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Taxifolin-Functionalized Rivastigmine Liposomal Nanoformulation: A Synergistic Approach for Alzheimer's Disease
Manoyogambiga M1, Rajaganapathy Kaliyaperumal1
1Faculty of Pharmacy, Bharath Institute of Higher Education and Research, Selaiyur, Chennai-600073, Tamil Nadu, India.
This study developed a novel Taxifolin-decorated Rivastigmine liposomal nanocarrier (Tax-Riva-Lipo) for Alzheimer's disease (AD). The nanocarrier offers combined cholinesterase inhibition, antioxidant, and anti-amyloid effects for improved neuroprotection and cognitive function.
Area of Science:
- Nanomedicine
- Neuroscience
- Pharmacology
Background:
- Alzheimer's disease (AD) involves cognitive decline, oxidative stress, and amyloid plaques.
- Current AD therapies offer symptomatic relief with limited brain delivery.
- Multifunctional nanocarriers are needed for synergistic therapeutic effects in AD.
Purpose of the Study:
- To formulate and evaluate a Taxifolin-decorated Rivastigmine liposomal nanocarrier (Tax-Riva-Lipo).
- To achieve synergistic neuroprotection via combined cholinesterase inhibition, antioxidant defense, and anti-amyloid activity.
Main Methods:
- Taxifolin was conjugated to DSPE-PEG and incorporated into Rivastigmine liposomes.
- Formulation characterized by DLS, TEM, FTIR, DSC.
- In vitro assays (release, enzyme inhibition, antioxidant, cell protection) and in vivo studies in an AD rat model were performed.
Main Results:
- Optimized Tax-Riva-Lipo showed uniform nanosize (~145 nm), high encapsulation (≈85%), and sustained release (48h).
- Demonstrated enhanced cholinesterase inhibition (AChE, BuChE), potent antioxidant activity, and significant neuroprotection (92% SH-SY5Y cell viability).
- In vivo studies revealed improved cognition, restored antioxidant enzymes, reduced inflammation, and preserved brain structure without toxicity.
Conclusions:
- Taxifolin functionalization provides synergistic antioxidant and anti-amyloid effects alongside sustained cholinesterase inhibition.
- Tax-Riva-Lipo is a promising nanotherapeutic platform for enhanced Alzheimer's disease management.
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