Brain targeted lactoferrin coated lipid nanocapsules for the combined effects of apocynin and lavender essential oil...

Area of Science:

• Neuroscience
• Pharmacology
• Nanotechnology

Background:

• Apocynin (APO) is a neuroprotective antioxidant with poor bioavailability, limiting its use in CNS disorders like epilepsy.
• Novel drug delivery systems are needed to overcome APO's limitations and improve brain targeting.

Purpose of the Study:

• To formulate and characterize lactoferrin-coated lipid nanocapsules (LF-APO-LAV/LNC) encapsulating apocynin (APO) and lavender oil (LAV).
• To evaluate the in vivo efficacy of LF-APO-LAV/LNC in a pentylenetetrazol (PTZ)-induced seizures rat model.

Main Methods:

• Lipid nanocapsules (LNC) were formulated with APO and LAV, then coated with lactoferrin (LF).
• Physicochemical properties (size, zeta potential, entrapment efficiency, release profile) were assessed.
• Pharmacokinetic parameters (AUC, MRT) and brain accumulation (Log BB) were determined after subcutaneous administration.
• Seizure activity, oxidant/antioxidant capacity, and inflammatory markers were evaluated in a PTZ-induced rat model.

Main Results:

• Optimized LF-APO-LAV/LNC exhibited optimal particle size, high entrapment efficiency (92%), and sustained release.
• LF-APO-LAV/LNC demonstrated a twofold increase in plasma AUC and MRT compared to APO alone, with enhanced brain accumulation.
• The formulation significantly reduced seizure severity, increased latency, and decreased duration in PTZ-treated rats.
• Significant improvements in oxidant/antioxidant balance and reduced inflammatory markers were observed in brain tissue.

Conclusions:

• Lactoferrin-coated nanocapsules effectively enhance APO and LAV delivery to the brain.
• The combined APO/LAV formulation in LF-coated LNC shows significant anticonvulsant activity.
• This nanocarrier system represents a promising therapeutic strategy for managing seizures and epilepsy.