Liposomes are a revolutionary way of encapsulating active ingredients to protect and deliver them directly to the cells of our tissues, which are reached via the bloodstream. 1
Liposomes stabilize therapeutic compounds—overcoming obstacles to cellular and tissue uptake—and improve the biodistribution of compounds to target sites.
Solves the Bioavailibility Problem
The aim of taking any supplement is to ensure its transport into the bloodstream via the mucosal and intestinal epithelial cells.
However, due to low absorption and bioavailability rates of traditional oral dietary capsules, active ingredients lose most of their potency while passing through the gastrointestinal tract or are simply not absorbed in the small intestine at all. The majority is excreted unused via the intestines or kidneys. 2
Liposomes are vesicles comprised of phospholipids—the primary building blocks of cell membranes. Because they are made of the same material our cell membranes are made of, as they bond to these membranes, they facilitate the delivery of nutrients that are difficult for your body to absorb.
Liposomal delivery offers a targeted and complete absorption of active ingredients with a delayed‑release effect, unlike all other nutrient delivery methods. This increased circulation time of key nutrients in the bloodstream significantly bioavailability. The higher the bioavailability of an active substance, the more effect it has on the body. 3
Liposomes are absorbed through the oral mucosal lining and through lymphatic mechanisms in the gut, bypassing first pass metabolism and breakdown in the liver ensuring the retention of liposome integrity. A synthesis takes place which allows vitamins, minerals or micronutrients to be transported more easily. This higher absorption, means greater efficacy and with smaller doses needed to achieve better results. 4
Phospholipids, which are found throughout the body in the membranes of body cells, are so naturally-occurring, that the body recognizes these as body-compatible and does not treat them as ‘toxic’ or ‘foreign’—and, so, does not mount an immune attack on the liposome. 5
Liposomes shield nutrients from detection by the body’s immune system, mimicking biological membranes and giving the active ingredients more time to reach their intended destination.
Phospholipids mask the active ingredients so that larger amounts can be absorbed and escape the selective function of the small intestine. Osmotic (hydrophilic) side effects of some high-dose vitamins and minerals can thus be reduced. 6
Crosses the Blood Brain Barrier
Liposomes have demonstrated the ability to cross this barrier, giving the liposomes the ability to deposit the supplement directly into the cells and enhance circulation of nutrients by your lymphatic system. 7
This profound effect of liposome size on complement recognition can also affect liver uptake. Generally, large unmodified liposomes are eliminated more rapidly than small liposomes, which is why our Fluidizing Liposomes™ are very small—less than 100 nm to prevent their uptake by macrophages of the liver and the spleen. 8
What are Liposomes made of?
The word liposome comes from the Greek words ‘lipo’ for fat and ‘soma’ for body. Liposomes are spherical ‘sacs’ consisting of a double ring of fatty-acid molecules—phosphatidylcholine molecules (phospholipid attached to a choline particle).
The liposomal spherical ‘sac’ can be used to enclose and deliver contents of the ‘sac’ directly into the cells and body tissues.
The phospholipid molecule consists of a hydrophilic phosphate head and two hydrophobic fatty acid tails. This enables liposomes to be carriers of both hydrophobic and hydrophilic compounds. Liposomes are lipid vesicles made of phospholipids strung together, which form a double membrane, just like almost all cell membranes of our body.
The encapsulation of hydrophilic or hydrophobic nutrients within liposomes, such as NMN, allows the active ingredient to bypass the destructive elements of the gastric system. improved its oral bioavailability and increase peak plasma concentration. 9
What does phosphatidylcholine do?
Phosphatidylcholine is required for many vital functions in the cardiovascular, reproductive, immune, and nervous systems. PC and its components are needed for the synthesis of important messenger molecules called prostaglandins which, among other functions, regulate the contraction and relaxation of muscles. Choline is required for the synthesis of intracellular messenger molecules including the neurotransmitters that allow nerve cells to communicate with muscles and each other, and are essential for proper heart and brain function.
At birth up to 90% of cellular membranes are made up of PC. As you age, the percentage of PC in your cellular membranes can decrease to about 10%. This fact leads many to recommend consistent supplementation with this essential phospholipid. 10
How do Liposomes work?
Liposomes release bioactive nutrients by membrane fusion. They delay the clearance and increase the intravascular circulation time of encapsulated nutrients and prolonging retention time.
At the first stage of liposome-cell interaction, liposomes adhere to the cell surface. Following such binding, the liposome is internalized into the cell by the mechanism of endocytosis (or phagocytosis). This is followed by the enzymatic digestion of the liposome in the intracellular compartment, accompanied by the intracellular distribution.
The active nutrient encapsulated in the liposome is protected from metabolism and the molecule becomes active only after release from liposome.
These encapsulating phospholipids bond with cell membranes to facilitate intracellular delivery. They are successful in this because they are able to bypass the digestive processes that normally degrade foreign substances.
Liposomes ensure safe delivery of encapsulated cargo retain it in tissues and cells.
Key Advantages of Liposomal Delivery:
- Protects against the harsh environment of the GI tract and increases transmucosal (oral) uptake and absorption.
- Optimizes both hydrophilic and hydrophobic, unstable compounds.
- Timing of the dose does not require accompaniment or exclusion of food as the absorption via the liposome avoids the digestive processes.
- Provides a larger nutrient payload per particle.
- Offers higher bioavailability and absorption compared to conventional capsules.
- Increases increase peak plasma concentration.
Research on Lipsomes for increased bioavailabilityLiposomes 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 bioavailableThis 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.
- (i)Nanocelle 1000ug -28% - A nano liposomal formulation of B12sublingual spray with an average particle size of about 20 nm