Poster presentation Gattefossé
See the presentation of Sophie Hughes from Gattefossé at CPhI Worldwide where she talked through a poster presentation on the formulating of cannabinoids with lipid excipients. To find out more about this and Gattefossé´s whole portfolio of solutions come to Hall 10.2 Stand B80 and visit our CPhI Special
Here is the transcript of the video:
Hi. I’m Sophie from Gattefossé, and I’m here at CPhI. And I’m going to talk to you about why you should formulate cannabinoids with lipid excipients.
So, the use of the cannabinoids to treat health problems is not new. It’s been around for 5,000 years. The first pharmacopeia describing cannabinoids was in the 1850s, and individual cannabinoids CBD and THC were actually isolated by chemists in the 1960s. Today, cannabinoids are approved for use in many states in the U.S.A. The first medicinal cannabinoid formulation was approved in 2011 in Europe. It’s an oral spray. And more recently, the USFDA have approved a new cannabinoid-based treatment for epilepsy.
The main cannabinoid compounds are THC and CBD. These are the compounds that are making all the noise at the moment. They’re very similar in molecular structure, but they have different effects. So, they are being investigated for different therapies. On this graph here, we can see on which therapeutic fields cannabinoids are under investigation. So, the top one is the central nervous system, followed by cancer, and then pain management. So, we’ll see new therapies coming out in these therapeutic fields in the future.
What can formulation do for THC and CBD? Well, these molecules are what we call grease balls. Grease balls mean they’re highly lipophilic — they’re soluble in lipids. They have a LogP of 5 or greater. And they have poor water solubility. They’re very sensitive to degradation. And formulation and the right choice of excipients can mitigate some of these problems. Choosing the right excipients can increase solubility and bioavailability, reduce first pass metabolism, and overcome some of the physicochemical stability issues.
So, then which excipients would you recommend using? Well, lipophilic compounds are soluble in lipids. Therefore, lipid-based excipients. Excipients are oils, fatty acid esters, and waxes. The excipients are made with natural plant oils and fatty acids. And many of the excipients in the Gattefossé range were specifically designed to solubilize lipophilic actives like THC and CBD.
So, how does lipid digestion or the digestion of lipid excipients help the absorption of cannabinoids? Well, it all begins in the stomach with digestion. So, when you eat a small amount of lipid, it stimulates the release of digestive enzymes which break down those lipids into components which help the body absorb poorly soluble compounds. And this is nature’s way of making sure that the body gets all the nutrients it needs, even for the soluble ones like vitamins, etc.
So, when you take a lipid excipient, exactly the same thing happens. Gastric lipases are stimulated, and these break down the lipid excipient and helps to maintain the poorly soluble active in solubility, and also prevent precipitation after digestion. So, the long-chain fatty acids that you find in our excipients like Maisine CC, Geloil SC, and soybean oil, they prevent drug precipitation after digestion, and thereby maintain the drug available for absorption.
Preferred administration routes for medical cannabinoids are oral. In this graph down here, we can see that the main drug delivery programs for cannabinoids are focusing on oral, injection, then skin, transmucosal. So, in oral drug delivery, CBDs, THCs are delivered as oily solutions in drops or in capsules. We have a number of excipients that can be used for oral delivery. Their functionality is as an oily vehicle or a self-emulsifying drug delivery system. Then moving onto the transmucosal administration route, here, we have alcohol-free solvents and solubilizers and permeation enhancers to boost drug delivery.
There are a number of research programs, drug delivery programs for cannabinoids in topical delivery for local effect. And Gattefossé offers a range of excipients that are solubilizers, emulsifiers, permeation enhancers. And finally, a forgotten form, but generally important for pediatric and geriatric patients — suppositories. And we have a range of suppocire excipients for powders and resins. Okay?
So, lastly, on this last graph, we can see that there are many drugs already marketed containing cannabinoids, but we can see quite a few in the pre-clinical phase, which means we’ll be seeing more innovative drugs on the market within the next 7-10 years with cannabinoid therapies.
So, I hope you found that useful. Gattefossé has a range of excipients for oral, topical, and rectal delivery. And we’re here at CPhI. So, come by our stand to find out more, or if you don’t have time, there’s more information available on our website. Thank you.
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