Research

Overview

The safety and effectiveness of Lexaria’s DehydraTECH™ technology has been extensively and thoroughly studied. Since 2015, a series of controlled and well designed in vitro and in vivo, , animal and human studies; as well as extensive molecular characterization investigation has been completed on molecules including nicotine and nicotine analogues, cannabinoids, NSAIDs and antiretroviral drugs.

Performance of total bioabsorption (directly and indirectly through surrogate biomarkers),blood-brain-barrier delivery characteristics, rapidity of onset, consumer appeal, metabolite production (an indication of first-pass liver bypass) and quality of effectiveness have all been quantified.  Studies to-date have focused on nicotine, NSAID and cannabinoid applications, although research is underway for the other bioactive compounds named in Lexaria’s patent portfolio and described under Commercial Applications.

Most urgently, Lexaria is currently investigating the role of DehydraTECH in improving delivery characteristics of antiretroviral drugs as potential treatment options against Coronavirus.

Pre-Clinical Research into Lexaria’s DehydraTECH™

An in vitro absorption study was performed to assess unidirectional CBD permeability using a human epi-intestinal tissue model with various formulations in the presence of simulated intestinal fluid.  The study was designed to, as closely as possible, mimic intestinal absorption as it would occur in a live subject.  Samples of Lexaria’s commercially available CBD-fortified ViPova™ black tea were administered in the model compared with concentration-matched CBD control preparations that lacked Lexaria’s patented formulation and process enhancements.  The study showed as much as a 499% improvement, on average, in intestinal tissue permeability with the ViPova™ black tea formulation relative to a concentration-matched CBD control preparation without any Lexaria technology enhancements.  The study also showed a 325% improvement, on average, in intestinal tissue permeability comparing the ViPova™ black tea preparation to a concentration-matched CBD control preparation that utilized Lexaria`s dehydration synthesis processing methodology but lacked its fatty acid ingredient incorporation, demonstrating the power of the Lexaria technology as a whole (see Figure 1).

medical cannabinoid research Lexaria Bioscience Corp. | Cannabis Research |

Figure 1

Clinical Research into Lexaria's DehydraTECH™

A series of independent, well designed and controlled human focus studies were undertaken in 2016 and 2017 corroborating Lexaria’s in vitro performance findings.  A study in healthy volunteers (n=6) suggested as much as a 5-10X increase in CBD absorption, which was assessed indirectly through measurement of the increase in salivary nitric oxide as a directly proportional surrogate biomarker, with onset of action in as little as 15-30 minutes.  In all cases, the maximum increased level of salivary nitric oxide remained evident at the 60-minute end period of this particular test. Further testing is required to determine the full duration of elevated nitric oxide levels.

Thereafter, a blinded human focus study was conducted to evaluate the performance of THC-infused chocolates formulated using Lexaria’s DehydraTECH™ technology.  This study compared the performance of the THC-infused chocolates powered by Lexaria’s technology to concentration matched THC-infused chocolates formulated using a commercial dextrin absorption enhancer.  The subjects (n=12) that participated in this study indicated a clear preference on taste and overall effectiveness with the chocolates formulated using Lexaria’s technology, and onset of effectiveness was again observed very quickly, in as little as 15-20 minutes.

An additional blinded human focus study (n=40) was conducted to evaluate other consumer products formulated with and without DehydraTECH. Once again, subjects communicated their experiences that the DehydraTECH-empowered products acted more quickly and had preferred taste profiles compared to the non-DehydraTECH products.

2018 European Human Clinical Study

Lexaria’s DehydraTECH™ – Powered TurboCBD™ vs. Control

Lexaria also undertook, in conjunction with a leading medical research university in Europe, the world’s first human study designed to evaluate whether cannabinoid supplementation, delivered through Lexaria’s consumer product TurboCBD™, liberates nitric oxide and improves vascular health (endothelial function) in otherwise healthy young and old humans. These studies also expected to quantify the influence of cannabidiol “CBD” on performance of both cognitive and/or physical exercise. Elevation in oxidative stress is a normal part of aging and noted in cardiovascular diseases and type 2 diabetes. Older populations have experienced improvements in vascular function in combination with antioxidants. It is postulated that older adults may benefit more than younger adults from CBD supplementation and potential antioxidant capacity, liberation of endothelial-derived nitric oxide and improved vascular function through vaso-relaxation.

The degree and speed of CBD absorption into blood plasma was tested in a randomized, placebo-controlled, double-blind clinical study in 12 healthy human volunteers comparing a 90 mg CBD dose of Lexaria’s TurboCBD™ powered by its patented DehydraTECH™ absorption and palatability enhancing technology to a concentration-matched control formulation without DehydraTECH™ incorporation.

Key Study Highlights

Higher Quantities delivered:

  • Lexaria’s DehydraTECH™ delivered 317% more CBD to blood at the 30 min mark than the control (18.4 ng/mL vs. 4.4 ng/mL; 95% CI, p=0.051);
  • By the 60 min mark, Lexaria’s DehydraTECH™ delivered more CBD to the blood than the control was able to achieve at any point during the 6 hour study (38.8 ng/mL);
  • By the 90 min mark, Lexaria’s DehydraTECH™ delivered 86% more CBD than the control (53 ng/mL vs. 28.4 ng/mL; 95% CI, p=0.034).

Lower Human Blood Pressure:

  • Mean arterial blood pressure (MAP) in a subgroup analysis was significantly decreased with only the TurboCBD™ 90 mg dose relative to baseline (p < 0.05).

Increased Blood Volumes:

  • Cerebral perfusion analysed by an index of conductance in the middle cerebral artery (MCA) in this subgroup was significantly higher with only the TurboCBD™ 90 mg dose relative to baseline (p < 0.001).

Results from this study were compared to the findings from a Mount Sinai study* previously conducted with orally administered CBD furnished by market leader GW Pharmaceuticals LLC (maker of FDA-approved Epidiolex), suggesting that Lexaria’s DehydraTECH™ delivered over 900% more CBD to the blood in the first 30 min than the GW formulation on a concentration-adjusted basis.

Lexaria chose to work with CBD in this study both to study its characteristics and also as a proxy for other cannabinoids and believes it was an accurate representation of similar expected performance from other cannabinoids.

Lexaria Bioscience Corp. will continue to evaluate global opportunities for research and development that leads to a better understanding of its technology at work.

2019 Studies

Lexaria conducted extensive animal testing during 2019, proving that its patented drug delivery formulations were superior to those commonly used in certain industry sectors. In the first set of tests, 10 male Sprague-Dawley rats were used in each arm of the study and blood was drawn at 2-minute intervals beginning at the 2-minute mark.

Speed and Effectiveness:

  • Lexaria formulations reached the blood stream in just 2 minutes.
  • At the 15-minute mark, Lexaria formulations delivered 475% more CBD into bloodstream than standard industry formulations.
  • Over the entire 60-minute study, the animals that received the standard DehydraTECH LCFA formulation achieved an average maximum CBD blood concentration level that was 334% more than the average maximum blood concentration level of the animals that received the MCT oil formulation (p<0.0021).
  • Over the entire 60-minute study, the area under the curve (AUC) (total quantity of CBD delivered) for the Lexaria DehydraTECH LCFA formulation was 389% more than the MCT oil formulation (p<0.0011).

Above: Lexaria LCFA Formulation vs. MCT Formulation

In an additional series of tests, another 10 male Sprague-Dawley rats were used in each arm of a study investigating new Lexaria formulations hypothesized to offer additional performance benefits. We have called these improvements “Enhanced DehydraTECH.”

Speed and Effectiveness:

  • Enhanced DehydraTECH led to 811% more CBD delivery into blood than generic industry MCT coconut-oil formulations (p=0.00008);
  • Enhanced DehydraTECH delivered 110% more CBD into blood than DehydraTECH in its traditional format (p=0.02)
  • Enhanced DehydraTECH delivered roughly twice as much CBD to animal blood at all measured time points in the study from the 15-minute mark onwards, compared to traditional DehydraTECH; and during the same time points from 717% to 1098% more CBD than the generic industry MCT coconut oil formulations
  • Enhanced DehydraTECH delivered an astonishing 1,937% more CBD into animal brain tissue after 8 hours compared to generic industry MCT coconut oil formulations; and 487% more than traditional DehydraTECH.

2019 Molecular Characterization Studies

Lexaria has had a long working relationship with the National Research Council (the “NRC”) of Canada, the largest federal research and development organization in Canada. Among other tasks, the NRC investigated whether Lexaria’s DehydraTECH technology caused the formation of a new molecular entity (an “NME”). NME’s are often subjected to intense scientific and regulatory rigor due to the unknowns related to human safety.

The NRC conducted an intense program on behalf of Lexaria, preparing over 50 formulations and using 33 of them for in-depth analytical examination. Active Pharmaceutical Ingredients (API’s) tested included CBD and THC, pure nicotine, nicotine polacrilex, and pure ibuprofen.

Analytical work included extensive use of liquid chromatography high-resolution mass spectrometry (“LC-HRMS”), nuclear magnetic resonance (“NMR”), and Fourier transform infrared (“FTIR”) spectroscopy. NMR was utilized as the main analytical technique due to it quantitative nature and ability to directly characterize the molecular construction of formulate products. The NMR and FTIR analyses demonstrated no shift in the spectral positioning for the API’s for all formulations tested, providing nearly incontrovertible evidence of a lack of any covalent-bonded NME.

A final part of 2019 molecular characterization work involved investigation of stability under varied pH conditions. The R&D program also tested Lexaria’s formulations at highly acidic levels of pH 1.12 and mildly acidic levels of pH 4.82, and Lexaria was delighted to report no chemical modification or presence of degradation of the API’s for both of the formulation classes analysed in this aspect of the program: cannabinoids and nicotine polacrilex