article · Pharmaceutics
Effective treatment of Alzheimer's disease is severely limited by the blood-brain barrier. To address this challenge, luteolin was formulated into bile-salt-based nano-vesicles, termed bilosomes, for non-invasive intranasal brain delivery. Formulations were optimised by adjusting surfactant concentration, cholesterol to phospholipid ratios, and bile salt content, yielding nanoparticles with high entrapment efficiency and sustained drug release over eight hours. In an animal model of sporadic Alzheimer's disease induced by streptozotocin, daily intranasal administration of luteolin bilosomes over twenty-one days outperformed simple luteolin suspensions. The nanocarrier treatment significantly improved both short-term and long-term spatial memory, lowered levels of proinflammatory mediators, and provided antioxidant protection. Furthermore, the formulation reduced amyloid beta accumulation and suppressed hyperphosphorylated Tau proteins in the hippocampus. These findings confirm the potential of intranasally delivered nanobilosomes to deliver neuroprotective agents directly to the brain.
Alzheimer's disease causes progressive memory loss, yet most potential medicines struggle to cross the protective blood-brain barrier. By packaging luteolin into lipid nanocarriers administered through the nasal passage, this strategy bypasses biological barriers to target the brain directly. This non-invasive delivery method presents a practical approach to relieve brain inflammation, reduce toxic protein build-up, and support cognitive recovery.
This work demonstrates an intranasal nanocarrier platform that could enable pharmaceutical developers to formulate bioactive compounds for neurodegenerative conditions. The approach targets direct nose-to-brain delivery, avoiding invasive administration routes. Because the data is derived entirely from pre-clinical testing in an animal model, the technology remains at an early stage of development and will require extensive formulation scaling, toxicity evaluations, and human clinical trials before reaching commercial use.
AI-generated from the published abstract. Always read the original work before citing.
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 2<sup>3</sup>-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.
This page summarises published work. The authoritative version sits with the publisher.
DOI: 10.3390/pharmaceutics14030576
Is something wrong with this record? Report it or request removal.
Discussion
Have you built on this work, tried to replicate it, or seen it applied in practice? Share what you know. Verified researchers and MARATTO™ domain experts can open a discussion, and any member can reply. Contributions are reviewed before they appear.
No discussion yet. Open the first thread.
New to MARATTO™? Create a free account.
