Trans-ferulic acid-based solid lipid nanoparticles and their antioxidant effect in rat brain microsomes

Area of Science:

• Nanotechnology
• Pharmacology
• Biochemistry

Background:

• Trans-ferulic acid (FA) is a potent antioxidant with limited bioavailability.
• Developing effective delivery systems is crucial for enhancing FA's therapeutic potential.
• Solid lipid nanoparticles (SLNs) offer a promising platform for lipophilic drug delivery.

Purpose of the Study:

• To prepare and characterize stearic acid- and stearyl ferulate-based solid lipid nanoparticles (SLN-FA and SLN-SF-FA) containing trans-ferulic acid (FA).
• To evaluate the in vitro antioxidant activity of these SLN formulations against lipid peroxidation.
• To compare the efficacy of SLN-FA and SLN-SF-FA with commercially available FA and its ethyl ester (FAEE).

Main Methods:

• Preparation and characterization of SLN-FA and SLN-SF-FA for loading efficiency, size, and shape.
• In vitro antioxidant activity assessment using rat brain microsomes.
• Evaluation against lipid peroxidation initiators: AAPH, NADPH/ADP-Fe(3+), and SIN-1.

Main Results:

• Both SLN-FA and SLN-SF-FA dose-dependently reduced lipid peroxidation induced by all three oxidants.
• SLN-SF-FA demonstrated superior efficacy (EC50) and potency against AAPH- and NADPH/ADP-Fe(3+)-induced lipid peroxidation.
• Commercially available FA and FAEE served as comparators in the study.

Conclusions:

• The developed SLN formulations, particularly SLN-SF-FA, show significant potential for enhancing FA bioavailability due to their lipophilic structure.
• Stearyl ferulate-based nanoparticles effectively protect entrapped FA from degradation, ensuring its availability for antioxidant activity.
• These novel nanoparticles represent a promising strategy for improving the delivery and efficacy of trans-ferulic acid.