The research is very clear that the biggest obstacle to boosting NAD+ levels is bioavailabilty.  We took the first step in solving that problem with our NMN and NAD+ powders and sublingual tablets.

Now we’ve taken an even bigger step with our advanced nanoliposome hydrogel featuring Control Release Kinetics designed for sublingual delivery.

LSG™ – combining the power of Liposomes & Sublingual delivery in advanced Gel technology

LSG™ nanoparticles are 20-40 nanometers – smaller than wavelengths of visible light – to maximize biological efficiency and precision performance. Smaller lipsomes penetrate the epithelium more readily, and are not filtered out by the liver as larger liposomes are.

This sublingual delivery system features Control Release Kinetics™, using sustained release liposomes to protect nutrients before release into systemic circulation with improved efficacy.

Our nanoparticulate Gel technology is formulated to improve active compound permeability across the epithelium, provide optimal solubilization and maximize systemic release kinetics.

LIPOSOMES

Liposomes are vesicles comprised of phospholipid molecules – the same molecules that comprise cell membranes. Liposomal drug delivery systems have excellent biocompatibility, low toxicity and lack of immune system activation.

Phospholipid molecules consist of a hydrophilic phosphate head and two hydrophobic fatty acid tails. These features enable liposomes to be able to transport hydrophobic and hydrophilic compounds effectively. Due to low absorption and bioavailability rates of traditional oral dietary capsules, the encapsulation of hydrophilic and hydrophobic nutrients within liposomes allows the active ingredient to bypass the destructive elements of the gastric system.

Liposomes release drug molecules by membrane fusion. To release the protected molecules to a site of action, the lipid bilayer fuses with other bilayers such as the cell membrane, delivering the liposome contents directly into the cells and tissues intact.

Read more about the power of Liposomes

SUBLINGUAL

Wikipedia: “When a chemical comes in contact with the mucous membrane beneath the tongue, it is absorbed. Because the connective tissue beneath the epithelium contains a profusion of capillaries, the substance then diffuses into them and enters the venous circulation. In contrast, substances absorbed in the stomach and intestines are subject to first-pass metabolism in the liver before entering the general circulation and typically have very poor bioavailability.” 

The phospholipids in liposomes utilize the sublingual pathway to bring their payload directly into systemic circulation.

However, the quantity of liposomes delivered in liquid or spray is extremely limited and larger dosages are required, resulting in more of the product being swallowed.

The highly permeable sublingual entry site can be utilized for longer duration when administered in the form of our proprietary bioadhesive gel.

Read more about the power of Sublingual delivery.

GEL

With a 0.1-0.7 mm thick mucus layer, the oral cavity is an effective route of administration for mucoadhesive dosages.

Our mucoadhesive gel is designed to adhere to biological tissues, prolong residence time and maintain an optimal release rate. LSG™ is designed to assure prolonged retention time by dynamically increasing the viscosity of the gel after application.

Controlled Release Kinetics™ within the hydrogel technology provide further advanced bioavailability and efficacy.

Bioadhesive Hydrogel – Innovative Liposomal Suspension

Our LSG™ technology provides controlled-release performance with liposomes suspended in a natural bioadhesive gel. The loaded hydrogel increases contact time to improve performance over liquid products where production of saliva induces swallowing rather than sublingual absorption.

The mucoadhesive gel in our LSG products is designed to avoid rapid clearance of nutrient nanoparticles and maintain a long-term concentration gradient at the mucosal surface to ensure the unidirectional diffusion, and provides unsurpassed bioavailability with higher systemic delivery of nutrients to systemic circulation.

Read more about our Gel technology

LSG Products

See all our Liposomal Products

Research on Liposomes

 

Research on Lipsomes for increased bioavailability

Liposomes protect products from digestion in the GI tract, but that is only the first step. The improved bioavailability varies greatly, depending on the molecule itself and the quality of the liposome. Water solubility. Molecules with very poor water solubility usually have the worst bioavailability and can benefit the most from liposomal delivery. Fisetin is one example shown below up to 27x more bioavailable. Liposome Stability. Liposomes need modification to increase stability so they do not break apart and release their payload when exposed to the GI tract and bloodstream. Recent advances in Liposomal technology enables skilled manufacturers to adjust the stability so the payload is protected for several hours. Different manufacturing techniques result in significant variation in stability and bioavailability. Liposome size. As noted above, size of the liposome is crucial. Larger Lipsomes are quickly filtered out by the liver and other parts of the RES. Smaller liposomes (below 50 nanometers) can circulate much longer. The study on B-12 below shows the larger size liposome formula increased bioavailability of 3xvs 5x for the smaller sized liposomal formula.

Liposomal Fisetin 1.6 to 27x more bioavailable

This study in mice found a 2.7-fold increase (in Cmax) with Liposomal Fisetin, with a dose 10 times lower than that of the free fisetin when given by IP.   With IV, the Cmax of liposomal fisetin was 10, vs 6 for free fisetin.  

Liposomal Vitamin B-12 formulas 3-5x more bioavailable than tablet.

Route and Type of Formulation Administered Influences the Absorption and Disposition of Vitamin B12 Levels in Serum This study compared five formulations for bioavailabilty in humans over 6 hours.A standard table (iii) was compared against an emulsion (ii), a chewabletablet (iv), an oral spray comprised of larger liposomes (v) and an oral spray comprised of very small (20 nanometer) liposomes.
(i)Nanocelle 1000ug -28% – A nano liposomal formulation of B12sublingual spray with an average particle size of about 20 nm
(ii) Emulsion 1000ug – 10% -An emulsion formulation of B12 sublingual (iii) Tablet 1000ug – 5% – A standard tablet formulation of B12 that is absorbed through the gastrointestinal tract. (iv) Chewable 5000ug – 27% – A dissolvabletablet of B12 that is absorbed through the sublingual mucosa (v) Liposome1000ug – 14% – A liposome oral spray of B12 with particle sizes of approximately 100 nm. The chewable showed similar increase as nano liposomal, but a 5x higher dosage was used. The standard liposomal product was 3x more bioavailable than tablet. The nano liposomal spray exhibitedsustained release with more than 5x increased bioavailability over standard tablets. Read more

Liposomal Berberine increases circulation time 23-46x

Preparation, Pharmacokinetics and Tumour-Suppressive Activity of Berberine Liposomes (Zheng, 2017) Administration of standard Liposomal Berberine  increased retention time in circulation from .42 to 10 hours. Use of PEG modified Liposomes further increased retention to to 14 hours. Administration of Berberine solution injection is hindered by unsatisfactory pharmacokinetics and, more importantly, the risk of lethal cardiovascular adverse reactions due to rapid uptake into heart and lung. This study validated common and long-circulating liposomes as safe and effective method for sustained release of Berberine. Read more

Liposomal Curcumin & Resveratrol capsules 10-20x more bioavailable in circulation and prostate tissue vs standard capsules

Liposome encapsulation of curcumin and resveratrol in combination reducesprostate cancer incidence in PTEN knockout mice Liposome capsules of resveratrol and curcumin may inhibit prostate cancer by increasing their bioavailability synergistically and enhance the anticancer effects. In this study, we determined the bioavailability of liposome encapsulated curcumin and resveratrol, individually and in combination and evaluated the inhibitory effects of these agents against prostate cancer growth and progression. Serum and prostate tissue samples harvested at different time points of 30 min to12 hr with plain liposome (0.1%), curcumin (50 mg/kg/bw), lipo-curcumin (50 mg/kg/bw),lipo-resveratrol (50 mg/kg/bw) and lipo-curcumin co administered with lipo-resveratrol (25 mg/kg/bw for each) figure a – Levels of curcumin and resveratrol recorded in the serum figure b – Levels of curcumin and resveratrol recorded in the prostate figure d – Quantification of tumor growth inhibition. Total number of adenocarcinomas observed under 10 high-power fields of control vs. treatment groups. Read more

Liposomal Transdermal

Harnessing the unique power of Liposomes to penetrate the epidermis and protect fragile molecules to carry them into systemic circulation.

Read more about our Transdermal Liposome products