Cannabinoids are naturally occurring organic molecular compounds found in the <i>Cannabis sativa</i> plant. Of these cannabinoids, the most studied cannabinoid is tetrahydrocannabinol (THC) and tetrahydrocannabinolic acid (THCa). THC has been shown to exhibit significant antagonistic activity on the CB1 and CB2 receptors within the endocannabinoid system. Therefore, potential therapeutic benefits of THC include acting as an antiemetic, appetite stimulant, analgesic, and anti-convulsant. Although THCa has no psychotropic effect, it has been shown to be a COX-1 and 2 inhibitor, two proteins commonly targeted by nonsteroidal anti-inflammatory drugs. As well as activation of TRPA1 and TRPV4, two ion channels, which mediate several physical and chemical stimuli. The potential therapeutic benefits from these binding effects suggest that THCa may act as a successful anti-inflammatory, neuroprotective, and immunomodulatory pharmaceutical. However, creating oral formulations of cannabinoids can be challenging because they are lipophilic and exhibit poor solubility in gastric fluids leading to low bioavailability. Some estimates are that only 6% of orally administered THC is bioavailable, and little work has been done on the bioavailability of THCa. To optimize drug delivery, amorphous solid dispersions of cannabinoids have been formulated using commonly used melt quench and spray drying techniques. The bioavailability of the cannabinoids was assessed using <i>in vitro</i> dissolution methods in standard gastric fluid mimic solutions. The molecular structure, homogeneity and composition of cannabinoid based amorphous solid dispersions (ASDs) were characterized using nuclear magnetic resonance (NMR) spectroscopy, vibrational spectroscopy, X-ray diffraction and thermal analysis.

Cannabinoid based amorphous solid dispersions

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ACS Fall 2022

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