Background: The β-caryophyllene (BCP), a phytocannabinoid present in various essential oils, demonstrated
selective action on the CB2 endocannabinoid receptor and attracted considerable attention because of its
several pharmacological activities. Despite this recognized potential, this hydrophobic compound is a volatile and
acid-sensitive sesquiterpene that readily oxidizes when exposed to air, and has low bioavailability in oral formulations.
Thus, the development of formulations that guarantee its stability and increase its bioavailability is a challenge
for its use in the pharmaceutical field.
Methods: The present review brings for the first time a comprehensive overview of the controlled and vectorized
release formulations tested for BCP administration. Among these, we have addressed nanoemulsions, inclusion
complexes with cyclodextrins, liposomes, wound dressings, nanocomposites and nanoparticles. A literature
search was performed on Pubmed, Web of Science and Science direct, and patents documents were also searched
on European Patent Office, World Intellectual Property Organization and Brazilian National Institute of Industrial
Results: The systems presented here may represent an interesting approach to overcome the limitations already
mentioned for this terpene. These systems proved to be promising for improving solubility, stability and controlled
release of this pharmacological relevant sesquiterpene. In the industrial field, some companies have filed
patent applications for the commercial use of the BCP, however, the use of pharmaceutical formulations still
Conclusion: This prospective study evidenced the new perspectives related to BCP vectorization systems in the
pharmaceutical and industrial marketing field and may serve as a basis for further research and pharmaceutical
use of this powerful cannabinoid.