What are liposomes and what does liposomal mean?
For some time now there has been a rethinking in the health world. Functional substances from nature and knowledge from traditional medicine can nowadays, by new findings in biochemistry, be confirmed as effective in many cases. The great potential of natural active ingredients becomes visible through intensive research. How can these minerals, vitamins or plant substances be effectively absorbed and consumed by the body?
The answer: through liposomes!
1. What are Liposomes?
The term liposome is derived from the Greek words "lipos" for fat and "soma" for body. The word stem also describes very well the properties of liposomes to represent a small body (vesicle).
Liposomes are lipid vesicles made of phospholipids (in our case derived from sunflowers) strung together, which form a double membrane. This double membrane can also be found in almost all biomembranes (for example the cell membranes of our body). Both in their aqueous interior and within their fat-soluble double membrane, liposomes can transport such different substances regardless of their charge, size or structure, while being protected from the body's own digestive enzymes and to some extent even from gastric acid.
The phospholipids, which are the main building blocks of liposomes, are mostly of plant origin, e.g. from sunflowers. Theoretically, liposomes can also fuse with cell membranes as the structure from a phospholipid double membrane is identical to those of our main building blocks. This fact makes the absorption of the phospholipid membranes and their uptake in the body a priority. Due to this deception, liposomes easily reach their destination via the digestive tract. We call them our “trojan horse” of drug delivery.
In conclusion, liposomes have three basic abilities:
Protection of the active ingredients: The rough environment of the stomach can damage some active ingredients. Encapsulation in liposomes protects the active ingredients in the digestive system.
Masking: 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.
Absorption: Liposomes are preferentially absorbed at the intestinal wall, as they consist of phospholipids just like our cell membranes. Through normal fat absorption, the active ingredients then enter the enterocytes (intestinal cells) directly, and from there into the blood via the lymphatic system. The route via the liver can thus be avoided, which ensures that direct discharge or inactivation is prevented .
2. What does liposomal mean?
The revolution in liposomal formulations is based on a natural phenomenon. Phospholipids trap liquids in a lipid bubble under certain conditions. Whether these fluids contain vitamins, minerals or micronutrients is irrelevant for the liposome. Essential substances in aqueous solutions are thus automatically enclosed by the liposomes during the formation phase. A foodstuff enriched with liposomes is therefore "liposomal" if the primary active substance contained in the foodstuff is enclosed in liposomes. Thus, a synthesis takes place which allows vitamins, minerals or micronutrients to be transported more easily. This is because the aim of taking any active ingredient is to ensure its transport into the bloodstream via the mucosal and intestinal epithelial cells.
Due to their amphiphilic structure (water-soluble and fat-soluble) liposomes can easily reach this goal and transport the active ingredient. This results in an almost complete drug delivery. Through this optimized absorption, the bioavailability can be significantly increased, which maximizes the effect of the active ingredient. This makes sense, for example, if high-dose or difficult to absorb active agents like curcumin, magnesium or vitamin C are taken. In fact, more than 75% of all active ingredients are affected by an impairment of bioavailability when applied orally, sometimes so drastically that only a few percent can be transported into the bloodstream. So, if a vitamin, mineral, plant substance or endogenous substance bears the attribute "liposomal", it simply means that the liposomal encapsulation technique (or liposomal formulation) has been used. The active ingredient is thus protected in a double membrane of phospholipids and is transported directly into the bloodstream, to the most efficient site of action.
3. Why take liposomal products?
The problem of conventional food supplements (NEM) is found in their nature. The target of every drug delivery are the cells of our tissues, which are reached via the bloodstream. In theory, intravenously administered dietary supplements provide the fastest transport to the site of action, but they are usually avoided due to their complicated administration. In practice, rejection is often outweighed by fears of the treated persons, but a higher risk of infection through the cannulas can also be a danger. Orally administered NEMs are omnipresent, they are the first and so far often the only choice when it comes to the supply of vital substances.
However, the main problem remains inefficiency, which has damaged the reputation of dietary supplements over a long period of time. Theoretical effects based on in-vitro studies often contrast with practical ineffectiveness in vivo. Some sensitive active ingredients lose much of their effects while passing through the gastrointestinal tract or are simply not absorbed in the small intestine. If molecular agglomerations are too large, have too little water solubility to be absorbed or are too hydrophobic to be dissolved, they can only marginally pass the intestinal wall and do not fulfil their function. The majority is excreted unused via the intestine or kidney.
Researchers discovered that liposomal formulations can be used to protect and transport therapeutic substances such as drugs, but also nutrients and vital substances. Already used for decades in the pharmaceutical industry under the keyword "drug targeting", liposomes are used for a more targeted and complete absorption of active ingredients. Studies from medicine and nutritional science confirm that liposomes increase bioavailability up to 30 times. This is the rate with which the active substance enters our bloodstream. From an economic point of view, this bioavailability can be compared with a price-performance ratio. The higher the bioavailability of an active substance, the more effect it has on the body. However, even more important than the superior price-performance ratio could be the fact that many substances can only be transported into the bloodstream to a significant extent in the first place. With the classic pill, certain quantities have never been achievable here.
4. Examples of liposomal formulations
In summary, liposomal supplements are highly bioavailable, efficient, functional foods that are conveniently taken orally and are well suited for everyday use. Finally, the full potential of natural active ingredients can be used!
5. How do we make liposomal products?
With ActiNovo we now offer the innovative transport system "Liposome" for the use of dietary supplements.
Take vitamin C as an example:
Trapped and protected in liposomes, the vitamin can get directly to and into the bloodstream and begin its work as an antioxidant.
Liposomal Vitamin C
Vitamin C is a water-soluble vital substance that plays a supporting role in collagen synthesis, energy metabolism and the immune system. As an antioxidant it fights cellular stress. The daily requirement of this vital vitamin must therefore be met. Often one also considers the benefit or danger of a substance in case of overdose, i.e. a dosage that is higher than the dosage specified by the manufacturer, legislator or authoritative institutions. Vitamin C is considered to be largely harmless even in very high concentrations .
In general, 2000 mg of vitamin C per day for adults over 19 years of age is considered safe over a long period of time . This refers to the amount of vitamin C obtained from food and dietary supplements together. However, if healthy people take an even higher amount over a longer period of time, adverse effects can occur.
Liposomes can also help here, as it is not the absorption mechanism of the vitamin C that is decisive here (active), but the absorption of the surrounding phospholipids (passive), in which the vitamin C is contained.
We would like to point out at this point that we explicitly do not advocate an overdose of any vital substance.
 Hyeongmin Kim, Yeongseok Kim, Jaehwi Lee, Liposomal formulations for enhanced lymphatic drug delivery,
Asian Journal of Pharmaceutical Sciences, Volume 8, Issue 2, 2013, Pages 96-103, ISSN 1818-0876, https://doi.org/10.1016/j.ajps.2013.07.012.
 Institute of Medicine. Food and Nutrition Board. Dietary Reference Intakes for Vitamin C, Vitamin E, Selenium, and Carotenoids. Washington, DC: National Academy Press, 2000.
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