Bioavailability of CBD Greatly Increased with ANANDA Scientific’s Nano-Enhanced CBD

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Bioavailability of CBD Greatly Increased with ANANDA Scientific’s Nano-Enhanced CBD

Cannabidiol (CBD) from industrial hemp is a multi-functional molecule, and the bioavailability of CBD is greatly increased because of ANANDA.
Scientific studies indicated that it may be a more powerful antioxidant than either Vitamin C or E, and CBD offers the prospect of successfully fighting chronic inflammation and protecting brain cells from reactive oxygen species (1-2).

CBD’s beneficial potential is discussed in numerous published papers. Further, it has promise in stabilizing and even reducing blood sugar levels; as a pain killer; for reducing the risk of artery blockage; in suppressing muscle spasms, seizures, and convulsions; for fighting varied cancers; and more (3-8).

Such promise is accompanied by a major limitation to its usefulness — low bioavailability. Because of this, any beneficial effects from CBD become patchy or erratic due to problems in getting CBD into the body in adequate amounts (9-14).

For a supplement taken by mouth, bioavailability means the proportion of a dose that enters the bloodstream from the small intestine (15-17). Therefore, once in the blood, the supplement can find its way to the target organ or body system, where it then goes to work in supporting health and wellness.

On average, only 5-6% of almost any CBD preparation gets into the bloodstream. As a result, the rest is wasted. Such poor oral bioavailability guarantees variable or unpredictable effects, along with increased costs from having to take larger doses to compensate.

Appropriate formulation strategies that assist in getting into the bloodstream are thus mandatory for CBD to attain its health-giving potential, as well as in a cost-efficient or economical fashion.

ANANDA Scientific’s research & development has yielded a patented CBD technology using GRAS ingredients that resolve CBD’s bioavailability problem. This patented technology is the first of its kind. “GRAS” means that a substance is Generally Recognized As Safe by the US Food and Drug Administration to be used in foods and beverages (18).

Comparison of bioavailability of CBD

Figure 1. ANANDA Scientific’s patented, proprietary technology (nextCBD) involves highly-ordered constructs made from GRAS compounds into which CBD is affixed. Therefore, this technology makes nextCBD very bioavailable when taken by mouth.

Purpose.

This study compares the bioavailability of CBD and ANANDA Scientific’s enhanced CBD in laboratory rats. The bioavailability of substances taken by mouth are comparable between rats and humans (19-28).

Methods.

This demonstration looks at the plasma contents of cannabidiol (CBD) after a single oral dose administered by gavage (through a tube leading down the throat to the stomach; 29) of regular CBD and ANANDA Scientific’s enhanced CBD over a 24-hour period.

In this example, female Sprague-Dawley rats (240-265 gm body weight) were used. The study design and animal usage were reviewed and approved by an Institutional Animal Care and Use Committee (IACUC) for compliance with regulations prior to study initiation. Animal welfare for this study with the U.S. Department of Agriculture’s (USDA) Animal Welfare Act (9 CFR Parts 1, 2, and 3) and the Guide for the Care and Use of Laboratory Animals (30).

A 50-mg CBD/kg body weight model was examined in animals given ANANDA Scientific’s nano-enhanced pure CBD and a control group for which powdered pure CBD in the same amount was fed. Ten animals were in each group.

Blood samples were taken immediately prior to gavage as well as 0.5, 1.0, 2.0, 4.0, 8.0, 12.0 and 24.0 hours after dosing. Venous blood was collected in an EDTA blood collection tube. Next, plasma was separated from red blood cells by centrifugation at 400 g for 15 min., transferred to a fresh microcentrifuge tube, and stored at −80°C.

CBD was quantified using validated high-performance liquid chromatography with tandem mass spectroscopy (LC-MS-MS) in multiple reaction monitoring (MRM) mode.

Findings.

The results verify that ANANDA’s enhanced methods greatly improves bioavailability of CBD. It was significantly more bioavailable than regular CBD at 0.5 and 2 hours.

As a result, far lower dosing is needed for enhanced CBD versus regular CBD. The results also intimate that products containing the regular, non-enhanced CBD found in most products may suffer from low bioavailability and a consequent ineffectiveness.

Study of the bioavailibility of CBD over time

Contact us today to get started with all your CBD needs.

References

1. Burstein, S. 2015. Cannabidiol (CBD) and its analogs: a review of their effects on inflammation. Bioorganic & Medicinal Chemistry 23(7):1377-1385.

2. Couch, D.G., H. Maudslay, B. Doleman, J.N. Lund, and S.E. O’Sullivan. 2018. The use of cannabinoids in colitis: a systematic review and meta-analysis. Inflammatory Bowel Disease 24(4):680-697.

3. Campos, A.C., M.V. Fogaça, A.B. Sonego, and F.S. Guimarães. 2016. Cannabidiol, neuroprotection and neuropsychiatric disorders. Pharmacological Research 112:119-127.


4. Mannucci, C., M. Navarra, F. Calapai, E.V. Spagnolo, F.P. Busardò, R.D. Cas, F.M. Ippolito, G. Calapai. 2008. Neurological aspects of medical use of cannabidiol. CNS & Neurological Disorders Drug Targets 16(5):541-553.

5. McAllister, S.D., L. Soroceanu, and P.Y. Desprez. 2015. The antitumor activity of plant-derived non-psychoactive cannabinoids. Journal of Neuroimmune Pharmacology 10(2):255-267.

6. Pisanti, S., A.M. Malfitan, E. Ciaglia, A. Lamberti, R. Ranieri, G. Cuomo, M. Abate, G. Faggiana, M.C. Proto, D. Fiore, C. Laezza, and M. Bifulco. 2017. Cannabidiol: state of the art and new challenges for therapeutic applications. Pharmacology & Therapeutics 175:133-150.

7. Robson, P.J. . 2014. Therapeutic potential of cannabinoid medicines. Drug Testing and Analysis 6(1-2):24-30.

8. Russo, E.B. 2008. Cannabinoids in the management of difficult to treat pain. Therapeutics and Clinical Risk Management 4(1):245-259.

9. Agurell, S., S. Carlsson, J.E. Lindgren, A. Ohlsson, H. Gillspie, L. Hollister. 1981. Interaction of THC with cannabinol and cannabidiol following oral administration in man. Assay of cannabinol and cannabidiol by mass fragmentography. Experientia 37:1090–1092.

10. Gaston, T.E., and D. Friedman. Pharmacology of cannabinoids in the treatment of epilepsy. Epilepsy & Behavior 70(Pt. B):313-318.

11. , F. 2003. Pharmacokinetics and pharmacodynamics of cannabinoids. Clinical Pharmacokinetics 42(4):327-360.

12. McGilveray, I.J. 2005. Pharmacokinetics of cannabinoids. Pain Research and Management 10(Suppl. A):15A-22A.

13. Ohisson, A., J.E. Lindgren, S. Andersson, S. Agurell, H. Gillespie, L.E. Hollister. 1986. Single-dose kinetics of deuterium-labeled cannabidiol in man after smoking and intravenous administration. Biomed Environ Mass Spectrometry 13:77–83.

14. Samara, E., M. Bialer, R. Mechoulam. 1988. Pharmacokinetics of cannabidiol in dogs. Drug Metabolism and Disposition 16:469–472.

15. Bhattaram, V.A., U. Graefe, C. Kohlert, and H. Derendorf. 2002. Pharmacokinetics and bioavailability of herbal medicinal products. Phytomedicine 9 (Suppl 3):1-33.

16. El-Kattan, A.F. 2017. Oral Bioavailability Assessment: Basics and Strategies for Drug Discovery and Development (Wiley Series on Pharmaceutical Science and Biotechnology: Practices, Applications and Methods). First Edition. Wiley, New York, 448 p.

17. Hu, M., and X. Li. 2011. Oral Bioavailability: Basic Principles, Advanced Concepts, and Applications. First Edition. Wiley, New York, 568 p. 18. GRAS Substances (SCOGS) Database. U.S. Food and Drug Administration. https://www.fda.gov/Food/IngredientsPackagingLabeling/GRAS/SCOGS

19. Akonur, A.I., C.J. Holmes, and J.k. Leypoldt. 2014. Predicting the peritoneal absorption of icodextrin in rats and humans including the effect of β-amylase activity in dialysate. Peritoneal Dialysis International 35(3)288-296.

20. Fagerholm, U., M. Johansson, and H. Lennernäs. 1996. Comparison Between Permeability Coefficients in Rat and Human Jejunum. Pharmaceutical Research 13(9):1336-1342.

21. Lawless E., B.T. Griffin B, A. O’Mahony A, and C.M. O’Driscoll. 2015. Exploring the impact of drug properties on the extent of intestinal lymphatic transport – in vitro and in vivo studies. Pharmaceutical Research 32(50:1817-1829.

22. Nagahara, N., Y. Akiyama, K. Higaki, and T. Kimura. 2006. Animal models for predicting potency of oral sustained-release adhesive microspheres in humans. International Journal of Pharmacy 331(1):46-53.

23. Pang, K.S. 2003. Modeling of intestinal drug absorption: roles of transporters and metabolic enzymes. Drug Metabolism and Disposition 31(12):1509-1517.

24. Salphati, L., K. Childers, L. Pan, K. Tsutsui, and L. Takahashi. 2001. Evaluation of a single-pass intestinal-perfusion method in rat for the prediction of absorption in man. Journal of Pharmacy and Pharmacology 53(7):1007-1013.

25. Stewart, B,H., O.H. Chan, R.H. Lu, E.L. Reyner, H.L. Schmid, H.W. Hamilton, B.A. Steinbaugh, and M.D. Taylor. 1995. Comparison of intestinal permeabilities determined in multiple in vitro and in situ models: relationship to absorption in humans. Pharmaceutical Research 12(5):693-699.

26. Zenghui Teng , Z., C. Yuan , F. Zhang, M. Huan, W. Cao, K. Li, J. Yang, D. Cao, S. Zhou, and Q. Mei. 2012. Intestinal absorption and first-pass metabolism of polyphenol compounds in rat and their transport dynamics in Caco-2 cells. PLoS One 7(1):e29647.

27. Zakeri-Milania,P., H. Valizadeha, H. Tajerzadehc, Y. Azarmia, Z. Islambolchilara, S. Barzegara, and M. Barzegar-Jalalia. 2007. Predicting human intestinal permeability using single-pass intestinal perfusion in rats. International Journal of Pharmacy and Pharmaceutical Sciences 10(3):368-379.

28. Zhang, D., and L._X. Gang. 2012. Preclinical experimental models of drug metabolism and disposition in drug discovery and development. Acta Pharmaceutica Sinica B 2(6):549-561.

29. Andrews, K., and S. McErla. 2012. Oral dosing (gavage) in adult mice and rats. University of British Columbia Animal Care Guidelines, Standard Operating Procedure (SOP) ACC-2012-Tech09.

30. National Research Council and Division on Earth and Life Studies. 2011. Guide for the Care and Use of Laboratory Animals. Eighth Edition. National Academies Press, Washington, D.C., 246 p.

Challenges and Solutions to Flavoring CBD Products

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Challenges and Solutions to Flavoring CBD Products

During the last few years, there’s been challenges in getting CBD products into marketing, and more importantly, good flavoring of CBD. In 2018, most CBD products were tinctures, vapes, softgels or capsules, gummies, dog chews, equine pellets, or in the skincare and cosmetics form.

Back in September 2019, Senate Majority Leader Mitch McConnell (R-KY) moved to insert language into a congressional spending report that calls on the Food and Drug Administration (FDA) to clear a path for the lawful marketing of hemp-derived CBD products.

In draft language shared by the U.S. Hemp Roundtable on Tuesday, the senator is asking FDA to “issue a policy of enforcement discretion with regard to certain products containing CBD” within 120 days. Industry stakeholders say this will clarify rules so that banks are more willing to service CBD companies.

Oil versus powder flavoring CBD

Hydrophobic vs. Oil-based Products

Starting out, all CBD products were hydrophobic/oil-based products. CBD was initially available in two main forms- curde or purified oil extract, or oil soluble powder. These oil-based products were the easiest to make, and required the least amount of effort.  All of the previous applications for CBS were the path of least resistance. With the passage of the 2018 Farm Bill, there was a flood of companies looking to be the first to market. The target audience for CBD products were all true CBD believers. Taste was less important than the medicinal properties of it.

As we move into the next generation of CBD products, we’re seeing more variety in the forms that CBD is offered in such as isolate, powdered, crystal, oil, and more. This variety in forms allows greater control over potency and purity. We’re moving from purely “Medicinal” products to more “Lifestyle” product categories. Some new lifestyle products we’re seeing are RTD Beverages, Shots, Infusions, Sleep Aides, Teas, and Lotions. We’re also seeing food products like mints, candies, gum, and chews.

Flavoring CBD graphEarly adopters with flavoring CBDWater Soluble CBD

Unlike the first generation of oil-based products, new water soluble CBD helps reduce stability problems and increases bioavailability. More refined CBD means less variation in consistency. A lower potency with water soluble products makes it easier to flavor these products.

Growing the category from just the “True Believers” and “Innovators” to begin to serve the “Early Adopters” requires a shift in product development. However, there’s a few hurdles in order to move past that initial 2.5% of the market. Kristen Nichols, from MJBiz Magazine, said, “There’s more to crafting a winning CBD beverage than figuring out how to get the cannabinoid into liquid, though. The bigger challenge is making a beverage people want to drink. Consumers want a tasty beverage that competes against fruit juices or heavily sweetened energy drinks, not something that tastes like medicine.”

Guide to terpines and flavoring CBD

Terpenes

This is where terpenes enter the picture. Terpenes are aromatic oils found in many plants. These  include cannabis varieties that can have distinctive flavors like citrus, berry, mint, piney, nutty, grassy and bitter. Over 100 different terpenes have been identified in the cannabis plant, and every strain tends toward a unique terpene type and composition. There are many factors that influence the taste profile of cannabinoids, including climate, weather, age and maturation, fertilizers, and soil type. Luckily, terpenes can be removed from CBD, but it’s easier to work with them than against them. For example, caryophyllene has a spicy, woody, pepper aroma. Some sample flavors that work with peppery terpenes are peppermint candy, mango chili pepper, cinnamon clove, and hot tamale.

When working with flavors and CBD, formulation will be specific to the strain, source, and delivery method. What you are tasting in CBD products… isn’t pure CBD. It’s the associated terpenes, compounds, chemicals and carriers of that particular ingredient source. As production and processing of CBD improves, the flavor profiles of the CBD of tomorrow won’t be the same as the CBD of today.

Flavoring CBD is important to create a good product

If you have unwanted taste in your CBD, an effective way to block unwanted taste attribute is to confuse the tongue with both different and like sensations. Bitter blockers can be sweet, sour, salt, bitter, or umami. Stevia and monk fruit or malic acic can also mask the taste. It’s important to consider the concentration of your CBD. Flavoring a 10% CBD solution is 90% easier than flavoring an 80% CBD solution. In order to flavor a solution, you must consider dilutions, carriers, delivery method, and emulsions. You must also consider water soluble ingredients that you choose to add to your CBD.

In Conclusion

There’s lots of aspects that go into making a good CBD product. With so many changes happening in the industry, Sensapure can be a great resource to help perfect your product. Send your approved CBD ingredient to our flavor lab to use as the source of your CBD product. Its use in a base product can make a significant difference in determining the best flavor solution. Give us a call to schedule a consult today.

Supply Side West 2018: Flavor Trends Take-aways

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Supply Side West 2018: Flavor Trends Take-aways

We worked with customers on their flavor systems while we learned from key industry experts. We toured the floor and got an inside look at upcoming flavor trends and patterns in the industry. Here are a few things we took away from Supply Side West 2018.

What’s New in Flavor Trends?

Pop Culture Co-branding / Nostalgia

Last year we saw flavor trends of Nostalgia. There was lots of co-branding through old-time favorites like candy flavors, breakfast cereals, and childhood memories like campfire s’mores. This year, nostalgia and co-branding prevailed with new twists on “look-alike” flavors and licensed co-branding deals. We saw flavors that remind us of our childhood, or confirm that we’ve never grown up. After many years of moms reminding us to drink leftover cereal milk, we’re seeing cereal flavored protein products.

Cross Cultural Blends

Tropical and exotic fruits have long been used to “spice up” product lines. And the blending of two different flavors to create a unique taste is also a staple of product development. So it was probably inevitable that these two flavor trends would ultimately connect. This “cross-cultural” blending can be seen in several examples such as “Dragonfruit White Tea” and “Limoncello Lychee.” Add into the equation any of the new international ingredient trends such as kombucha, matcha, açaí, et al. You can see the myriad of possibilities with cross cultural flavor experiences. Industry leaders think about ways these new trendy ingredients pair with interesting flavor systems to create unique customer experiences.

The Hemp Revolution

While the laws regarding cannabis are changing in states across the country, the unavoidable takeaway is asking what this means for the flavor industry as the core ingredients (CBD and THC) present new and unique challenges for an entire health category that has never existed before in the supplemental space. Walking around the show, it was impossible to not see the signs and banners advertising CBD and THC offerings. Add to that the hemp extracts workshops, suppliers, as well as data presented by Natural Products Insider estimating CBD and Hemp rising dramatically by 2022 calling it “The Hemp Revolution,” explaining that because the data is still being collected, it’s probably a far bigger market than we realize.

We had such a great experience at Supply Side West, 2018 and we are looking forward to utilizing the knowledge we gained to help our clients achieve their goals in all things flavors.

—Your Sensapure Team

1945 S. Fremont Drive
Salt Lake City, UT 84104

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