Mucosal Delivery of Cannabidiol: Influence of Vehicles and Enhancers
In this study, the mucosal permeation and deposition of cannabidiol (CBD) with neat and binary vehicles were investigated. Permeation experiments were performed using static diffusion cells coupled with fresh porcine esophageal mucosa. The CBD–vehicle solutions were applied at a fixed dose (~5 mg/cm...
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| Format: | Article |
| Language: | English |
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MDPI AG
2022-08-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/14/8/1687 |
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| author | Peera Tabboon Thaned Pongjanyakul Ekapol Limpongsa Napaphak Jaipakdee |
| author_facet | Peera Tabboon Thaned Pongjanyakul Ekapol Limpongsa Napaphak Jaipakdee |
| author_sort | Peera Tabboon |
| collection | DOAJ |
| description | In this study, the mucosal permeation and deposition of cannabidiol (CBD) with neat and binary vehicles were investigated. Permeation experiments were performed using static diffusion cells coupled with fresh porcine esophageal mucosa. The CBD–vehicle solutions were applied at a fixed dose (~5 mg/cm<sup>2</sup>), and the corresponding permeation parameters were calculated. In neat vehicles, the permeation flux (<i>J<sub>ss</sub></i>) ranged from 0.89 ± 0.15 to 179.81 ± 23.46 µg·cm<sup>−2</sup>·h<sup>−1</sup>, while the CBD deposition ranged from 11.5 ± 1.8 to 538.3 ± 105.3 μg·cm<sup>−2</sup>. Propylene glycol (PG) and diethylene glycol monoethyl ether (DEGEE) yielded the highest permeability (<i>P<sub>s</sub></i>) and CBD deposition, while medium-chain triglycerides (MCT) yielded the lowest <i>P<sub>s</sub></i> and deposition. This was due to the difference in apparent partition coefficient (<i>K</i>), which is related to the solubility of CBD in the vehicle. The PG:DEGEE binary vehicle boosted <i>J<sub>ss</sub></i> (1.5–1.6 fold) and deposition (2.0–2.7 folds) significantly, compared to neat DEGEE. The combination of DEGEE with MCT dramatically enhanced <i>J<sub>ss</sub></i> (11–44 fold) and deposition (1.6–4.7 fold). The addition of lipophilic enhancers, laurocapram, and oleic acid, to PG:DEGEE and DEGEE:MCT vehicles significantly reduced <i>J<sub>ss</sub></i> (0.3–0.7 fold) and deposition (0.4–0.8 fold) while nerolidol had no effect. These permeation reductions were found to be related to modification of the <i>K</i> and/or diffusivity values. This study provides useful basic information for the development of CBD formulations intended for transmucosal delivery. |
| first_indexed | 2024-03-09T12:45:45Z |
| format | Article |
| id | doaj.art-4e5bf045d95a416db1949cd4071ce4ed |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-09T12:45:45Z |
| publishDate | 2022-08-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-4e5bf045d95a416db1949cd4071ce4ed2023-11-30T22:11:53ZengMDPI AGPharmaceutics1999-49232022-08-01148168710.3390/pharmaceutics14081687Mucosal Delivery of Cannabidiol: Influence of Vehicles and EnhancersPeera Tabboon0Thaned Pongjanyakul1Ekapol Limpongsa2Napaphak Jaipakdee3Division of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Khon Kaen University, Khon Kaen 40002, ThailandDivision of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Khon Kaen University, Khon Kaen 40002, ThailandCollege of Pharmacy, Rangsit University, Pathum Thani 12000, ThailandDivision of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Khon Kaen University, Khon Kaen 40002, ThailandIn this study, the mucosal permeation and deposition of cannabidiol (CBD) with neat and binary vehicles were investigated. Permeation experiments were performed using static diffusion cells coupled with fresh porcine esophageal mucosa. The CBD–vehicle solutions were applied at a fixed dose (~5 mg/cm<sup>2</sup>), and the corresponding permeation parameters were calculated. In neat vehicles, the permeation flux (<i>J<sub>ss</sub></i>) ranged from 0.89 ± 0.15 to 179.81 ± 23.46 µg·cm<sup>−2</sup>·h<sup>−1</sup>, while the CBD deposition ranged from 11.5 ± 1.8 to 538.3 ± 105.3 μg·cm<sup>−2</sup>. Propylene glycol (PG) and diethylene glycol monoethyl ether (DEGEE) yielded the highest permeability (<i>P<sub>s</sub></i>) and CBD deposition, while medium-chain triglycerides (MCT) yielded the lowest <i>P<sub>s</sub></i> and deposition. This was due to the difference in apparent partition coefficient (<i>K</i>), which is related to the solubility of CBD in the vehicle. The PG:DEGEE binary vehicle boosted <i>J<sub>ss</sub></i> (1.5–1.6 fold) and deposition (2.0–2.7 folds) significantly, compared to neat DEGEE. The combination of DEGEE with MCT dramatically enhanced <i>J<sub>ss</sub></i> (11–44 fold) and deposition (1.6–4.7 fold). The addition of lipophilic enhancers, laurocapram, and oleic acid, to PG:DEGEE and DEGEE:MCT vehicles significantly reduced <i>J<sub>ss</sub></i> (0.3–0.7 fold) and deposition (0.4–0.8 fold) while nerolidol had no effect. These permeation reductions were found to be related to modification of the <i>K</i> and/or diffusivity values. This study provides useful basic information for the development of CBD formulations intended for transmucosal delivery.https://www.mdpi.com/1999-4923/14/8/1687cannabidiolcannabinoidspermeationdepositionfatty acidsterpenes |
| spellingShingle | Peera Tabboon Thaned Pongjanyakul Ekapol Limpongsa Napaphak Jaipakdee Mucosal Delivery of Cannabidiol: Influence of Vehicles and Enhancers Pharmaceutics cannabidiol cannabinoids permeation deposition fatty acids terpenes |
| title | Mucosal Delivery of Cannabidiol: Influence of Vehicles and Enhancers |
| title_full | Mucosal Delivery of Cannabidiol: Influence of Vehicles and Enhancers |
| title_fullStr | Mucosal Delivery of Cannabidiol: Influence of Vehicles and Enhancers |
| title_full_unstemmed | Mucosal Delivery of Cannabidiol: Influence of Vehicles and Enhancers |
| title_short | Mucosal Delivery of Cannabidiol: Influence of Vehicles and Enhancers |
| title_sort | mucosal delivery of cannabidiol influence of vehicles and enhancers |
| topic | cannabidiol cannabinoids permeation deposition fatty acids terpenes |
| url | https://www.mdpi.com/1999-4923/14/8/1687 |
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