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Development of a Novel Nanoemulsion Formulation to Improve Intestinal Absorption of Cannabidiol
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| Zeitschriftentitel: | Medical Cannabis and Cannabinoids |
|---|---|
| Personen und Körperschaften: | , , , , |
| In: | Medical Cannabis and Cannabinoids, 2, 2019, 1, S. 35-42 |
| Format: | E-Article |
| Sprache: | Englisch |
| veröffentlicht: |
S. Karger AG
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| Schlagwörter: |
| author_facet |
Nakano, Yukako Tajima, Masataka Sugiyama, Erika Sato, Vilasinee Hirunpanich Sato, Hitoshi Nakano, Yukako Tajima, Masataka Sugiyama, Erika Sato, Vilasinee Hirunpanich Sato, Hitoshi |
|---|---|
| author |
Nakano, Yukako Tajima, Masataka Sugiyama, Erika Sato, Vilasinee Hirunpanich Sato, Hitoshi |
| spellingShingle |
Nakano, Yukako Tajima, Masataka Sugiyama, Erika Sato, Vilasinee Hirunpanich Sato, Hitoshi Medical Cannabis and Cannabinoids Development of a Novel Nanoemulsion Formulation to Improve Intestinal Absorption of Cannabidiol Pharmacology (medical) Complementary and alternative medicine Pharmacology |
| author_sort |
nakano, yukako |
| spelling |
Nakano, Yukako Tajima, Masataka Sugiyama, Erika Sato, Vilasinee Hirunpanich Sato, Hitoshi 2504-3889 S. Karger AG Pharmacology (medical) Complementary and alternative medicine Pharmacology http://dx.doi.org/10.1159/000497361 <jats:p><b><i>Background:</i></b> Cannabidiol (CBD) is highly lipophilic, and its oral bioavailability is known to be very low in humans. In this study, we developed a novel nanoemulsion preparation of CBD (CBD-NE) to improve the poor solubility and absorption of CBD. The pharmacokinetic profiles of CBD in rats were evaluated after oral administrations of CBD oil and CBD-NE, and the effect of bile secretion on CBD absorption was also evaluated. <b><i>Methods:</i></b> The CBD-NE formulation developed in this study consisted of vitamin E acetate, ethanol, Tween-20, and distilled water (1.7/3.8/70/24.5, w/w%). A CBD oil formulation (CBD oil, control) 100 mg/kg or CBD-NE 50 mg/kg was orally administered to rats, and the blood samples were collected over time. Moreover, the CBD oil or CBD-NE was orally administered to bile-fistulated rats, and the pharmacokinetic profiles of CBD were also evaluated. CBD concentrations in plasma were measured using LC-MS/MS. <b><i>Results:</i></b> The particle size of CBD-NE was 35.3 ± 11.8 nm. Mean T<sub>max</sub> of CBD-NE was shortened significantly by the factor of 3 (from 8.00 to 2.40 h, <i>p</i> &#x3c; 0.001) and AUC<sub>0–</sub><sub>∞</sub>/dose increased by 65% (from 0.272 ± 0.045 to 0.448 ± 0.087 h L/kg) compared with CBD oil. AUC<sub>0–</sub><sub>∞</sub>/dose and C<sub>max</sub>/dose after oral administration of CBD oil were significantly reduced by the factor of 27 and 23 (<i>p</i> &#x3c; 0.05 and <i>p</i> &#x3c; 0.01), respectively, in bile-fistulated rats compared with the untreated rats. In contrast, all pharmacokinetic parameters after oral administration of CBD-NE were not significantly different between the untreated and bile-fistulated rats. Therefore, these results demonstrated that conventional CBD oil formulation but not CBD-NE requires bile-mediated micelle formation. <b><i>Conclusions:</i></b> The novel NE formulation developed in this study successfully improved the absorption of CBD regardless of bile secretion. The newly developed oral CBD-NE preparation could be useful to achieve a more stable and quicker onset of action by CBD.</jats:p> Development of a Novel Nanoemulsion Formulation to Improve Intestinal Absorption of Cannabidiol Medical Cannabis and Cannabinoids |
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10.1159/000497361 |
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Chemie und Pharmazie Medizin |
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S. Karger AG, 2019 |
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Medical Cannabis and Cannabinoids |
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| title |
Development of a Novel Nanoemulsion Formulation to Improve Intestinal Absorption of Cannabidiol |
| title_unstemmed |
Development of a Novel Nanoemulsion Formulation to Improve Intestinal Absorption of Cannabidiol |
| title_full |
Development of a Novel Nanoemulsion Formulation to Improve Intestinal Absorption of Cannabidiol |
| title_fullStr |
Development of a Novel Nanoemulsion Formulation to Improve Intestinal Absorption of Cannabidiol |
| title_full_unstemmed |
Development of a Novel Nanoemulsion Formulation to Improve Intestinal Absorption of Cannabidiol |
| title_short |
Development of a Novel Nanoemulsion Formulation to Improve Intestinal Absorption of Cannabidiol |
| title_sort |
development of a novel nanoemulsion formulation to improve intestinal absorption of cannabidiol |
| topic |
Pharmacology (medical) Complementary and alternative medicine Pharmacology |
| url |
http://dx.doi.org/10.1159/000497361 |
| publishDate |
2019 |
| physical |
35-42 |
| description |
<jats:p><b><i>Background:</i></b> Cannabidiol (CBD) is highly lipophilic, and its oral bioavailability is known to be very low in humans. In this study, we developed a novel nanoemulsion preparation of CBD (CBD-NE) to improve the poor solubility and absorption of CBD. The pharmacokinetic profiles of CBD in rats were evaluated after oral administrations of CBD oil and CBD-NE, and the effect of bile secretion on CBD absorption was also evaluated. <b><i>Methods:</i></b> The CBD-NE formulation developed in this study consisted of vitamin E acetate, ethanol, Tween-20, and distilled water (1.7/3.8/70/24.5, w/w%). A CBD oil formulation (CBD oil, control) 100 mg/kg or CBD-NE 50 mg/kg was orally administered to rats, and the blood samples were collected over time. Moreover, the CBD oil or CBD-NE was orally administered to bile-fistulated rats, and the pharmacokinetic profiles of CBD were also evaluated. CBD concentrations in plasma were measured using LC-MS/MS. <b><i>Results:</i></b> The particle size of CBD-NE was 35.3 ± 11.8 nm. Mean T<sub>max</sub> of CBD-NE was shortened significantly by the factor of 3 (from 8.00 to 2.40 h, <i>p</i> &#x3c; 0.001) and AUC<sub>0–</sub><sub>∞</sub>/dose increased by 65% (from 0.272 ± 0.045 to 0.448 ± 0.087 h L/kg) compared with CBD oil. AUC<sub>0–</sub><sub>∞</sub>/dose and C<sub>max</sub>/dose after oral administration of CBD oil were significantly reduced by the factor of 27 and 23 (<i>p</i> &#x3c; 0.05 and <i>p</i> &#x3c; 0.01), respectively, in bile-fistulated rats compared with the untreated rats. In contrast, all pharmacokinetic parameters after oral administration of CBD-NE were not significantly different between the untreated and bile-fistulated rats. Therefore, these results demonstrated that conventional CBD oil formulation but not CBD-NE requires bile-mediated micelle formation. <b><i>Conclusions:</i></b> The novel NE formulation developed in this study successfully improved the absorption of CBD regardless of bile secretion. The newly developed oral CBD-NE preparation could be useful to achieve a more stable and quicker onset of action by CBD.</jats:p> |
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| author | Nakano, Yukako, Tajima, Masataka, Sugiyama, Erika, Sato, Vilasinee Hirunpanich, Sato, Hitoshi |
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| description | <jats:p><b><i>Background:</i></b> Cannabidiol (CBD) is highly lipophilic, and its oral bioavailability is known to be very low in humans. In this study, we developed a novel nanoemulsion preparation of CBD (CBD-NE) to improve the poor solubility and absorption of CBD. The pharmacokinetic profiles of CBD in rats were evaluated after oral administrations of CBD oil and CBD-NE, and the effect of bile secretion on CBD absorption was also evaluated. <b><i>Methods:</i></b> The CBD-NE formulation developed in this study consisted of vitamin E acetate, ethanol, Tween-20, and distilled water (1.7/3.8/70/24.5, w/w%). A CBD oil formulation (CBD oil, control) 100 mg/kg or CBD-NE 50 mg/kg was orally administered to rats, and the blood samples were collected over time. Moreover, the CBD oil or CBD-NE was orally administered to bile-fistulated rats, and the pharmacokinetic profiles of CBD were also evaluated. CBD concentrations in plasma were measured using LC-MS/MS. <b><i>Results:</i></b> The particle size of CBD-NE was 35.3 ± 11.8 nm. Mean T<sub>max</sub> of CBD-NE was shortened significantly by the factor of 3 (from 8.00 to 2.40 h, <i>p</i> &#x3c; 0.001) and AUC<sub>0–</sub><sub>∞</sub>/dose increased by 65% (from 0.272 ± 0.045 to 0.448 ± 0.087 h L/kg) compared with CBD oil. AUC<sub>0–</sub><sub>∞</sub>/dose and C<sub>max</sub>/dose after oral administration of CBD oil were significantly reduced by the factor of 27 and 23 (<i>p</i> &#x3c; 0.05 and <i>p</i> &#x3c; 0.01), respectively, in bile-fistulated rats compared with the untreated rats. In contrast, all pharmacokinetic parameters after oral administration of CBD-NE were not significantly different between the untreated and bile-fistulated rats. Therefore, these results demonstrated that conventional CBD oil formulation but not CBD-NE requires bile-mediated micelle formation. <b><i>Conclusions:</i></b> The novel NE formulation developed in this study successfully improved the absorption of CBD regardless of bile secretion. The newly developed oral CBD-NE preparation could be useful to achieve a more stable and quicker onset of action by CBD.</jats:p> |
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| imprint | S. Karger AG, 2019 |
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| institution | DE-D275, DE-Bn3, DE-Brt1, DE-Zwi2, DE-D161, DE-Gla1, DE-Zi4, DE-15, DE-Pl11, DE-Rs1, DE-105, DE-14, DE-Ch1, DE-L229 |
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| series | Medical Cannabis and Cannabinoids |
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| spelling | Nakano, Yukako Tajima, Masataka Sugiyama, Erika Sato, Vilasinee Hirunpanich Sato, Hitoshi 2504-3889 S. Karger AG Pharmacology (medical) Complementary and alternative medicine Pharmacology http://dx.doi.org/10.1159/000497361 <jats:p><b><i>Background:</i></b> Cannabidiol (CBD) is highly lipophilic, and its oral bioavailability is known to be very low in humans. In this study, we developed a novel nanoemulsion preparation of CBD (CBD-NE) to improve the poor solubility and absorption of CBD. The pharmacokinetic profiles of CBD in rats were evaluated after oral administrations of CBD oil and CBD-NE, and the effect of bile secretion on CBD absorption was also evaluated. <b><i>Methods:</i></b> The CBD-NE formulation developed in this study consisted of vitamin E acetate, ethanol, Tween-20, and distilled water (1.7/3.8/70/24.5, w/w%). A CBD oil formulation (CBD oil, control) 100 mg/kg or CBD-NE 50 mg/kg was orally administered to rats, and the blood samples were collected over time. Moreover, the CBD oil or CBD-NE was orally administered to bile-fistulated rats, and the pharmacokinetic profiles of CBD were also evaluated. CBD concentrations in plasma were measured using LC-MS/MS. <b><i>Results:</i></b> The particle size of CBD-NE was 35.3 ± 11.8 nm. Mean T<sub>max</sub> of CBD-NE was shortened significantly by the factor of 3 (from 8.00 to 2.40 h, <i>p</i> &#x3c; 0.001) and AUC<sub>0–</sub><sub>∞</sub>/dose increased by 65% (from 0.272 ± 0.045 to 0.448 ± 0.087 h L/kg) compared with CBD oil. AUC<sub>0–</sub><sub>∞</sub>/dose and C<sub>max</sub>/dose after oral administration of CBD oil were significantly reduced by the factor of 27 and 23 (<i>p</i> &#x3c; 0.05 and <i>p</i> &#x3c; 0.01), respectively, in bile-fistulated rats compared with the untreated rats. In contrast, all pharmacokinetic parameters after oral administration of CBD-NE were not significantly different between the untreated and bile-fistulated rats. Therefore, these results demonstrated that conventional CBD oil formulation but not CBD-NE requires bile-mediated micelle formation. <b><i>Conclusions:</i></b> The novel NE formulation developed in this study successfully improved the absorption of CBD regardless of bile secretion. The newly developed oral CBD-NE preparation could be useful to achieve a more stable and quicker onset of action by CBD.</jats:p> Development of a Novel Nanoemulsion Formulation to Improve Intestinal Absorption of Cannabidiol Medical Cannabis and Cannabinoids |
| spellingShingle | Nakano, Yukako, Tajima, Masataka, Sugiyama, Erika, Sato, Vilasinee Hirunpanich, Sato, Hitoshi, Medical Cannabis and Cannabinoids, Development of a Novel Nanoemulsion Formulation to Improve Intestinal Absorption of Cannabidiol, Pharmacology (medical), Complementary and alternative medicine, Pharmacology |
| title | Development of a Novel Nanoemulsion Formulation to Improve Intestinal Absorption of Cannabidiol |
| title_full | Development of a Novel Nanoemulsion Formulation to Improve Intestinal Absorption of Cannabidiol |
| title_fullStr | Development of a Novel Nanoemulsion Formulation to Improve Intestinal Absorption of Cannabidiol |
| title_full_unstemmed | Development of a Novel Nanoemulsion Formulation to Improve Intestinal Absorption of Cannabidiol |
| title_short | Development of a Novel Nanoemulsion Formulation to Improve Intestinal Absorption of Cannabidiol |
| title_sort | development of a novel nanoemulsion formulation to improve intestinal absorption of cannabidiol |
| title_unstemmed | Development of a Novel Nanoemulsion Formulation to Improve Intestinal Absorption of Cannabidiol |
| topic | Pharmacology (medical), Complementary and alternative medicine, Pharmacology |
| url | http://dx.doi.org/10.1159/000497361 |