Publications, Pharmaceutical

Acute Migraine Relief: Nose-to-Brain Delivery with Lipid Nanoparticles

Migraine is a widespread and debilitating neurological condition, particularly affecting individuals under the age of 50. Current migraine treatments primarily rely on oral analgesics and non-steroidal anti-inflammatory drugs (NSAIDs) for mild symptoms, while triptans or 5-HT1B/1D receptor agonists are used for moderate to severe cases. However, delivering these medications effectively poses a significant challenge due to the difficulty in crossing the blood-brain barrier, which restricts drug delivery to the brain. This limitation often leads to poor bioavailability and reduced therapeutic efficacy in migraine management.

Download Nose-to-Brain Delivery with Lipid Nanoparticles Publication
Author(s): Joana Torres, University of Porto Renata Silva,University of Porto Gonçalo Farias, Aptar Pharma José Manuel Sousa Lobo, University of Porto Domingos Carvalho Ferreira, University of Porto Ana Catarina Silva, University of Porto
28 Oct 2024

To overcome these barriers, research is increasingly focused on alternative delivery systems that bypass the blood brain barrier, such as the nose-to-brain route. This innovative approach involves administering drugs through the intranasal pathway, directly transporting them to the brain, which can improve treatment outcomes for acute migraine. The nose-to-brain route allows drugs to reach the brain more efficiently, avoiding the need to cross the blood brain barrier and enhancing drug concentration at the site of action.

A promising strategy in this field is the use of lipid nanoparticles, particularly solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC). These nanoparticles offer several advantages when administered through the nose-to-brain pathway. They enhance drug absorption and reduce enzymatic degradation, which helps improve the overall bioavailability of the treatment. Moreover, SLN and NLC are capable of co-encapsulating multiple drugs, enabling simultaneous delivery of therapeutic agents to the brain.

This study highlights the potential of SLN and NLC as innovative delivery systems for acute migraine treatment through the nose-to-brain route. The initial sections of the study delve into the pathophysiology of migraines and current pharmacological treatments. It also outlines the mechanisms of drug transport via the nose-to-brain route, emphasizing how this method bypasses the blood-brain barrier, offering a more efficient way to deliver migraine medication.

SLN and NLC have been shown to enhance the effectiveness of drug delivery through the nose-to-brain route. Recent in vivo studies suggest that these nanoparticles significantly increase drug concentrations in the brain compared to conventional oral or intravenous administration. This enhanced delivery is due to the ability of SLN and NLC to encapsulate drugs, protecting them from premature degradation and facilitating a more targeted release.

Moreover, integrating SLN and NLC into in situ-forming hydrogels can further improve their efficacy. These hydrogels extend the retention time of the formulation in the nasal cavity, ensuring a prolonged release and absorption of the medication. This longer residence time allows for higher drug concentrations to reach the brain, potentially providing faster relief for migraine sufferers. This characteristic makes SLN and NLC-based formulations particularly promising for treating acute migraine attacks, where quick and efficient drug delivery is essential.

Despite these promising findings, there remain specific challenges in the application of SLN and NLC for nose-to-brain delivery. One area of interest is the co-encapsulation of different drug classes, such as NSAIDs and triptans, within a single nanoparticle formulation. The combined administration of these two drug types has been shown to prolong the therapeutic effects and prevent migraine relapses, making it a highly desirable treatment strategy. However, to date, no studies have explored the co-encapsulation of NSAIDs and triptans within SLN or NLC, highlighting a significant gap in research and an opportunity for future innovation.

The study concludes that the nose-to-brain route, combined with SLN and NLC, represents a promising alternative to conventional drug delivery methods for treating acute migraines. By facilitating direct drug transport to the brain, this approach can enhance therapeutic outcomes and improve the quality of life for individuals suffering from migraines. The ability of SLN and NLC to co-encapsulate drugs and improve drug delivery through the intranasal route positions them as valuable tools in the development of new migraine therapies.

However, for this technology to advance to clinical use, further research is needed. Future studies should aim to use more reliable in vitro and in vivo models that better mimic human physiology. This will help ensure that the data obtained from experimental studies can be more effectively translated into clinical applications. By addressing these research needs, the scientific community can unlock the full potential of SLN and NLC for nose-to-brain delivery, offering new hope for those affected by acute migraines.

In summary, this review underscores the potential of solid lipid nanoparticles and nanostructured lipid carriers as novel vehicles for delivering migraine medications through the nose-to-brain route. With their ability to bypass the blood-brain barrier and improve drug bioavailability, SLN and NLC could revolutionize the way acute migraines are treated. As research continues to explore the capabilities of these nanoparticles, their application could become a key element in providing more effective and targeted relief for migraine sufferers.

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