Nasal CBD reaches the brain and eases autism-like behaviors in rats

Nose-to-brain administration of cannabidiol-loaded polymeric micelles improves the core behavioral symptoms of autism spectrum disorder.

Bioactive materials • • Highly Relevant
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AI Summary

Researchers developed a nasal formulation in which cannabidiol (CBD) is packaged in tiny polymeric micelles. In laboratory testing, the formulation showed good compatibility and permeability in a human nasal-cell model. In autism spectrum disorder (ASD)-like rats, imaging confirmed that intranasal administration delivered the micelles to the brain.

The formulation produced a 27.8% increase in brain CBD concentration 20 minutes after intranasal administration, despite using a dose three times lower than the oral comparison. Behavioral testing also found that the treatment improved core ASD-like symptoms in rats. These are preclinical findings: they do not establish that nasal CBD is effective or safe for people with ASD, and the abstract does not report human outcomes or clinical benefits for cannabis users.

💡 Key Findings

1
CBD-loaded polymeric micelles were compatible with and permeable through a human nasal-cell model.
Moderate
50%
2
In ASD-like rats, imaging confirmed that intranasally administered micelles accumulated in the brain.
Moderate
50%
3
Intranasal delivery produced a 27.8% higher brain CBD concentration 20 minutes after dosing, despite using a dose three times lower than the oral comparison.
Moderate
50%
4
The nasal CBD formulation improved core ASD-like behavioral symptoms in rats.
Moderate
50%

📄 Original Abstract

Neurodevelopmental disorders including autism spectrum disorder (ASD) affect 5.9% of the global population. Research shows the potential therapeutic use of cannabidiol (CBD) to treat different neurodevelopmental disorders, including ASD. Intranasal drug delivery (i.n.) is a non-invasive and painless administration route that enhances drug bioavailability in the brain bypassing the blood-brain barrier. Various polymeric nanoparticles have been investigated for i.n. delivery with different success levels. In this study, we developed and characterized polymeric micelles of the poly(ethylene oxide)-b-poly(propylene oxide) block copolymer Pluronic® F127 loaded with 25% w/w CBD (based on solid weight) for nose-to-brain delivery in ASD. CBD-loaded polymeric micelles display a hydrodynamic diameter of 41 ± 1 nm by Intensity and 23 ± 1 nm by Number, as measured by dynamic light scattering, and very good compatibility and permeability in the human nasal septum cell line RPMI 2650, an in vitro model of the nasal epithelium. The accumulation of CBD-loaded polymeric micelles administered intranasally in the brain of ASD-like rats is confirmed by bioimaging. The CBD pharmacokinetics upon the i.n. (dose of 5 mg/kg) and oral (15 mg/kg) administration of the loaded polymeric micelles shows a 27.8% increase of the CBD concentration in the brain of ASD-like rats 20 min after i.n. administration, despite the 3-fold decrease in the dose. Finally, the efficacy of this nanoformulation to improve the core symptoms of ASD is demonstrated in behavioral studies in a behavioral model of the disorder in rats.

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