Formulation, optimization, and pharmacodynamic evaluation of chitosan/phospholipid/β-cyclodextrin microspheres

Area of Science:

• Biomaterials Science
• Neuroscience
• Pharmacology

Background:

• Alzheimer's disease (AD) is characterized by cognitive impairment due to cholinergic neurotransmission loss.
• Phospholipids (PLs) are crucial for memory, learning, and acetylcholine synthesis.
• Chitosan/phospholipid/β-cyclodextrin (CTS/PL/β-CD) microspheres offer a novel therapeutic approach.

Purpose of the Study:

• To prepare and optimize CTS/PL/β-CD microspheres for improved cognitive function in AD.
• To characterize the physical, chemical, and thermal properties of the microspheres.
• To evaluate the in vivo efficacy and neuroprotective effects of the microspheres.

Main Methods:

• Microspheres prepared using spray drying and optimized via orthogonal design.
• Characterization included SEM, FTIR, DSC, drug loading, and encapsulation efficiency.
• In vivo studies utilized the Morris water maze test and immunohistochemistry in a rat model.

Main Results:

• Optimized CTS/PL/β-CD microspheres exhibited spherical morphology with slightly wrinkled surfaces.
• FTIR and DSC confirmed hydrogen bonding between PLs, CTS, and β-CD.
• Microsphere treatment significantly improved spatial learning and memory in rats, reducing microglial activation and Protein Kinase C-δ expression.

Conclusions:

• Optimized CTS/PL/β-CD microspheres demonstrate significant potential for treating cognitive impairment in Alzheimer's disease.
• The microspheres exhibit favorable physicochemical properties and in vivo efficacy.
• Further research into these microspheres could lead to novel AD therapeutics.