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Human skin permeation of Delta8-tetrahydrocannabinol, cannabidiol and cannabinol.
J Pharm Pharmacol. 2004 Mar; 56(3):291-7.JP

Abstract

The purpose of this study was to quantify the in-vitro human skin transdermal flux of Delta8-tetrahydrocannabinol (Delta8-THC), cannabidiol (CBD) and cannabinol (CBN). These cannabinoids are of interest because they are likely candidates for transdermal combination therapy. Differential thermal analysis and in-vitro diffusion studies with human tissue were completed for the compounds. Heats of fusion, melting points and relative thermodynamic activities were determined for the crystalline compounds, CBD and CBN. Flux, permeability, tissue concentration and lag times were measured in the diffusion experiments. CBN had a lower heat of fusion and corresponding higher calculated relative thermodynamic activity than CBD. Ethanol concentrations of 30 to 33% significantly increased the transdermal flux of Delta8-THC and CBD. Tissue concentrations of Delta8-THC were significantly higher than for CBN. Lag times for CBD were significantly smaller than for CBN. The permeabilities of CBD and CBN were 10-fold higher than for Delta8-THC. Combinations of these cannabinoids with ethanol will be further studied in transdermal patch formulations in vitro and in vivo, as significant flux levels of all the drugs were obtained. CBD, the most polar of the three drugs, and other more polar cannabinoids will also be the focus of future drug design studies for improved transdermal delivery rates.

Authors+Show Affiliations

Division of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, KY 40536-0082, USA. astin2@email.uky.eduNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

15025853

Citation

Stinchcomb, Audra L., et al. "Human Skin Permeation of Delta8-tetrahydrocannabinol, Cannabidiol and Cannabinol." The Journal of Pharmacy and Pharmacology, vol. 56, no. 3, 2004, pp. 291-7.
Stinchcomb AL, Valiveti S, Hammell DC, et al. Human skin permeation of Delta8-tetrahydrocannabinol, cannabidiol and cannabinol. J Pharm Pharmacol. 2004;56(3):291-7.
Stinchcomb, A. L., Valiveti, S., Hammell, D. C., & Ramsey, D. R. (2004). Human skin permeation of Delta8-tetrahydrocannabinol, cannabidiol and cannabinol. The Journal of Pharmacy and Pharmacology, 56(3), 291-7.
Stinchcomb AL, et al. Human Skin Permeation of Delta8-tetrahydrocannabinol, Cannabidiol and Cannabinol. J Pharm Pharmacol. 2004;56(3):291-7. PubMed PMID: 15025853.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Human skin permeation of Delta8-tetrahydrocannabinol, cannabidiol and cannabinol. AU - Stinchcomb,Audra L, AU - Valiveti,Satyanarayana, AU - Hammell,Dana C, AU - Ramsey,Diana R, PY - 2004/3/18/pubmed PY - 2004/7/21/medline PY - 2004/3/18/entrez SP - 291 EP - 7 JF - The Journal of pharmacy and pharmacology JO - J Pharm Pharmacol VL - 56 IS - 3 N2 - The purpose of this study was to quantify the in-vitro human skin transdermal flux of Delta8-tetrahydrocannabinol (Delta8-THC), cannabidiol (CBD) and cannabinol (CBN). These cannabinoids are of interest because they are likely candidates for transdermal combination therapy. Differential thermal analysis and in-vitro diffusion studies with human tissue were completed for the compounds. Heats of fusion, melting points and relative thermodynamic activities were determined for the crystalline compounds, CBD and CBN. Flux, permeability, tissue concentration and lag times were measured in the diffusion experiments. CBN had a lower heat of fusion and corresponding higher calculated relative thermodynamic activity than CBD. Ethanol concentrations of 30 to 33% significantly increased the transdermal flux of Delta8-THC and CBD. Tissue concentrations of Delta8-THC were significantly higher than for CBN. Lag times for CBD were significantly smaller than for CBN. The permeabilities of CBD and CBN were 10-fold higher than for Delta8-THC. Combinations of these cannabinoids with ethanol will be further studied in transdermal patch formulations in vitro and in vivo, as significant flux levels of all the drugs were obtained. CBD, the most polar of the three drugs, and other more polar cannabinoids will also be the focus of future drug design studies for improved transdermal delivery rates. SN - 0022-3573 UR - https://www.unboundmedicine.com/medline/citation/15025853/Human_skin_permeation_of_Delta8_tetrahydrocannabinol_cannabidiol_and_cannabinol_ L2 - https://academic.oup.com/jpp/article-lookup/doi/10.1211/0022357022791 DB - PRIME DP - Unbound Medicine ER -