Increase in bioavailability of food supplements using liposomal formulations
Liposomes are made from extracts of lecithin which contain phospholipids, mixed with other molecules that we may wish to attach. Liposomes vary in size from low nanometer up to tens of micrometers. When combined with water, phospholipids form microscopic structures with a central void encapsulating water and within that water we can dissolve other molecules, such as Vitamin C or Glutathione which we would like to have absorbed easily into the body. Whilst hydro-philic molecules can be held within the encapsulated water, hydrophobic chemicals can be dissolved into the membrane itself and in this way liposomes have the ability to carry both hydrophobic and hydrophilic molecules. Due to their unique properties liposomes are used for the formulation of drugs, food supplements and cosmetics.
The attraction of using liposomes to deliver nutrients, supplements and drugs into the body is that they are easily absorbed by the gastro-intestinal tract and in so doing the additional encapsulated molecules are absorbed at the same time. This overcomes the barrier that faces many beneficial products of getting absorbed into the body in effective levels. The body will often break down many complex molecules before they are absorbed or will just not readily absorb them and so absorption levels are reduced. But as Liposomes are easily absorbed the products encapsulated by Liposomes achieve much higher blood dosage levels than found in non-encapsulated products such as traditional tablets.
However, Liposomes can also go further, to assist to deliver the active molecules to the cellular sites of action where the body requires a high level of the nutrient. The lipid bilayer of the liposome can fuse with other bilayers such as the cell membrane itself, thus delivering the liposome contents into the cells.
Liposome Production
The formation of liposomes requires significant levels of energy. Phospholipids are combined with water and energy is applied in a controlled process using sonification or an ultra-turrax. The lipid vesicles will then form into either single, or multiple, bi-layers separated by water molecules. This process is controlled to create particles small enough to be readily absorbed into the blood stream.
Abstract: Oral bioavailability of food supplements can be increased using liposomes as carriers of active ingredients. It solves a lot of absorption problems normally seen with supplements. Curesupport has developed different active ingredients in reliable and safe dosage forms building them in a liposomal matrix. With this technology it is possible to increase plasma levels of Vitamin C, B12, Curcumin and many other ingredients in a very safe and gentle way. These levels could never be reached with only higher amounts given in tablets. It does much more than only resulting in a higher blood level with lower amounts of active ingredients. It helps reaching plasma levels which would be impossible using only tablets or capsules.
A reliable suppletion of food supplements is dependent on the bioavailability of the active ingredients. That means that for instance in a vitamin-tablet with many ingredients, some will be absorbed as required but that many others are dependent on what happens with the material of the body. This means that for supplements it is not always a good idea to present them in the form of tablets/ capsules/ powders. Some will be absorbed, many will not. In Table I some active ingredients are given with a different Bio-availabilities.
Table 1: Different food supplements and their oral bio-availability from tablets and capsules.
| ACTIVE INGREDIENT | BIOAVAILABILITY | LITERATURE |
| Ascorbic acid | Decrease with increasing dosage (> 1 grs per day) | Levine et al; 1996 |
| Cobalamine | Extreme low | Kripke, 2006 |
| Resveratrol | Low | Walle T, 2004 |
| Curcumin | Low | Prasa. S et al; 2014 |
| Quercetrin | Unreliable | Graefe et al, 2001 |
| Coenzyme Q10 | Low | Zmitek et al, 2008 |
| Vitamin D | Good, but not always reliable | Borel P, 2015 |
| Vitamin B6 | Depends different parameters like food and salts used | Reynolds, 1988 |
| Silymarin | Low | Dixit Nitin et al; 2007 |
| Magnesium (salts) | Depends different parameters like food and salts used | Fairweather – tate et al; 1996 |
| Iron (salts) | Depends different parameters like food and salts used | Fairweather – tate et al; 1996 |
| Calcium (salts) | Depends different parameters like food and salts used | Fairweather – tate et al; 1996 |
From the data in Table 1 it is very clear that tablets and capsules are not a very reliable formulation for many food supplements. It is, just as with many medicines, very important to make a satisfying formulation for giving the required dosage to the body.
It is very remarkable that up to now so little interest has been given to formulation research with respect to food supplements. Although they are absolutely no drugs, they are normally pure chemical substances which need “help” to enter the body. A very good example is Vitamin B12 which has so poor bioavailability that it is almost impossible to get absorption with tablets.
CureSupport has focused on developing reliable food supplements in which the formulation is composed with the goal to get a controlled absorption of the active ingredients.
Liposomal systems:
We developed different liposomal formulations in CureSupport in order to increase bio-availability of products with a poor and or unreliable bioavailability. In the Wikipedia liposomes are very nicely defined as follows.
Liposomes are artificially constructed vesicles consisting of a phospholipid bilayer. First discovered in 1961 by Alec Bangham, a British scientist studying blood clotting, liposomes are now being studied for their potential in both laboratory techniques as well as medical applications. Of particular interest are their ability to cross cell membranes and to transport certain types of drugs to pre-designated locations within the human body. Liposomes are frequently synthesized by mixing and dissolving the phospholipids in organic solvent, such as chloroform or a chloroform-methanol mixture. It is shown that hydrophilic molecules such as Vitamin C have a better bioavailability orally then in tablets. Also hydrophobic molecules such as Curcumin, resveratrol or Co-enzyme Q10, have a better bioavailability orally when build into Liposomes. (Chee Ho Choi et al, 2010; Bojana et al, 2013; Hasan et al, 2014)In our research we show the increase of bio-availability of liposomal Vitamin C and liposomal Hydroxocobalamin (Vitamin B12).
Absorption within the cell:
Siekmeier et al. (2008) show in their review article how Liposomal systems might merge with cells in the intestines and enter their encapsulated product into the cell. This is a natural reaction as the biological bilayers of the cell wall are usually composed of amphiphilic phospholipids which has the same molecular structure as the phospholipids in the liposomes.
It is suggested that this is the absorption of liposomal drugs through the gastrointestinal cells. This is also seen with in vitro experiments using everted sacs and isolated perfused intestinal loop systems and has led a number of investigators to suggest that liposomal entrapment of macromolecules may facilitate their intestinal absorption by an endocytosis mechanism.
Once entered the body it is seen that because of their strong chemical and structural similarity liposomes merge with cell membranes and facilitate drug delivery into the interior of the cell. This is thought to be the main reason liposomes increase the bioavailability for active ingredients with low or unreliable absorption.
Depending on their structure liposomes have a high transport capacity and allow transport of a large number of different lipophilic and hydrophobic compounds. If liposomes come into contact with phospholipids cell membranes, the liposomal membrane fuses with the cell membrane facilitating the entry of the encapsulated drug into the interior of the cell.
Liposomal systems are able to make the bio-availability of food supplements much more reliable and higher. The bio-availability increases from 3 x up to 9 or 10 times as found with Curcumin and Vitamin B12. The levels reached will never be reached with the use of more tablets. The system of absorption from tablets and capsules differs fundamentally from that of liposomes. This makes liposomes a far more reliable and safe alternative for tablets and capsules in order to get a high and effective blood plasma level for many supplements.
At CureSupport we decided to take a profoundly different approach, very scientific based and with major stress on quality, efficiency and bioavailability of our products. Furthermore, there is a library of more than 300 scientific papers available to our partners to gain profound knowledge on every substance/product we offer!
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