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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.
Background:
Glioblastoma mutliforme is the most common and has the poorest prognosis of any malignant tumor of the central nervous system. Luteolin, the most abundant xanthone extracted from vegetables and medicinal plants, has been shown to have treatment effects in various cancer cell types. Luteolin is however, hydrophobic and has poor biocompatibility, which leads to low bioavailability.
Patients And Methods:
In this study, folic acid modifiedpoly(ethylene glycol)-poly(e-caprolactone) (Fa-PEG-PCL) nano-micelles was used to encapsulate the luteolin, creating luteolin loaded PEG-PCL (Lut/Fa-PEG-PCL) micelles to treat glioma both in vitro and in vivo.
Results:
When compared with the free luteolin and Lut/MPEG-PCL, Lut/Fa-PEG-PCL induced a significant cell growth inhibition and more apoptosis of GL261 cells both in vitro and in vivo. The safety assessment also showed no obvious side effects were observed in mice which were administrated with free luteolin or Lut/MPEG-PCL and Lut/Fa-PEG-PCL.
Conclusion:
These results suggested Lut/Fa-PEG-PCL may be used as an excellent intravenously injectable formulation for the treatment and chemoprevention.
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.
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