Co-crystallization of hemp oil constituents and assessment for bioaccessibility using the TIM-1 in vitro gastrointestinal digestion model

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In Canada, cannabis may be prescribed as a physician-recommended herbal therapy. While cannabis is typicallysmoked, inhalation of burned dry plant matter has obvious inherent health risks. Oral administration offersseveral key advantages, including elimination of pulmonary health risks and more accurate dosing of activeingredients such as THC and CBD. Oral administration does, however, suffer certain shortcomings andchallenges as well. Bioavailability is defined as the proportion of a drug or other substance that enterscirculation when introduced into the body and so is able to have an active effect. This is therefore an importantproperty to assess when developing cannabis formulations for oral administration. Research has thus far shownthat extensive liver metabolism reduces the oral bioavailability of THC to roughly 2-14%, while inhalation ofmarijuana smoke offers a systemic bioavailability generally ranging between 10-35%. Others have reportedTHC bioavailability after oral ingestion to be approximately 6% compared to 25% after smoking. The goal ofour current research project is to develop novel formulations of cannabinoids in an effort to improve oralbioavailability. Assessing for bioavailability poses some serious challenges, as human or animal subjects arerequired and plasma samples must be drawn. The TIM-1 simulated in vitro gastrointestinal digestion modeldeveloped by TNO in the Netherlands is an advanced dissolution model with high correlation to in vivo testingand has been validated for use in drug delivery testing. Novel formulations can be assessed for bioavailabilityin a quick and cost-effective manner without the need for ethical approval when dealing with human or animaltest subjects. This will allow rapid assessments of formulations and significantly increase the rate of innovationand discovery into enhancing oral bioavailability of cannabinoids.