Liposomal CBD - A Game Changer

by Apoorva Shivankar, M.D

Liposomal CBD - A Game Changer

What is Liposomal CBD?

Seldomly heard a decade before, CBD is the new buzzword in the market involving healthcare, sports, fitness, cosmetics, and whatnot. CBD products are now everywhere even with their controversial legal status. Why? Their work, benefits, efficiency, safety; and last but not the least, happy and satisfied consumers, all stand for CBD.

Come on, let’s have a proper introduction for CBD

CBD (Cannabidiol) is a natural chemical derived from hemp variety of cannabis plants. Being a hemp-extract, it lacks the psychoactive, intoxicating effects of THC; but retains the medicinal benefits of cannabis. Depending on the composition, CBD products are grouped under 3 varieties

  1. Full spectrum CBD – contains the entire spectrum of chemicals present in the cannabis plant including CBD, other cannabinoids, terpenes, flavonoids, and trace amounts of THC. Most potent variety.
  2. Broad spectrum CBD- contains the same entire spectrum of chemicals sans THC.
  3. CBD isolate- 99% pure CBD and nothing else. Least potent but safest.

All these forms of CBD are ruling the markets for their unmatched therapeutic potential. Though none of the CBD products except Epidiolex is approved by Food and drug Administration, they are the most sought-after drugs nowadays.

By working along with the widespread Endocannabinoid system, CBD is able to touch almost every aspect of healthcare. Some of its 

Life-changing health benefits include

  • Happy Day Every day

CBD imposes a magical spell on you with its anti-anxiety, anti-depressant, and stress bursting formula, making you relaxed and relieved every day.

  • Stay Pain - free

CBD is a strong analgesic and an anti-inflammatory agent that can knock out your sufferings from migraines, arthritis, acute injuries, and even neuropathic pains.

  • Dream sleep

By inducing a sense of relaxation and calmness along with a free mind from anxiety, depression; CBD is a well-proven solution for sleep disorders.

  • Ray of Hope for incurable illnesses

CBD has shown positive results in relieving the sufferings of patients with Irritable bowel syndrome, fibromyalgia, Restless leg syndrome, and many more diseases whose cure we are yet to find out.

  • Clear head

By enhancing sleep, relieving anxiety and frustration, CBD clears your head and makes you more alert and focussed. CBD is also known to improve memory and cognition. 

  • Enjoy youthful skin

The antioxidant and anti-inflammatory properties of CBD makes it an apt solution for acne, signs of aging, psoriasis, etc.

  • Epilepsy

CBD is a well-established, food and drug administration certified remedy for rare forms of epilepsy in kids.

  • Protects you from diseases of aging

The neuroprotective benefits of CBD are known to prevent or delay the onset of neurodegenerative disorders such as Alzheimer’s disease, Parkinson’s disease, etc.

And the list goes on..

These benefits make CBD ‘a must have for good health and a quality lifestyle. It undeniably opens 

A gateway to a healthier, stronger, better and beautiful life.’ Doesn’t it?

But Wait, we have a speed breaker here,

The very low BIOAVAILABILITY of CBD products.

By bioavailability, we mean the ability of a drug to be absorbed and utilized by the body.

In humans, this ability to utilize orally ingested CBD is drastically low owing to the 

MIS-MATCH IN THE CHEMISTRY’:

  1. CBD is LIPOPHILLIC - a lipid-lover and dissolves only in lipids not water.
  2. We, the humans, are full of water almost 60%.
  3. Science says, lipid and water can’t come together.

Sad but true.

When taken orally, most of the CBD molecules refuse to dissolve in the aqueous milieu of the human body. Also, a significant amount of CBD is lost when it passes through the harsh digestive system (acids and enzyme attacks) and hence, only 6-9% of CBD reaches the bloodstream to yield the desired effects. The remaining unabsorbed CBD is then flushed out of the body unutilized. What a waste?

Vaping can be an alternative but it lacks long lasting effects.

Thus, to mitigate this tricky question of bioavailability, in came the LIPOSOMAL CBD, a ground-breaking achievement in the field of drug delivery.

What is a Liposomal CBD?

An advanced drug delivery system for CBD molecules to optimize their bioavailability in humans. It provides a water-friendly capsule-like carrier for the CBD molecule to escort its journey within our body. Yes, it’s nothing but

‘CBD encapsulated in a Liposomal molecule’.

But then, what is a liposome? 

ALipid vesicle=pocket of Fat’

A liposome is a spherical vesicle resembling a cell with a highly protective concentric bilayer membrane made up of phospholipids (phosphatidylcholine) which are exactly the same kind as those found in the cell membranes. As liposomes are composed of a similar material as that of cell membranes, they are

  • biocompatible
  • biodegradable
  • biologically inert- evoke a less immunogenic reaction, and
  • better absorbed as they can easily bond and fuse with the cell membranes.

Owing to this, the liposomes are quickly becoming commonplace for targeted drug deliveries. 

Phospholipids are amphiphilic, characterized by a hydrophilic (water-loving) head and hydrophobic (lipophilic) tail on the same molecule. When the bilayer is suspended in an aqueous medium, the hydrophilic heads orient themselves towards the aqueous medium whereas the hydrophobic (lipophilic) tails constitute the inner core forming a bi-layered vesicle-the liposomes.

CBD molecule settles inside this lipophilic core and travels easily through the digestive system, crosses the lining of the digestive tract to get absorbed, and reaches its target safely without any wastage.

Design of a liposome

 

Best known advantage of Liposomal CBD is its significantly increased BIOAVAILABILITY

Here’s how it works- 

Once the CBD products enter the system, the liposomal covering helps them to overcome

4 major barriers to absorption

    1. Water insolubility.
      With its water-friendly heads facing outwards, liposomes easily carry the CBD molecules through our digestive tract.

    2. Gastric acidity. 
      The encapsulating lipid bilayer insulation of liposomes protects CBD from the harsh gastric acidic degradation.

    3. Unwanted protein binding and Enzymatic attacks.
      The liposomal capsule also prevents the unwanted binding of the drug to various proteins and shields it from the enzymatic attacks circulating in the blood, making most of it available to be released at the targeted site of action.

    Additionally, the liposomal delivery system also promotes

    1. Targeted drug delivery-Liposomal bilayer membrane, being made of similar biological components as cell membranes can easily fuse with the membrane of desired cell and deliver CBD directly within the cell

    2. The liposome acts as a depot and ensures controlled slow release of the drug to maintain therapeutic levels for a longer duration without wastage or toxicity.

    Thus, the liposomal carrier of CBD, transports and efficiently releases the drug at the right place, at the right time. As per studies, a good quality liposomal CBD allows 4x better absorption and up to 3x longer-lasting effects. As a result, a better efficacy (INCREASED BIOAVAILABILITY) can be achieved at much lower doses making it cost-effective too.

    Thus, Liposomal CBD comes out to be ‘an IDEAL SOURCE of CBD.’

    Expansion of liposomes in CBD world:

    Liposomal delivery is not restricted to CBD oil or other oral forms only, CBD liposomes are also improving the bioavailability of CBD through transdermal patches especially in cosmetics. 

    But, then the Puzzle arrives,

    How to select the best Liposomal CBD product from the hundreds of similar products in the market?

    Don’t worry, here comes the solution too, 

    Just check for the following characteristics and you are done: 

    • Optimum CBD content from quality strains of hemp-extract.
    • 100% organically grown and naturally processed to exceed industry standards.
    • Phosphatidylcholine content should be higher (around 90%)
    • Phospholipids derived from sunflower lecithin should be preferred.
    • Small liposomal size 100-400nm should be preferred to facilitate easy dispersion.
    • Read label- check for other ingredients.
    • Check for Certificate of Analysis-3rd party tested.
    • Customer reviews are also important as the production of CBD products are not regulated like other drugs.
    • non-GMO.
    • GMP certified. 
    • 100% safe and pure with all-natural ingredients.
    • Vegan, make sure they are soy-, gluten-, and dairy-free

    Is liposomal CBD safe?

    The structure and composition of liposomes is totally physiological (lipid bilayer) and thus do not seem to cause any harm. Even the body easily accepts liposomal forms due to the same reason.

    Multiple studies have been performed to check the safety profile of liposomal delivery and till now no significant untoward effect is found in the human body.

    To conclude:

    With liposomal delivery, you will reap the maximum health benefits of CBD oil in much lower dose and that too for a longer duration. An increased bioavailability of liposomal CBD oil claims:

    ‘NO MORE WASTING OF CBD- NO MORE WASTING OF MONEY.’

    What is Elixinol used for?

    Elixinol is one of the best brands of full-spectrum CBD products marketing CBD oil, CBD capsules, tinctures, balms, creams, and many more. With Elixinol, we get the assured quality as they use 100% organically grown hemp plants for their products and stringently follow all the purity norms. The products undergo double third-party testings to be more sure off.

    Advanced CBD delivery systems:

    • Latest to join the bandwagon are ‘Nano-emulsified CBD/ Nano-liposomes’
    • Fondly known as Tiny soldiers.
    • Comprises of emulsified CBD particles of much smaller size (25 nanometres).
    • The smaller size provides a larger surface area and even better absorption compared to liposomal delivery.
    • Nano-emulsified CBD products are also usually mixed with penetration enhancers such as ethanol or propylene glycol or MCT oil such as coconut
    • Resultant 80% more absorption than conventional methods.

     

    FAQs

    What all Vitamins and nutrients use liposomal drug delivery systems?

    Vitamin A, Vitamin C, Vitamin D3, Vitamin K, cosmetics, hormones, etc.

    Which forms of CBD has the highest bioavailability?

    Intravenous CBD is absorbed almost 100%.

    Here’s a ranking of the bioavailability for different methods of using CBD:

    • Intravenous — 100% absorption
    • Inhalation — up to 40% absorption
    • Sublingual — up to 35% absorption
    • Oral — between 6 and 9% absorption
    • Transdermal (through the skin) — up to 2% absorption

    What is First Pass Effect?

    The first pass effect is a phenomenon of metabolism whereby the concentration of a drug or nutrient is greatly reduced during the digestive process before it reaches the bloodstream.

    Is there any legal THC drug available?

    Yes, 2 medicines called Marinol and Syndros containing Dronabinol (the synthetic form of THC) are approved by the FDA for the treatment of chemotherapy induced nausea and vomiting as well as to treat anorexia due to AIDS.

    Will Hemp-CBD extract give positive drug tests?

    Drug tests are mostly to screen psychoactive compound THC. CBD isolates and broad-spectrum CBD lack THC and hence give negative test results. Hemp-derived full spectrum CBD contains THC in very low amounts but still, the possibility of positive test results especially when taken in higher doses can’t be denied. 

    Does Hemp milk contain CBD?

    No, hemp milk is derived from hemp seeds which are rich in omega 3 and omega 6 fatty acids and lack all cannabinoids including CBD. CBD is present in the leaves and flowers of the hemp plant and hence found in CBD oil and not in hemp milk.

    Can we travel with liposomal CBD oil?

    It depends on the country’s law you are travelling to. Please check the legal status of CBD in the respective country along with the airline rules you are travelling with. The USA allows travelling with food and drug administration approved CBD products.

    CBD products shipping is also legal in the USA, if the CBD oil contains <0.3 % of THC.


    References:

    1. Daeihamed M, Dadashzadeh S, Haeri A, Akhlaghi MF. Potential of Liposomes for Enhancement of Oral Drug Absorption. Curr Drug Deliv. 2017;14(2):289-303. doi: 10.2174/1567201813666160115125756. PMID: 26768542.
    2. Millar SA, Stone NL, Yates AS and O’Sullivan SE.
      A Systematic Review on the Pharmacokinetics of Cannabidiol in Humans. Front. Pharmacol., 26 November 2018 | https://doi.org/10.3389/fphar.2018.01365
    3. Shade CW. Liposomes as Advanced Delivery Systems for Nutraceuticals. Integr M (Encinitas). 2016 Mar;15(1):33-6. PMID: 27053934; PMCID: PMC4818067.
    4. Bruni N, Della Pepa C, Oliaro-Bosso S, Pessione E, Gastaldi D, Dosio F. Cannabinoid Delivery Systems for Pain and Inflammation Treatment. Molecules. 2018 Sep 27;23(10):2478. doi: 10.3390/molecules23102478. PMID: 30262735; PMCID: PMC6222489.
    5. Phytotherapy Research27 No. 5(2013): 633-636, Cannibidiol in Inflammatory Bowel Disease. Authors: G. Esposito, D.D. Filippis, C. Cirillo, T. Iuvone, E. Cappocia, C. Scuderi, A. Steardo, R. Cuomo, L Steardo.
    6. Blessing EM, et al. Cannabidiol as a potential treatment for anxiety disorders. Neurotherapeutics. 2015; 12(4): 825-836.
    7. Rajesh M, Mukhopadhyay P, Bátkai S, Patel V, Saito K, Matsumoto S, Kashiwaya Y, Horváth B, Mukhopadhyay B, Becker L, Haskó G, Liaudet L, Wink DA, Veves A, Mechoulam R, Pacher P. Cannabidiol attenuates cardiac dysfunction, oxidative stress, fibrosis, and inflammatory and cell death signaling pathways in diabetic cardiomyopathy. J Am Coll Cardiol. 2010 Dec 14;56(25):2115-25. doi: 10.1016/j.jacc.2010.07.033. PMID: 21144973; PMCID: PMC3026637.
    8. Linge R, Jiménez-Sánchez L, Campa L, Pilar-Cuéllar F, Vidal R, Pazos A, Adell A, Díaz Á. Cannabidiol induces rapid-acting antidepressant-like effects and enhances cortical 5-HT/glutamate neurotransmission: role of 5-HT1A receptors. Neuropharmacology. 2016 Apr;103:16-26. doi: 10.1016/j.neuropharm.2015.12.017. Epub 2015 Dec 19. PMID: 26711860.
    9. Linares IMP, et al. No acute effects of cannabidiol on the sleep-wake cycle of healthy subjects: A randomized, double-blind, placebo-controlled, crossover study. Front
      Pharmacol
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    10. Mucke M, et al. Cannabis-based medicines for chronic neuropathic pain in adults. Cochrane Database Syst Rev. 2018; 3:CD012182.
    11. Philpott HT, et al. Attenuation of early phase inflammation by cannabidiol prevents pain and nerve damage in rat osteoarthritis. Pain. 2017; 158(12): 2442-2451.
    12. Swaminath A, et al. The role of cannabis in the management of inflammatory bowel disease: A review of clinical, scientific, and regulatory information: Commissioned by the Crohn’s and Colitis Foundation. Inflamm Bowel Dis. 2019; 25(3): 427-435.
    13. CNS Neurol Disorders—Drug Targets13 No. 6 (2014): 953-960, Antidepressant-like and Anxiolytic-like Effects of Cannabidiol: a Chemical Compound of Cannabis sativa. Authors: A.R. de Mello Schier, N.P. de Oliveria Riberio, D.S. Coutinho, S. Machado, et al.
    14. British Journal of Clinical Pharmacology 75 No. 2(May 25, 2012): 323-333,Cannabidiol for Neurogenerative Disorders: Important New Clinical Applications for this Phytocannabinoid? Authors: J. Fernandez-Ruiz, O. Sagredo, M.R. Pazos, C. Garcia, R. Pertwee, R. Mechoulam, J. Martinez-Orgado.

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