Delivery luteolin with folacin-modified nanoparticle for glioma therapy

Cong Wu1, Qian Xu1, Xinyue Chen1

  • 1Department of Neurosurgery, West China Hospital, West China Medical School, Sichuan University, Chengdu 610041, People's Republic of China.

Abstract

Insights

Folic acid-modified nano-micelles effectively delivered luteolin to treat glioblastoma, significantly inhibiting tumor growth and increasing apoptosis with no observed side effects in mice.

Area of Science:

  • Neuro-oncology
  • Nanomedicine
  • Pharmacology

Background:

  • Glioblastoma multiforme presents a poor prognosis among central nervous system tumors.
  • Luteolin, a plant-derived xanthone, exhibits anti-cancer properties but suffers from low bioavailability due to hydrophobicity.
  • Developing effective delivery systems is crucial for luteolin's therapeutic potential in cancer treatment.

Purpose of the Study:

  • To develop and evaluate luteolin-loaded folic acid-modified nano-micelles (Lut/Fa-PEG-PCL) for glioblastoma treatment.
  • To assess the in vitro and in vivo efficacy and safety of Lut/Fa-PEG-PCL compared to free luteolin and non-modified micelles.

Main Methods:

  • Encapsulation of luteolin within folic acid-modified poly(ethylene glycol)-poly(e-caprolactone) (Fa-PEG-PCL) nano-micelles.
  • In vitro and in vivo evaluation of luteolin-loaded micelles in GL261 glioblastoma models.
  • Comparative analysis of cell growth inhibition, apoptosis induction, and safety profiles.

Main Results:

  • Lut/Fa-PEG-PCL demonstrated significantly enhanced inhibition of GL261 cell growth compared to free luteolin and Lut/MPEG-PCL.
  • Increased apoptosis of GL261 cells was observed with Lut/Fa-PEG-PCL treatment both in vitro and in vivo.
  • Safety assessments revealed no significant adverse effects in mice treated with the various luteolin formulations.

Conclusions:

  • Lut/Fa-PEG-PCL represents a promising, intravenously injectable formulation for glioblastoma treatment.
  • The enhanced delivery system improves luteolin's efficacy for potential therapeutic and chemopreventive applications.
  • Targeted delivery via Fa-PEG-PCL micelles overcomes luteolin's bioavailability limitations for CNS tumor therapy.