Many nutraceuticals are labile substances, easily degraded during processing and/or storage, and during passage in the gastrointestinal tract (1). In addition, some vitamins may interact with other vitamins, mineral salts or preservatives found in complex multivitamin-mineral preparations. Most commonly, decomposition reactions occur in such mixtures, resulting in a reduction in the content of selected active ingredients (2,3,4), which can result in a discrepancy between the declared and actual content of them in the product (4).
In addition to the aforementioned factors negatively affecting the functionality and therefore the health effect of many bioactive components, poor water solubility of some of them, such as curcumin, polyphenols or vitamins A, D, E and K, is also important (1).
Available literature data indicate that an effective way to increase the stability and bioavailability of biological substances is their micro – and nanoencapsulation, especially in lipid carriers, including liposomes (1,5).
Main advantages of liposomes include their biocompatibility and safety due to the similarity of their structure to biomembranes (6). Moreover, liposomes are highly effective in entrapping active substances (7) and protecting them against degradation caused by i.a. the presence of oxygen, other food ingredients (8), incorrect pH, light or digestive enzymes (7). At the same time, encapsulation of some active substances (e.g. vitamin C or magnesium citrate) in liposomal vesicles minimizes their side effects, such as epithelial irritation, also in the gut.
Due to the above, the use of this group of carriers in the food, pharmaceutical, agricultural and biotechnology industries awakes growing interest. Unfortunately, there are a number of factors that can significantly limit the scaling-up of laboratory production of liposomes. They include: unsatisfactory size distribution of the particles obtained, poor reproducibility of the properties of successive batches of the product, chemical and physical instability of the carriers in liquid suspensions, and the presence of difficult-to-remove organic solvent residues in their composition (9).
Indeed, the use of liposomes in the form of liquid suspensions still poses many problems due to the chemical and physical destabilization of these carriers during long-term storage. Liposomal particles can aggregate, flocculate, coalesce or fuse, resulting in their precipitation. Hydrolysis and/or oxidation of phospholipids can also result in leakage of active substances from the carrier, making them more easily degraded, including in the human gastrointestinal tract (10,11). As a consequence, liquid liposomal suspensions require refrigerated storage and consumption within a few months of manufacture (11).
An effective solution to increase the stability and thus the bioactivity and bioavailability of newly produced liposomes is to dehydrate them (10,11).
In Bart, we applied the novel technological solution, including drying of the obtained liposomes, which:
- Significantly increases the storage stability of the powdered products compared to its liquid forms
- Eliminates the need to maintain refrigerated temperatures during transport and storage of Liposovit® powders
- Eliminates the need to add preservatives, making our productssafe for people with broadly defined food hypersensitivities
- Enables problem-free use of Liposovit® in powder mixtures.
Figure 1. Macroscopic images of selected Liposovit® products
Liposovit® products are in the form of fine, loose powders with homogeneous structure (Figure 1). They are distinguished through:
- good solubility in water*
- better absorption and higher bioavailability typical for liposomal formulations in comparison to traditional forms of active ingredients. Increased effectiveness of supplementation has so far been confirmed for Liposovit®-C and Liposovit®-Mg, in a clinical trial and a pilot study, respectively
- the ability to effectively protect encapsulated active substances from chemical and enzymatic degradation during storage, including in complex multivitamin-mineral mixtures, and during passage through the digestive tract
- ability to protect sensitive gastric epithelium from irritation caused by selected conventional forms of active substances, e.g. ascorbic acid or magnesium citrate
- small size of liposomal particles (≤ 300 nm), not affected by the drying process
- simple, GMO- and allergen-free composition
- full safety, biodegradability and biocompatibility.
* Liposovit®-Curcumin achieves enhanced dispersibility relative to the conventional form of turmeric extract.
The most effective liposomes are those characterized by small particle diameter and narrow particle size distribution (12). As shown in Figure 2, the drying process, which is an integral part of our innovative technology, does not affect the quality and uniform particle size distribution of the liposomes produced.
Figure 2. Liposomes particle size distribution in the powder form of the selected Liposovit® products.
At BART, we also develop granular forms of our liposomal products (Figure 3). They combine the advantages of lipid nanocarriers of active substances and the benefits of granules. Consequently, it is possible to significantly improve the effectiveness of the supplementation of active substances in fast-dissolving products and/or formulas intended for direct consumption.
Figure 3. Macroscopic images of Liposovit® DIRECT products
The uniqueness of the technology we developed directly translates into the properties of Liposovit® products, i.e.:
- their stability,
- favourable pharmacokinetic properties, successively confirmed in in vitro, pilot and/or clinical studies,
and
- the simple, allergy-friendly composition of liposomal powder forms and their wide range of applications.
They definitely stand out in the market, representing the future of the dietary supplement segment.