Abstract
Impaired memory and cognitive function are the main features of Alzheimer’s disease (AD). Unfortunately, currently available treatments cannot cure or delay AD progression. Moreover, the blood–brain barrier hampers effective delivery of treatment to the brain. Therefore, we aimed to evaluate the impact of intranasally delivered luteolin on AD using bile-salt-based nano-vesicles (bilosomes). Different bilosomes were prepared using 23-factorial design. The variables were defined by the concentration of surfactant, the molar ratio of cholesterol:phospholipid, and the concentration of bile salt. Results demonstrated optimized luteolin-loaded bilosomes with particle size (153.2 ± 0.98 nm), zeta potential (−42.8 ± 0.24 mV), entrapment efficiency% (70.4 ± 0.77%), and % drug released after 8 h (80.0 ± 1.10%). In vivo experiments were conducted on an AD mouse model via intracerebroventricular injection of 3 mg/kg streptozotocin. We conducted behavioral, biochemical marker, histological, and immune histochemistry assays after administering a luteolin suspension or luteolin bilosomes (50 mg/kg) intranasally for 21 consecutive days. Luteolin bilosomes improved short-term and long-term spatial memory. They also exhibited antioxidant properties and reduced levels of proinflammatory mediators. They also suppressed both amyloid β aggregation and hyperphosphorylated Tau protein levels in the hippocampus. In conclusion, luteolin bilosomes are an effective, safe, and non-invasive approach with superior cognitive function capabilities compared to luteolin suspension.
Highlights
Patients with neurodegenerative disorders, such as Parkinson’s disease, schizophrenia, migraine, and Alzheimer’s disease (AD), have limited treatment options.AD is one of the fatal neurodegenerative diseases characterized by advanced memory and cognition deterioration [1]
Low coefficient of variation was observed in the obtained quadratic model, confirming that the model can be used to explore the design space
This study was the first evaluation of the antioxidant, anti-inflammatory, and antiamyloidogenic potentials of luteolin-loaded bilosomes
Summary
Patients with neurodegenerative disorders, such as Parkinson’s disease, schizophrenia, migraine, and Alzheimer’s disease (AD), have limited treatment options.AD is one of the fatal neurodegenerative diseases characterized by advanced memory and cognition deterioration [1]. To date, the available pharmacological treatments are limited and cannot cure AD or delay its progression. These include symptomatic treatments using FDA-approved anticholinesterase medications (donepezil, galantamine, tacrine, and rivastigmine) [4]. Such treatments can induce side effects, such as headache, dizziness, nausea, vomiting, and appetite loss [4]. Other treatment strategies, such as antioxidants and anti-inflammatory agents, may be useful against memory-related disorders [4]. The development of non-invasive drug delivery to the brain for treatment of chronic central nervous system disorders is challenging.
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