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Fenofibrate-loaded PLGA microparticles: effects on ischemic stroke.

D Klose¹, M Laprais, V Leroux

¹College of Pharmacy, JE 2491, University of Lille, 3 Rue du Professeur Laguesse, 59006 Lille, France.

European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences

|January 27, 2009

Summary

Local controlled drug delivery using fenofibrate-loaded microparticles effectively reduced ischemic stroke consequences in rats. This approach shows promise for treating central nervous system diseases beyond cancer.

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Area of Science:

Biomedical Engineering
Neuroscience
Pharmacology

Background:

Many drugs cannot cross the Blood Brain Barrier (BBB), limiting treatment options for Central Nervous System (CNS) diseases.
Local controlled drug delivery is a challenging but promising strategy to overcome BBB limitations.
Current applications are limited, with only one product available for malignant glioma treatment.

Purpose of the Study:

To evaluate the efficacy of local controlled drug delivery to the CNS for reducing ischemic stroke consequences.
To investigate the potential of fenofibrate and fenofibric acid delivered via PLGA microparticles for stroke treatment.

Main Methods:

Fenofibrate and fenofibric acid were encapsulated into PLGA microparticles.
The efficacy of these microparticle formulations was assessed in a Wistar rat model of ischemic stroke.
Infarct volumes (total, cortical, striatal) were measured to quantify treatment effects.

Main Results:

Fenofibrate-loaded microparticles significantly reduced total, cortical, and striatal infarct volumes in Wistar rats.
Fenofibric acid-loaded microparticles did not demonstrate significant in vivo efficacy.
Potential reasons for fenofibric acid's limited efficacy include restricted brain distribution or cell uptake.

Conclusions:

Local controlled drug delivery to the CNS holds significant potential for treating ischemic stroke and other non-cancerous CNS diseases.
This drug delivery strategy can aid in early in vivo proof-of-concept studies for drug candidates that cannot cross the BBB.
PLGA microparticle encapsulation of fenofibrate is an effective method for mitigating ischemic stroke damage.