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10 results for “cannabinoid system”
Co-Dispersion Delivery Systems with Solubilizing Carriers Improving the Solubility and Permeability of Cannabinoids (Cannabidiol, Cannabidiolic Acid, and Cannabichromene) from Cannabis sativa (Henola Variety) Inflorescences
<p>Article, Dataset for article</p> <p> </p> <h2>Abstract</h2> <div>Cannabinoids: cannabidiol (CBD), cannabidiolic acid (CBDA), and cannabichromene (CBC) are lipophilic compounds with limited water solubility, resulting in challenges related to their bioavailability and therapeutic efficacy upon oral administration. To overcome these limitations, we developed co-dispersion cannabinoid delivery systems with the biopolymer polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol (Soluplus) and magnesium aluminometasilicate (Neusilin US2) to improve solubility and permeability. Recognizing the potential therapeutic benefits arising from the entourage effect, we decided to work with an extract instead of isolated cannabinoids. <span>Cannabis sativa</span> inflorescences (Henola variety) with a confirming neuroprotective activity were subjected to dynamic supercritical CO<sub>2</sub> (scCO<sub>2</sub>) extraction and next they were combined with carriers (1:1 mass ratio) to prepare the co-dispersion cannabinoid delivery systems (HiE). In vitro dissolution studies were conducted to evaluate the solubility of CBD, CBDA, and CBC in various media (pH 1.2, 6.8, fasted, and fed state simulated intestinal fluid). The HiE-Soluplus delivery systems consistently demonstrated the highest dissolution rate of cannabinoids. Additionally, HiE-Soluplus exhibited the highest permeability coefficients for cannabinoids in gastrointestinal tract conditions than it was during the permeability studies using model PAMPA GIT. All three cannabinoids exhibited promising blood-brain barrier (BBB) permeability (P<sub>app</sub> higher than 4.0 × 10<sup>−6</sup> cm/s), suggesting their potential to effectively cross into the central nervous system. The improved solubility and permeability of cannabinoids from the HiE-Soluplus delivery system hold promise for enhancement in their bioavailability.</div> <div> <div> <div>Keywords: </div> <a href="https://www.mdpi.com/search?q=cannabidiol">cannabidiol</a>; <a href="https://www.mdpi.com/search?q=cannabidiolic+acid">cannabidiolic acid</a>; <a href="https://www.mdpi.com/search?q=cannabichromene">cannabichromene</a>; <a href="https://www.mdpi.com/search?q=cannabis">cannabis</a>; <a href="https://www.mdpi.com/search?q=solubility">solubility</a>; <a href="https://www.mdpi.com/search?q=permeability">permeability</a></div> </div>
Cannabinoids Effects on the Pain Modulation System
ClinicalTrials.gov study NCT02560545. IPD Sharing: NO. Countries: 1. Publications: 1.
Figure 3 from: Nocheva H, Sabit Z, Bakalov D, Grigorov E (2021) Interactions between the cannabinoid and the serotonergic systems in modulation of pain perception. Pharmacia 68(1): 109-115. https://doi.org/10.3897/pharmacia.68.e49219
Figure 3 Bidirectional effects of (A) DPAT, (B) AEA, and (C) AEA+DPAT in intact animals and after 1h HS.
Figure 2 from: Nocheva H, Sabit Z, Bakalov D, Grigorov E (2021) Interactions between the cannabinoid and the serotonergic systems in modulation of pain perception. Pharmacia 68(1): 109-115. https://doi.org/10.3897/pharmacia.68.e49219
Figure 2 Effects of CB1-agonist (AEA) and 5НТ1А-agonists (DPAT) alone administration on nociceptive (PP) thresholds in (A) intact animals (int) and (B) animals subjected to 1 hour of heat stress (1h HS) without and after pretreatment with CB1- and 5НТ1А-antagonists (AM and NAN, respectively). PP-thresholds are represented as mean values ± S.E.M. in arbitrary units (AU). ***p < 0.001, **p < 0.01, *p < 0.05 vs. controls. A. +++p < 0.001, ++p < 0.01 vs. int+AEA+DPAT. int+NAN+DPAT were compared to int+DPAT – xxxp < 0.001, xxp < 0.01; int+AM+AEA were compared to int+AEA – $$$ p < 0.001. B. +++p < 0.001, ++p < 0.01 vs. 1h HS; xxxp < 0.001, xxp < 0.01 vs. 1h HS+AEA+DPAT. 1h HS+NAN+DPAT were compared to 1h HS+DPAT – $$$p < 0.001, $$p < 0.01; 1h HS+AM+AEA were compared to 1h HS+AEA – &&&p < 0.001.
Figure 1 from: Nocheva H, Sabit Z, Bakalov D, Grigorov E (2021) Interactions between the cannabinoid and the serotonergic systems in modulation of pain perception. Pharmacia 68(1): 109-115. https://doi.org/10.3897/pharmacia.68.e49219
Figure 1 Effects of CB1- and 5НТ1А-agonists (AEA+DPAT) administration on nociceptive (PP) thresholds in (A) intact animals (int) and (B) animals subjected to 1 hour of heat stress (1 h HS) without and after pretreatment with CB1- and 5НТ1А-antagonists (AM and NAN, respectively). PP-thresholds are represented as mean values ± S.E.M. in arbitrary units (AU). ***p < 0.001, **p < 0.01 vs. controls. A. +++p < 0.001, ++p < 0.01 vs. int+AEA+DPAT. B. +++p < 0.001 vs. 1 h HS; xxxp < 0.001, xxp < 0.01 vs. 1 h HS+AEA+DPAT.
Figure 3 from: Suleymanoglu Y, Bakalov D, Sabit Z, Vodenicharov V, Tafradjiiska-Hadjiolova R, Nocheva H (2024) The endogenous cannabinoid and the adrenergic systems in modulation of stress-response. Pharmacia 71: 1-8. https://doi.org/10.3897/pharmacia.71.e115659
Figure 3 A. Stress (and its many sensory inputs) activates different areas in the brain – the prefrontal cortex (PFC), the thalamus (Thal), the limbic system (LS, comprising the amygdala, hippocampus and hypothalamus), with subsequent adverse effects for the whole organism: fear‐related behaviour, depressive-like conditions, anxiety, helplessness and hopelessness, sleep and feeding disorders; B. Endocannabinoids modulate the activity of pyramidal glutamate neurons and prefrontal glutamatergic plasticity, and have been proved beneficial in decreasing anxiety and depressive-like symptoms, alleviation of fear-conditioned memories, improvement of sleep and feeding.
Figure 2 from: Suleymanoglu Y, Bakalov D, Sabit Z, Vodenicharov V, Tafradjiiska-Hadjiolova R, Nocheva H (2024) The endogenous cannabinoid and the adrenergic systems in modulation of stress-response. Pharmacia 71: 1-8. https://doi.org/10.3897/pharmacia.71.e115659
Figure 2 Effects on r-SIA (1 h RS) estimated by PP-test after A. Clonidine (Clo); B. Desipramine (Des); and C. Yohimbine (Yoh) administrations alone or in combination with anandamide (AEA) / AM251 (AM). Mean values ± S.E.M. are presented in arbitrary units (AU) on the 10th, 20th, 30th, and 40th min after substances administration. A–C ***p < 0.001 vs. controls; +++p < 0.001vs. 1 h RS; xxxp < 0.001vs. A. 1 h RS+Clo; B. 1 h RS+Des; C. 1 h RS+Yoh; xp < 0.05 vs. B. 1 h RS+Des; $$$p < 0.001vs. A. 1 h RS+Clo+AEA; B. 1 h RS+Des+AEA; C. 1 h RS+Yoh+AEA; $p < 0.05 vs. C. 1 h RS+Yoh+AEA.
Figure 1 from: Suleymanoglu Y, Bakalov D, Sabit Z, Vodenicharov V, Tafradjiiska-Hadjiolova R, Nocheva H (2024) The endogenous cannabinoid and the adrenergic systems in modulation of stress-response. Pharmacia 71: 1-8. https://doi.org/10.3897/pharmacia.71.e115659
Figure 1 Effects of AEA on r-SIA estimated by PP-test after one hour of restraint (1 h RS) in rats. Mean values ± S.E.M. are presented in arbitrary units (AU) on the 10th, 20th, 30th, and 40th min after substances administration. ***p < 0.001 vs. controls; +++p < 0.001vs. RS.
Probing the Cannabinoid System in Individuals With a Family History of Psychosis
ClinicalTrials.gov study NCT02102113. IPD Sharing: Not stated. Countries: 1. Publications: 0.
Cannabinoid receptor 2 selective agonist alleviates systemic sclerosis by inhibiting Th2 differentiation through JAK/SOCS3 signaling
GEO Series GSE261552. Mus musculus. 4 samples. Type: Expression profiling by high throughput sequencing.
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OpenNeuro
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