N-oleoylethanolamine - phosphatidylcholine complex loaded, DSPE-PEG integrated liposomes for efficient stroke.

Area of Science:

• Neuroscience
• Pharmacology
• Biotechnology

Background:

• Stroke is a leading cause of death with limited treatment success.
• N-oleoylethanolamine (OEA) is an endogenous neuroprotective agent but is highly hydrophobic.
• Developing effective delivery systems for hydrophobic drugs like OEA is crucial for stroke therapy.

Purpose of the Study:

• To develop and evaluate N-oleoylethanolamine (OEA) loaded liposomes (OEA NPs) as an intravenous formulation for stroke treatment.
• To assess the neuroprotective efficacy of OEA NPs in a rat model of stroke.

Main Methods:

• Formation of hydrogen bonds between OEA and soybean phosphatidylcholine (SPC).
• Self-assembly of OEA-SPC complex and DSPE-PEG into liposomes (OEA NPs).
• In vivo assessment in MCAO rat model, including survival rate, Garcia score, TTC staining, Morris water maze, and immunofluorescence assays.

Main Results:

• OEA NPs demonstrated a drug loading of 8.21 ± 0.18 wt% and uniform particle size.
• Administration of OEA NPs significantly improved survival rates and Garcia scores in MCAO rats compared to free OEA.
• OEA NPs markedly reduced cerebral infarct volume, edema, neuronal apoptosis, and brain inflammation, while improving spatial learning and memory.

Conclusions:

• OEA NPs represent a promising liposomal formulation for enhancing the delivery and efficacy of OEA.
• The developed OEA NPs show significant potential for clinical application as an anti-stroke therapeutic agent.