Formulating cannabinoids with lipid excipients
Cannabinoids: challenging drugs to formulate
Cannabinoids are challenging drugs to formulate:
- Being highly lipophilic compounds with low water solubility, cannabinoids need to be solubilized for subsequent absorption in the gastro-intestinal tract or in the skin.
- With high sensitivity to light, temperature and oxidation, special care has to be taken during handling, processing and storage.
- With high first-pass metabolism, significant food effect and high potency, bioavailability of cannabinoids is highly dependent on the formulation for oral delivery.
- Available as powder, liquid, resin, their physical state may require specific preparation to be incorporated in the dosage form.
High solubilizing capacity of lipid excipients
All our excipients show exceptional solubilizing capacity for cannabinoids and ensure the complete solubilization of the therapeutic dose, whatever the final dosage form.
Solubility data for CBD |
Solubility data for THC |
||
---|---|---|---|
Freely soluble |
Very soluble |
Freely soluble |
Very soluble |
Gelucire® 44/14 Gelucire® 48/16 Gelucire® 50/13 Labrafac™ Lipophile WL 1349 Labrafil® M 1944 CS Labrafil® M 2125 CS Lauroglycol™ FCC Maisine® CC Peceol™ Plurol® Oleique CC 497 Suppocire® AM |
Capryol® PGMC Capryol® 90 Geleol ™ mono and diglycerides NF Labrafac™ PG Labrasol® ALF Lauroglycol™ 90 Transcutol® HP |
Capryol® PGMC Capryol® 90 Labrafac™ Lipophile WL 1349 Labrafil® M 1944 CS Labrafil® M 2125 CS Labrasol® ALF Lauroglycol™ 90 Lauroglycol™ FCC Peceol™ Transcutol® HP |
Labrafac™ PG Maisine® CC Plurol® Oleique CC 497 |
Protecting cannabinoids from degradation during handling and processing
Cannabinoids are very susceptible to degradation in presence of oxygen, light, heat, or at low pH. And most importantly, their degradation metabolites have different effects and potencies. It is therefore critical to prevent degradation during handling and processing and to formulate with care.
CBD ad THC are very sensitive to heat, and should be incorporated at temperatures below 60°C in the formulation to prevent degradation. Furthermore, we have carried out stability studies showing that our lipid excipients provide >95% THC stability, over 3 months at room temperature, eventually admixed with a combination of antioxidants with complementary modes of action.
Formulating cannabinoids for oral and topical routes of administration
With fully solubilized and stabilized cannabinoids, our lipid excipients can help formulate high quality tinctures, drops, sprays, tablets, creams, gels, suppositories.