It is well-recognized in the scientific literature that CBD, THC, and other cannabinoids and terpenes, in general, show limited oral bioavailability due to their poor aqueous solubility and extensive first pass metabolism.
To overcome these limitations, a novel self-emulsifying drug delivery system (SEDDS) based on VESIsorb® formulation technology was developed by Vesifact.
Vesifact has recently expanded its scientific research leadership position with two peer-reviewed published studies demonstrating the safety and performance of novel formulations for both Cannabidiol (CBD) and β-caryophyllene (BCP). The studies demonstrated statistically significant improvements for all measured pharmacokinetic parameters for both CBD and BCP. These results are unmatched in the global marketplace compared to all available published literature.
Coenzyme Q10 plays a key role in mitochondrial energy supply and physiology. Due to its poor aqueous solubility and its relatively high molecular weight, the oral bioavailability of CoQ10 is limited.
To overcome these limitations, a novel self-emulsifying drug delivery system (SEDDS) based upon VESIsorb® technology was developed by Vesifact.
The peer-reviewed journal, Alternative Therapies in Health & Medicine, published a human pharmacokinetic study comparing the VESIsorb® CoQ10 formulation with three marketed "bio-enhanced" CoQ10 formulas. The data of this study as well as a comparison with available published literature shows an unmatched enhancement of CoQ10 bioavailability achieved by the VESIsorb® CoQ10 formulation.
While CoQ10 has very low aqueous solubility and a relatively high molecular weight, rendering it poorly bioavailable after oral administration, Omega-3 Essential Fatty Acids (EFAs) are known to be heavily food dependent for oral absorption and bioavailability.
To overcome these obstacles, Vesifact developed a novel self-emulsifying drug delivery system (SEDDS) based on VESIsorb® formulation technology, achieving an industry benchmark for unprecedented active loading, improved bioavailability, and mitigating food dependency. Consumer compliance is dramatically improved with fewer capsules needed to achieve optimized therapeutic blood levels.
Human clinical trials have demonstrated the dramatic improvement in oral bioavailability of these two, science-backed ingredients in both well-designed Phase I study (Pharma, Omega-3 EPA) and peer-reviewed published study (Nutritional, CoQ10) by VESIsorb® formulations. Moreover, the food dependency of the VESIsorb® formulation was significantly mitigated.
Established topically applied non-steroidal anti-inflammatory drugs (NSAID) have fallen short to meet the consumer need for fast-acting pain relief with minimal systemic side effects.
To address this unmet medical need, Vesifact developed a novel Diclofenacs solution utilizing a colloidal droplet delivery system based on VESIsorb® technology.
The results of an in vitro penetration/permeation study using human skin (Franz cell experimental setup) showed that VESIsorb® provided faster and superior delivery of Diclofenac across human skin compared to marketed formulations. The comparator products included the leading brand, Voltaren® (OTC, Emulgel), and the Rx product Pennsaid®, a DMSO-based Diclofenac formulation approved for the topical treatment of osteoarthritic pain.
Ibuprofen, a widely used non-steroidal analgesic drug reaches peak plasma concentrations and maximal analgesic onset only within 1.5 to 2 hours after oral administration. For the treatment of acute pain (e.g., headache), a fast-acting oral dosage form would be highly desired.
To shorten the timeframe between oral administration and onset of action, Vesifact developed a self-emulsifying drug delivery system (SEDDS) based on VESIsorb® technology.
A human clinical study was conducted with the objective to evaluate the pharmacokinetic profile of the Ibuprofen VESIsorb® formulation. The study demonstrated that the time to reach maximum plasma concentration (Tmax) could be reduced from 90 to 35 minutes for a standard oral tablet formulation versus VESIsorb® technology-based capsule formulation.
Treatment of moderate hyperlipidemia with Omega-3 EPA Ethyl Esters requires the medication to be taken with food/fat, which is highly contradicting the general medical advice to reduce fat intake.
To address this marketplace need, Vesifact developed a self-emulsifying drug delivery system (SEDDS) based on VESIsorb® technology to improve the bioavailability and reduce the food/fat dependency of the oral Omega-3 EPA absorption.
The data of a Phase I human pharmacokinetic study showed a 26-fold improvement in bioavailability (AUC) for the VESIsorb® formulation compared to a commercially available Rx brand in the fasted state. Moreover, a dramatically reduced food dependency was observed for the VESIsorb® formulation, whereas the comparator product was highly dependent on food/fat intake for Omega-3 EPA absorption. In conclusion, the VESIsorb® formulation allows the EPA medication to be taken with or without fatty meals.
While various studies have confirmed Panthenol's moisturizing and skin barrier enhancement potential, it is well recognized that Panthenol has limited anti-inflammatory effects after dermal application.
To overcome these limitations, Vesifact developed an aqueous colloidal droplet system based on VESIsorb® technology for use in a proprietary fast-breaking foam spray application.
A UV-induced erythema study in humans clearly demonstrated superior efficacy (reduced redness, improved moisturizing, cooling) and, importantly, early onset of action ("fast-acting") of the VESIsorb® formulation compared to the marketed Panthenol ointment (Bepanthen®) and even comparable to the positive control which was an OTC hydrocortisone formulation.
Skin moisture can principally be improved either by hydrophilic substances binding water on the skin surface (humectants, e.g., glycerol) or by enriching the Natural Moisturizing Factor (NMF) of the skin. There is a significant age-related decline in the levels of NMF.
To supplement the skin with NMF, Vesifact developed a VESIsorb® technology-based liposomal NMF formulation containing a specific triple amino acids complex.
The VESIsorb® liposomal NMF formulation increased skin moisture significantly and dose-dependently during the two weeks of application. The positive effect of the liposome-delivered NMF on skin moisture surpassed that of the humectant control (hydrogel containing glycerol) and was also noticeable 11 days after termination of the treatment. In contrast, the humectant control showed a rapid drop of skin moisture to values lower than before treatment.
It has been well established that cannabinoids in topical applications often have poor chemical stability and limited penetration/permeation across human skin.
In response to this unmet marketplace need, Vesifact developed an aqueous colloidal formulation for incorporation into serums, lotions, salves, and foam sprays as well as a self-emulsifying drug delivery system (SEDDS) for a proprietary Dermagel® application both based on VESIsorb® formulation technology.
Successful storage stability data has been established for both VESIsorb® formulations. A human patch test for primary skin irritation and sensitization showed excellent tolerability in all of the 50 panelists of either sex for both formulations. In addition, an in vitro penetration/permeation study using human skin (Franz cell experimental setup) is underway to measure improvements in penetration, permeation, and onset time.
Dry eyes affects hundreds of millions of people throughout the world and is one of the most frequent causes of patient visits to eye care practitioners. In almost 80% of patients, a lipid layer disorder of the tear film is observed, causing increased evaporation of water from the aqueous phase of the tear film.
To supplement the lipid layer with polar and non-polar lipids, Vesifact developed a VESIsorb® technology-based colloidal droplet formulation containing phospholipids and triglycerides for spray application onto the eyelid. In addition to the lipids, the formulation contains Ectoin, which by itself was shown to be beneficial for the treatment of dry eyes.
A human clinical study showed that the VESIsorb® formulation was as effective for relieving the discomfort associated with dry eyes as the leading liposomal brand, TearsAgain®. In addition, the VESIsorb® formulation can be sterile-filtered and does not require a preservative, certainly a unique benefit for the treatment of chronic dry eyes.
Normally healed, inconspicuous scars are usually line-shaped and are flat, pale and soft. In some cases, scarring is associated with pathological processes such as the formation of a bulge. Occlusion, moisturizing, and UV protection of the scar are thought to prevent abnormal scar healing.
To occlude, moisturize, and protect the scar from UV radiation, Vesifact developed a silicone-free VESIsorb® technology-based formulation, which quickly forms an elastic, tack-free, water and rub-off resistant polymer film after application onto the scar. In addition to the polymer providing occlusion, the formulation contains moisturizers (phospholipids, Equol) and UVA/UVB filters.
A clinical study with patients having surgical scars compared the VESIsorb® formulation with one of the market leaders and benchmark product, Kelo-Cote® UV, a silicone-based formulation. For all patients treated with the VESIsorb® formulation, the scars were healed completely or almost completely after three months. Furthermore, the respective skin portion was identical or highly similar to normal skin. In contrast, all patients treated with the benchmark product still had visible scars after three months. Moreover, the VESIsorb® formulation provided excellent UV protection (SPF 50).
According to the International Menopausal Society, up to 40% of post-menopausal women are affected by vaginal discomfort caused by declining estrogen levels. The local therapy with hormones is controversial. A non-hormonal treatment based on Equol, a phytoestrogen, might represent an effective treatment option.
For efficient vaginal delivery of Equol, Vesifact developed a self-emulsifying drug delivery system (SEDDS) and a colloidal droplet formulation both based on VESIsorb® formulation technology. The SEDDS formulation was administered within a fast dissolving vaginal capsule, whereas the colloidal droplet formulation was administered as a hydrogel.
To show the benefits of Equol for local treatment of menopausal vulvovaginal atrophy (VVA) a clinical study with post-menopausal women was conducted. According to the study results, treatment with Equol showed overall good efficacy and high acceptance in the patients. Symptoms of VVA, such as vaginal itching, vaginal dryness and pain during intercourse, were reduced and therefore both VESIsorb® formulations may improve the quality of life of menopausal women.
