Details

Autor(en) / Beteiligte

• Banerjee, Abhinandan
• Hayward, John J
• Trant, John F

Titel

"Breaking bud": the effect of direct chemical modifications of phytocannabinoids on their bioavailability, physiological effects, and therapeutic potential

Ist Teil von

• Organic & biomolecular chemistry, 2023-05, Vol.21 (18), p.3715-3732

Ort / Verlag

England: Royal Society of Chemistry

Erscheinungsjahr

2023

Quelle

MEDLINE

Beschreibungen/Notizen

• Tetrahydrocannabinol (THC) and cannabidiol (CBD) are the two "major cannabinoids". However, their incorporation into clinical and nutraceutical preparations is challenging, owing to their limited bioavailability, low water solubility, and variable pharmacokinetic profiles. Understanding the organic chemistry of the major cannabinoids provides us with potential avenues to overcome these issues through derivatization. The resulting labile pro-drugs offer ready cannabinoid release in vivo , have augmented bioavailability, or demonstrate interesting pharmacological properties in their own right. This review identifies and discusses a subset of these advanced derivatization strategies for the major cannabinoids, where the starting material is the pure phytocannabinoid itself, and the final product either a cannabinoid pro-drug, or a novel pharmacoactive material. The derivatization of THC and CBD for improved bioactivity is reviewed, demonstrating the pharmacophoric versatility, and the limitations of chemical modification, of the cannabinoids. Regulatory and scientific challenges are highlighted.