Functionalized nanoparticles based on β-chitosan and styrene copolymer derivative for donepezil delivery

Area of Science:

• Biomaterials Science
• Nanotechnology
• Pharmacology

Background:

• Effective drug delivery across the blood-brain barrier is essential for treating neurological disorders.
• Current treatments face challenges in achieving adequate drug concentrations in the brain.
• Donepezil is a key therapeutic agent for Alzheimer's disease, but its delivery is limited.

Purpose of the Study:

• To develop a novel polyelectrolyte complex (PEC) nanogel system for enhanced drug delivery of Donepezil.
• To investigate the structural characteristics and drug encapsulation efficiency of the PEC nanogels.
• To evaluate the in vitro sustained drug release and acetylcholinesterase (AChE) inhibitory activity of the drug-loaded nanogels.

Main Methods:

• Preparation of sulfonated styrene-maleic anhydride (S-SMA) and its complexation with β-chitosan (CS) to form PEC nanoparticles.
• Characterization of nanoparticle size, surface charge, and morphology using techniques like Transmission Electron Microscopy (TEM).
• Encapsulation of Donepezil hydrochloride (DH) into the optimized CS-S3 nanogel formulation (CS-S3-DH) and assessment of in vitro drug release kinetics and AChE inhibition.

Main Results:

• Tunable nanoparticle size and surface charge were achieved by varying S-SMA content in the PECs.
• CS-S3-DH nanoparticles exhibited a mean diameter of 111 ± 0.4 nm, with successful encapsulation of Donepezil hydrochloride.
• Sustained in vitro release of DH over 72 hours and significantly enhanced AChE inhibition (63.9%) were observed for CS-S3-DH compared to the blank nanogel (16.5%).

Conclusions:

• The developed β-chitosan/sulfonated styrene-maleic anhydride PEC nanogels represent a promising platform for efficient Donepezil delivery.
• The nanogel system demonstrates potential for improving therapeutic outcomes in neurological conditions by enhancing drug bioavailability and efficacy.
• Further research into in vivo performance and blood-brain barrier penetration is warranted.