Engineered Novel Brijaluronic Terpesomes for Brain-Targeted Quercetin Delivery: Optimization, Ex Vivo and...

Area of Science:

• Nanotechnology
• Pharmaceutics
• Neuroscience

Background:

• Quercetin (QER) has potential neurotherapeutic benefits but faces challenges in brain delivery.
• Developing effective delivery systems is crucial for enhancing QER's efficacy in treating brain disorders.

Purpose of the Study:

• To create and optimize a novel Brijaluronic-based terpesomal system for efficient brain transport of quercetin.
• To evaluate the physicochemical properties, stability, and brain-targeting potential of the developed terpesomes.

Main Methods:

• Terpesomes were fabricated using an ethanol-injection method and optimized via Design-Expert software.
• Formulation parameters including terpene-to-drug ratio, surfactant type, and hyaluronic acid amount were systematically evaluated.
• Physicochemical characterization, in-vitro release studies, stability assessments, antioxidant activity assays, and radio-kinetic brain targeting evaluations were performed.

Main Results:

• The optimized terpesomes exhibited high encapsulation efficiency (88.66%), optimal size (72.09 nm), and a stable zeta potential (-26.5 mV).
• The formulation demonstrated excellent stability over three months, a biphasic in-vitro release profile, and a significant 3.5-fold enhancement in antioxidant activity.
• Radio-kinetic studies confirmed superior brain targeting efficiency compared to nasal quercetin solution, with higher brain/blood ratios at all time points.

Conclusions:

• Brijaluronic terpesomes represent a promising, stable, and innovative nano-platform for quercetin delivery to the brain.
• This engineered system significantly enhances quercetin's antioxidant capacity and brain targeting, offering potential for improved neurotherapeutic applications.