Reading an interesting article just published end Aug. A lot does go over my head not being from a science background
but....
Inclusion of Medium-Chain Triglyceride in Lipid-BasedFormulation of Cannabidiol Facilitates Micellar SolubilizationIn Vitro, but In Vivo Performance Remains Superior with PureSesame Oil Vehiclehttps://www.mdpi.com/1999-4923/13/9/1349Maybe
@hottod or others might want to have a read through to see what they their thoughts are.
In the AVE Ann back in Oct 2020 "TPM® Cannabinoid Development Program Proceeding to Human Clinical Trials"
HERE they wrote that:
For this study, they were used to compare theamount of CBD absorbed between different formulations. CBD absorption from
formulationscontaining TPM® was compared against a commonly prescribed CBD product comprising CBD at 100mg/ml.I think the question thrown around by some posters was if it was something like prescription Epidiolex used in the comparison which if it was, this is the composition as per
https://www.medicines.org.uk/emc/product/10781#COMPOSITION(my bold)
Each ml of oral solution contains 100 mg cannabidiol.
Excipients with known effect
Each ml of solution contains:
79 mg anhydrous ethanol
736 mg refined sesame oil0.0003 mg benzyl alcohol
For the full list of excipients, see section 6.1.
Reason for the bold is the aforementioned article is:
Abstract:Oral sesame oil-based formulation facilitates the delivery of poorly water-soluble drug cannabidiol (CBD) to the lymphatic system and blood circulation. However, this natural oil-based formulation also leads to considerable variability in absorption of CBD.
It goes on to discuss additional surfactants as part of the study inc TPGS which is noted for various positive attributes:
To enhance further the emulsification and micellar solubilization, nonionic surfactants can be used. In this study, selection of surfactants was based on their hydrophilic–lipophilic balance (HLB) value. Surfactants with an HLB value ranging from 8 to 18 are suitable for the oil in water emulsification. Therefore, Tween 85, Tween 80 and Span 20 have been selected for this study [25,26].
In addition, a derivative of Vitamin E, d-α-tocopherol polyethylene glycol 1000 succinate (TPGS), which has been previously shown as a powerful solubilizer for lipophilic compounds, has also been selected [27–29]. The free α-tocopherol released from TPGS could also prevent the fatty acid oxidation process [30–32]. It has also been reported that TPGS can enhance lymphatic transport of lipophilic compounds by stimulating the chylomicron secretion in Caco-2 cells [33].What I'm curious about is whether the TPM comparison in the Ann was indeed Epidiolex and if so then sesame oil is part of the composition similar to the article.
Some of the thoughts in the discussion in the article on the addition of TPGS as per below:
The TPGS is a surfactant with antioxidant properties,which has been reported to enhance chylomicron formation, as well as potentially beingdelivered into the intestinal lymphatic system by association with the chylomicrons [33].
However, it has also been reported that TPGS and oleic acid-containing mixed micelleshave a negative effect on the bioavailability and lymphatic transport of the antiretroviraldrug saquinavir in comparison to oleic acid microemulsions [64]. Another work suggestedthat TPGS was not hydrolyzed by pancreatic lipase in the GI tract and remains in the intactform until it transports to the enterocyte [58].
Therefore, it is possible that addition of theTPGS restricted the drug association with chylomicrons in the current studyThe overall results of the biodistribution studies suggest that sesame oil has a moreefficient performance in enhancing the intestinal lymphatic transport of CBD compared toboth Formulations 3 and 4.
So again, the question is....was TPM compared against a sesame oil based CBD like Epidiolex (or similar "prescribed" CBD product) and if so, the below early results showed CBD absorption would be enhanced against sesame oil based whereby this recent published article appears to indicate the addition of TPGS doesn't seem to have the same impact?
Study results:
• All TPM® formulations produced higher mean AUC and Cmax than the commercial CBD
formulation.
• Increases in AUC produced by TPM® formulations ranged from ~4-40 times
• Increases in Cmax produced by TPM® formulations ranged from ~6-41 times
• These increases were statistically significant for the best performing TPM® formulations.