-Polyglycolic Acid Copolymer / chemistry*
  • Rats
  • Seizures / drug therapy

Substances

  • Drug Carriers
  • Emulsions
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Polyethylene Glycols
  • Catechin
  • epigallocatechin gallate