The effectiveness of LPT (Liposome Technology) ensures high bioavailability of cannabidiol, offering a significant advantage over other common delivery methods such as oral, sublingual, or inhalation. In a clinical study conducted in dogs, the injection of LPT-CBD resulted in nearly 100% bioavailability of CBD, significantly outperforming oral administration, which has a reported bioavailability of only 6 to 20%.
Use of CBD-loaded Liposome technology ensures the prolonged and controlled release of synthetic CBD into the bloodstream after a single injection. Our tests have shown that one LPT-CBD injection under the skin provides sufficient CBD exposure across a period of 3 to 4 weeks resulting in an efficacy that can be equivalent to administering oral CBD twice a day for the same time.
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Pharmacokinetic Profile of Innocan subcutaneous injectable LPT-CBD compared to direct intravenous injection of Free CBD
Efficacy and Safety Studies
Anti-inflammatory Efficacy in Mice
We evaluated the effect of LPT-CBD on an inflammatory response induced in mice. Inflammation, which can occur during mechanical tissue injury, is often associated with pain. In this study, mice were subcutaneously injected with various concentrations of LPT-CBD. After 2, 3, and 4 weeks, the mice were stimulated to induce local inflammation in their paws. After 24 hours, paw swelling was measured and compared to a control group of naive mice.
The results, shown in the figure below, indicate that LPT-CBD injections at the tested doses significantly reduced paw swelling at 2, 3, and 4 weeks post-administration. These findings suggest that a single LPT-CBD injection provides a prolonged anti-inflammatory effect lasting at least 4 weeks.
Pain Efficacy in Clinical Dogs with Naturally-Occurring Osteoarthritis
The level of pain in the dogs was scored via the use of Canine Brief Pain Inventory (CBPI) and Pain Interactive Visual Analog Scale (iVAS) methods. CBPI is a validated owner questionnaire that evaluates canine pain severity, while iVAS uses a 0-10 scale for owners to mark their interpreted pain levels of their dogs.
This study demonstrated that a single subcutaneous administration of LPT-CBD provides a long-term analgesic effect, lasting several weeks, as evidenced by:
- Significant improvement in CBPI total scores at weeks 2–3 (p = 0.001 and 0.028, respectively) and borderline improvement at week 6 (p = 0.052)
- Significant improvement in CBPI quality of life at weeks 2–3 (p = 0.046 for both weeks)
- iVAS pain scores were significantly improved at 1–3 weeks (p < 0.001) and at 4 weeks following injection (p = 0.034)
Pharmacokinetics in Clinical Dogs
Plasma samples were collected from each dog to evaluate the pharmacokinetic profile of LPT-CBD. Data was collected at baseline, 2 and 6 hours, 1, 2, and 4 days, and weekly for 1 to 6 weeks. The pharmacokinetic profile of CBD, is presented below.
Results from the pharmacokinetic study show that a single subcutaneous administration of LPT-CBD provides long-term CBD plasma concentrations for up to 6 weeks. LPT-CBD ensures slow drug release, as evidenced by a prolonged time to reach Cmax, indicating a sustained plasma profile. Based on pharmacokinetics calculations it was evidenced that a single dose of 5mg/kg LPT-CBD yielded an area under the curve (AUC) value normalized to dose of 2,351 ng*h/ml/mg/kg (median value of 6 dogs). This value was compared to a previously reported IV study done in dogs with oral CBD and found to be corresponded to 100% bioavailability.
Basic Safety in Clinical Dogs
During the study, dogs were monitored for selected safety parameters, including vital signs, hematology, and serum biochemistry. Local responses at injection sites and other adverse events were also evaluated. Blood samples were collected 1 and 4 weeks after the LPT-CBD injection.
The evaluated safety parameters indicate a good tolerance of the drug.
Mini Pigs drug tolerance
We conducted a pharmacokinetic and basic safety evaluation of LPT-CBD following its subcutaneous administration to minipigs at 3 ascending doses. The animals demonstrated blood levels of CBD for up to 28 days post injection. Importantly, the pigs demonstrated excellent drug tolerance with no drug-related adverse events or injection site reactions (ISR) observed during the study.
Donkey Laminitis
As part of an observational study, we administered a liposomal-CBD injection to an amputee female donkey suffering from Laminitis in its left front limb. This innovative therapy provided immediate, noticeable pain relief and improved mobility.
Goat Scoliosis
In an observational study, we treated a 4-year-old male goat with a liposomal-CBD injection. The LPT-CBD therapy offered significant relief to the animal, which was born with neurological defects and scoliosis, resulting in hind-limb paralysis and fore-limb deformity.
Canine Polyarthritis
A compassionate care trial improved walking abilities and significantly decreased pain in participating canines, in an observational study. An 11-year-old spayed dachshund mix suffering from severe autoimmune-mediated polyarthritis, which caused almost complete inability to walk and severe pain, was included in the trial. Despite treatment with joint supplements (Glycoflex), steroids, and hydrotherapy, the dog remained very lame and could only walk a few steps. After administering Innocan’s liposomal CBD injection in addition to the other treatments, the dog showed remarkable improvement, walking longer distances and much faster than before.
