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

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.

thc_stability_in_gattefosse_excipients

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.