Breakthrough Liposomal Technology Uses Nanoscale Science to Nourish Cells
We live in a time of extraordinary food abundance—just walk into any supermarket and you’ll find a veritable Garden of Eden, with fresh fruits, greens, and vegetables from around the globe, as well as freshly baked whole-grain bread, wild-caught fish, and a panoply of yogurts crafted from dairy or nut milks. We also luxuriate in the cheapest food available in history–in the 1930s, Americans spent a quarter of our disposable income on food while today we spend under a tenth. And our choice of healthy foods has expanded—there has been a 27% increase in consumption of fresh fruit and a 21% increase in consumption of fresh vegetables from 1970 to 2010. We’re eating more broccoli, cauliflower, tomatoes, onions, apples, bananas, and grapes.
Yet in spite of all this bounty, we are often nutrient-deficient— over 40 percent of adults have dietary intakes of vitamin A, C, D and E, calcium and magnesium below the average requirement for their age and gender. And these statistics do not even take into account the important antioxidants that keep us healthy, such as glutathione, Coenzyme Q10, and resveratrol.
Are standard, oral multivitamin supplements the answer? Nearly two out of three adults in America think so since they take vitamin, mineral or herbal supplements. But the typical oral supplement may not deliver its full therapeutic potential. Enzymes in the stomach and gastrointestinal tract can degrade oral supplements. On their own, potent antioxidants may not be able to efficiently cross cell membranes. For instance, numerous flavonoids that show potent antioxidant activity in vitro in the laboratory, achieve only very low concentrations in the blood after oral consumption. One of the most storied antioxidants, resveratrol, associated with a longer lifespan, lower risk of heart disease, and lower levels of inflammation, is poorly absorbed in oral supplement form. CoQ10 supplementation can be challenging: as a lipid-loving (lipophilic) molecule, CoQ10 is best digested with fats and suffers poor absorption in water.
According to William Judy, founder of SIBR Research, less than 1 percent of simple CoQ10 powder is absorbed. Similarly, typical oral delivery of glutathione, the most potent intracellular antioxidant our bodies make, is greatly inhibited by its breakdown in the stomach. In one study of 40 healthy adults, supplementation with oral glutathione had no effect on blood levels of the antioxidant, and no significant changes were observed in biomarkers of oxidative stress.
In order to offer health benefits, vitamins and minerals need to reach the target tissue of action. Bioavailability is key for supplements and functional foods and related health claims. Many factors affect bioavailability—including digestive problems, low stomach acid, and low uptake of a nutrient. In addition, supplements themselves vary in the amounts of vitamins, minerals, and antioxidants they offer—some offer more than the recommended daily amount, some less. Products are sold in many different forms (powders, liquids, tablets, capsules, chewables, and gummy candies), all of which result in variable amounts. According to one study: “Many ingredients in adult MVMs had mean percentage differences that were above label claims and were highly variable between individual products in a representative sampling of the US market.”
Enter Liposomal Delivery Systems: Taking a Cue From Nature
The starburst of complex life we see all around us every day began with single cells 3.8 billion years ago—simple, free-floating bacteria that were one of life’s earliest and most ingenious inventions.
Those simple cells, just like our cells today, possessed a membrane composed of a lipid bilayer. The membrane performed all kinds of extraordinary feats: not only did it protect the inside of the cell, but it also allowed nutrients to pass through and wastes and toxins to be expelled. And it evolved the capacity to carry electricity and to store energy as ATP molecules. Mostly composed of phospholipids, the cell membrane was not only protective, but it was also highly active.
Fast forward to the 1960’s, when smart scientists began to experiment with liposomal delivery of medications. Liposomes are tiny phospholipid bubbles with a bilayer structure very similar to that of our cell membranes. Liposomes turn out to be ideal carriers for therapeutic molecules, highly effective at delivering nutrients directly into the cell. Liposomes are highly biocompatible, and they are capable of holding either water-soluble or fat-soluble molecules. Their size, electrical charge, and surfaces can be tweaked in a lab. Liposomal delivery systems have been used successfully in clinical trials for an astonishing variety of therapeutics—delivering everything from anticancer to antifungal, anti-inflammatory, and antibiotic medications as well as sophisticated gene medicines and vaccines.
Liposomal supplements offer a nutritional delivery system with rapid uptake and effective delivery into the cells. Liposomes are highly efficient in terms of facilitating antioxidant delivery, and because they are prepared from natural phospholipids, they are biocompatible and nontoxic. Liposomal delivery systems are becoming increasingly popular for nutraceuticals because they protect these therapeutic molecules from a breakdown in the digestive system. In cell culture studies, liposomes can increase intracellular delivery 100-fold over non-liposomal delivery.
Liposomal nutraceuticals and health supplements offer many benefits over typical oral formulations. These include:
- High bioavailability and absorption
- Protecting nutrients against the harsh environment of the GI tract
- Increasing oral uptake in the mouth via the mucosa
- Increased uptake into cells
- Liposomes can be formulated to hold both water-soluble and fat
- The liquid format of liposomes may be more compatible for those who have trouble swallowing large tablets
Size Matters—And Small is Better
Not all liposomes are alike. Smaller liposomes are far likelier to persist and deliver their therapeutic molecules. These smaller liposomes offer the most rapid uptake and are less easily scavenged and cleared by our immune systems. Liposomal delivery systems usually fall into three categories:
- MLV (Multi-Lamellar Vesicles) are about 500-5000nm (nanomolars) and have more than one bilayer.
- LUV (Large Unilamellar Vesicles) are ~200-800nm with a single bilayer.
- SUV (Small Unilamellar Vesicles) range from 20-150nm and have a long circulation half-life and better cellular delivery than larger particles.
The ultra-small, unilamellar liposomes are created with sophisticated high-shear equipment. The result is tightly controlled, tiny vesicles that are actually the size of nanoparticles. The smallest, unilamellar (one layer) liposomes circulate in the blood the longest and are most stable. Cellular uptake is markedly increased—as much as nine times–as liposome size decreases from 236nm down to 97nm. At the smallest size (64 nm), uptake is 34 times higher.
Lipid nanoparticle delivery systems have been shown to dramatically improve absorption of many natural substances such as DIM (Diindolylmethane) and milk thistle, which are known to have poor bioavailability on their own. Nanoparticle liposomes are ideal for the delivery of numerous molecules, especially when longer-term effects are desirable.
A Closer Look at Liposomal Supplements
Glutathione benefits dramatically from liposomal formulations. Liposomal glutathione can restore immune system responses. Liposomal technology is also superbly suited to a water-soluble antioxidant like Vitamin C, increasing blood levels over standard oral supplements.Coenzyme Q10, the body’s most potent lipid-soluble antioxidant, also benefits from the liposomal formulation. High-quality complex mixtures of pure compounds and botanicals compounded into liposomal formulations offer superb efficacy and ease of use.
With sophisticated, well-designed, lipid nanoparticle delivery systems, the bioavailability, absorption, and cellular uptake of many natural substances can be dramatically enhanced. And as a side benefit, phosphatidylcholine, which composes the membrane of high-quality lipid nanoparticles, also nourishes the lipid membranes of cells, providing phospholipids that can be used for cellular repair.
 Gambini J, . Inglés M, Olaso G et al. Properties of Resveratrol: In Vitro and In Vivo Studies about Metabolism, Bioavailability, and Biological Effects in Animal Models and Humans Oxid Med Cell Longev. 2015; 2015: 837042