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Truly Water-Soluble Cannabinoids for Sleep

Updated: Jan 23

Consumers increasingly report seeking cannabis and cannabinoids for sleep problems, and recent research advancements have shown an extensive relationship between the endocannabinoid system and the physiological regulation of sleep and wakefulness.

With increased sleep-promoting cannabinoid product formulations in the marketplace, formulators can set themselves apart from the competition with innovative water-soluble cannabinoids.

Chronic Sleep Disorders

According to the Centers for Disease Control and Prevention (CDC), an estimated 70 million Americans suffer from chronic sleep problems. A persistent lack of sleep contributes to the risk of chronic illnesses, mental health problems, and a poor quality of life.

Chronic sleep disorders include:

  • Insomnia: problems falling asleep or staying asleep

  • Narcolepsy: excessive, uncontrollable daytime sleepiness

  • Restless Legs Syndrome (RLS): an uncomfortable urge to move the legs while sitting or lying down

  • Sleep apnea: a sleep disorder in which breathing starts and stops during sleep

Sleep problems affect overall health substantially and should be taken seriously. Chronic sleep disorders increase the risk of several serious health conditions, such as depression, diabetes, and cardiovascular disease.

Do Cannabinoids Aid Sleep?

The endocannabinoid system is a physiological system that modulates interconnected biological processes related to maintaining homeostasis, including sleep and wakefulness.

Cannabinoid therapies for sleep disorders are of growing interest to researchers, clinicians, and consumers, and some scientific evidence shows the potential benefits of cannabis and cannabinoids for sleep. A 2017 survey of over 1,500 New England dispensary members found that roughly (65.2%) decreased the use of sleep medications following medical cannabis use. A recent review of 10 studies found that treating posttraumatic stress disorder (PTSD) with cannabinoids improved PTSD-associated sleep disorder symptoms. Some states, including New Mexico and Minnesota, list obstructive sleep apnea as a qualifying medical condition for their medical cannabis programs.

A zeitgeber is an external or environmental time cue that synchronizes circadian rhythms, or the body’s natural clock. Zeitgebers cue the body’s physiology for patterns of rest and wakefulness. For example, sleep-related zeitgebers include sunlight, bedroom temperature, alarm clocks, sunrise and sunset, eating and drinking habits, and social cues. Some research shows tetrahydrocannabinol (THC) in cannabis may act as a zeitgeber for some people with disrupted circadian function by signaling the biological clock when it is time to sleep.

Cannabidiol (CBD) and Sleep

Cannabidiol (CBD) is a non-intoxicating cannabinoid with potential uses for sleep problems, including insomnia and REM sleep behavior disorder. CBD also has possible wake-promoting effects for excessive daytime sleepiness.

Cannabinol (CBN) and Sleep

The most prominent cannabinoid in cannabis plants after THC and CBD is cannabinol (CBN). It is formed as a byproduct when THC degrades over time. Many cannabis consumers believe increased CBN in stale cannabis flower causes sleepiness, but there are currently not enough rigorous studies to scientifically establish a sedative effect.

Water-Soluble Cannabinoids Solve Sleep Product Formulation Challenges

Cannabinoid bioavailability in a product formulation describes the extent to which a cannabinoid reaches its intended site of physiological action. A cannabinoid with low bioavailability requires a higher dose to achieve a physiological effect. When product formulators enhance cannabinoid bioavailability, a lower dose is needed to reach the same threshold of effectiveness.

Cannabinoids are hydrophobic or “water-fearing” molecules that do not naturally dissolve in water. Formulators enhance bioavailability by improving cannabinoid water solubility. Traditional methods to improve cannabinoid water solubility, such as emulsification, vary in effectiveness because they do not fundamentally change the hydrophobic molecular structure. However, truly water-soluble cannabinoids demonstrate substantially increased bioavailability, resulting in lower amounts required in product formulations to achieve a consistent physiological effect.

Formulators of sleep-supporting cannabinoid products use innovative water-soluble cannabinoid ingredients to optimize effectiveness and improve dose consistency. Specificity in sleep-related cannabinoid dosing is essential because of the biphasic response, a term to describe a pharmacological phenomenon where the same substance can promote opposite responses at a low dose compared to a high dose. For example, a low THC dose may cause drowsiness, whereas a high dose may increase energy or anxiety. Furthermore, consumers should avoid excessive THC doses because tolerance can develop if supratherapeutic doses are consumed consistently. Therefore, cannabinoid product formulators ensure consistent dosages in sleep formulations by optimizing bioavailability for predictable physiological results.

Takeaways On Water-Soluble Cannabinoids for Sleep

Innovations in truly water-soluble cannabinoid ingredients improve the bioavailability and efficacy of cannabis and hemp product formulations well beyond the results achieved with nanotechnology and other traditional methods to improve cannabinoid bioavailability. Water-soluble cannabinoids allow formulators to create cannabinoid products that deliver predictable and biologically available cannabinoids for sleep support.

Our flagship ingredient, CannaSorb CB Active, is made via a patented process akin to polysorbate chemistry. While other ingredients aim to make hydrophobic compounds more hydrophilic, CannaSorb CB Active is made by chemically reacting a fat-soluble compound and converting it into a water-soluble compound. This process creates an opaque liquid that dilutes quickly, easily, and fully into water to create a clear, stable, permanent solution.

You're in the right place if you seek high-value cannabis formulation ingredients and white-label opportunities. Our industry know-how and expert support at Synergy Life Science will help you get your high-quality products on the retail shelves efficiently and affordably. Contact us here to find out more.

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