Lipophilic Vitamins – A, D3, E, and K2

The four lipophilic vitamins A, D, E, and K are essential nutrients involved in numerous processes in the human body.

 Figure 1: Selected examples of 14 EFSA approved health claims.

PhytoSolve® Technology

The PhytoSolve® delivery technology enhances the uptake of lipophilic nutrients in a natural way. Fat-soluble substances, like the four lipophilic vitamins A, D, E and K, require a carrier to be effectively absorbed. Due to their amphiphilic properties, phospholipids can enclose fat droplets in the form of an emulsion. The performance of the PhytoSolve® technology could be shown in an in vivo study with vitamin E.

PhytoSolve® ADEK

The unique formulation PhytoSolve® ADEK stands out from typical ADEK products owing to its excellent performance and high customer convenience. It enables a homogeneous distribution of the four lipophilic vitamins in an easy to dose but still small volume. PhytoSolve® ADEK can be mixed in any ratio with water, juice, dairy products, and many more.

Poor solubility, slow dissolution rate, gastrointestinal degradation, and low permeability are typical factors that limit oral bioavailability of drugs. In order to overcome these limitations advanced formulations with phospholipids can be used. Phospholipids are diversely used as excipients in such formulations as dispersing agents, emulsifiers, or as additional or sole matrix components for solid dispersions (Fig. 1). Liposomes dissociate in the gastrointestinal tract and release phospholipids, which provide solubilising effects.
Moreover, phospholipids are applied as technical excipients in tablet coatings or as processing aids to produce soft gel capsules.

Self-Emulsifying Systems

Self-emulsifying systems (often referred to as SEDDS) are water-free formulations that spontaneously form emulsions in aqueous media, including gastrointestinal fluids. They are used predominantly for solubilization of lipophilic drugs to increase their bioavailability. In formulations for oral ingestion, self-emulsifying systems are typically applied as oily liquid or in form of a soft gel capsule. The preconcentrate can be administered in its water-free form but may also be diluted in an appropriate beverage before administration.

Mixed Micelles

In the gastrointestinal tract, mixed micelles composed of endogenous phospholipids and bile salts solubilize lipophilic nutrients to make them available for absorption. Pharmaceutically applied mixed micellar formulations consist of soybean phosphatidylcholine and therefore offer a natural vehicle for lipophilic drugs such as Vitamin K.

Solid Dispersions

Solid dispersions are widely employed to enhance the dissolution of poorly soluble crystalline drugs by amorphization of the drug substance. Phospholipids are investigated as complementary or sole matrix material for this purpose. In addition to amorphization, phospholipids contribute to drug solubilization by enhancing wettability, forming colloidal structures upon hydration and stimulating the secretion of bile.

Concluding Remarks

Phospholipids are multifunctional excipients with versatile applications in oral formulations. Their physiological role in digestion and absorption processes underscores their biocompatibility, functionality, and safety.

Phospholipids are amphiphilic, endogenous molecules with excellent biocompatibility and tolerability. Therefore, they are an ideal choice for various “over-the-counter” (OTC) products, including formulations for sensitive tissue such as the ocular surface. Phospholipids can serve as active principle, as excipients to modulate tissue interaction, and as building blocks to form lipid particles such as emulsions and liposomes (Fig. 1).

Application in topical OTC products

Phospholipids are essential components of all mucosal surfaces. On the ocular surface, phospholipids stabilize the outer non-polar lipid layer that prevents evaporation and thereby keeps the eye mucosa moisturized. In the nasal and oral cavity, a surfactant film covers the air-mucus interface, which contains mainly saturated and unsaturated phospholipids (Fig. 2). Topical phospholipid-based products restore and moisturize mucosal surfaces in a natural way. For this purpose, phospholipids often serve as active principle but may also be combined with additional actives.

Further applications

Also, in a broad variety of other OTC formulations phospholipids are used. In dermal topicals, phospholipids can modulate intrinsic metabolism pathways, restore the skin barrier properties, or enhance skin interaction of co-formulated actives. In oral dosage forms, phospholipids function as emulsifiers and building blocks for colloidal species or serve as an active, typically in products for liver protection.

In addition, phospholipids are used as technical excipients, e.g., in suppositories. The highly versatile use as technical and functional components underscores the suitability of phospholipids for a wide variety of OTC formulations.

Fig. 1: Fatty liver disease is characterized by an increasing storage of fat in hepatocytes.

The Liver – Central Organ of Lipid Metabolism

A healthy liver is essential for a well-functioning fat metabolism.
A disturbance can lead to the accumulation of fats and result in fatty liver disease. Especially the non-alcoholic form (NAFLD) is very common in industrial countries due to the Western Style Diet and a lack of physical activity. The prevalence for NAFLD is increasing but, fortunately, the storage of fat is reversible. Therefore, choosing nutrients with hepatoprotective properties becomes more and more important.

The Importance of Phosphatidylcholine

Dietary and supplemented PC supports liver function in a natural way by regulating the fat metabolisms. In addition, polyunsaturated phospholipids (PPL) are very popular for liver protection. In several clinical studies their antioxidative and anti-inflammatory properties could be shown.

PC is also a safe and natural source of the vitamin-like substance choline. The EFSA-approved health claims illustrate the importance of the nutrient.

Lipoid offers a wide range of products enriched in polyunsaturated phosphatidylcholine. Various forms of application, like capsules or innovative liquid solutions, are possible. Due to the emulsifying properties of phospholipids the formulations are mixable with any kind of beverages. To find a suitable application for liver protecting PC just ask for our support and guidance.

PPL with high phosphatidylcholine content are the natural solution for a healthy liver.

The most important natural source of astaxanthin is the alga Haematococcus pluvialis.

Astaxanthin – Nature’s Powerful Antioxidant

Astaxanthin is a powerful antioxidant that is naturally produced by aquatic organisms like algae. In comparison to other antioxidant nutrients, it exhibits higher capacity to scavenge reactive oxygen species (ROS).

During vigorous physical exercise, ROS are associated with soreness, fatigue, and muscle damage. Intake of astaxanthin contributes to higher endurance, reduced muscle soreness and faster recovery, making it an ideal supplement for sports nutrition.

PhytoSolve® Astaxanthin

Lipophilic nutrients like astaxanthin require solubilization to be absorbed in the human body and exert their beneficial effects. In PhytoSolve®, highly purified phospholipids enclose small oil droplets, forming an emulsion. This vehicle effectively enhances the uptake of lipophilic nutrients in a natural way.

Moreover, the formulation contains glycerol and medium-chain triglycerides (MCT). Both ingredients offer additional benefits for sports nutrition. Glycerol is used for pre-exercise hyperhydration to minimize the risk of dehydration. MCT can be used as energy source due to their rapid metabolism.

PhytoSolve® Astaxanthin is a self-preserving formulation, can be mixed with any kind of beverage, and has a very pleasant taste and smooth mouthfeel.

PhytoSolve® Astaxanthin is the smart way to formulate astaxanthin.

Schematic depiction of an emulsion droplet and its components.

The Basics of Liposomes

LIPOID Liposome Basic is a high-quality pre-formulated concentrate that can be combined with your nutrients of choice. The liposomes are made up of 100 % natural phospholipids which self-organize in water as bilayer structures due to their amphiphilic properties. Liposomes can help to improve the bioavailability, the stability, and the digestibility of active ingredients.

Fig. 1: Schematic diagram of phospholipids and a liposome

Why Quality Makes the Difference

We choose only natural and well selected raw materials for our formulations by meeting the highest quality standards. LIPOID Liposome Basic is self-preserving and therefore free of preservatives and ethanol. Due to its small and uniform particle size LIPOID Liposome Basic has a transparent
appearance and a great stability. The pleasant taste makes all the difference.

Versatile Applications of Liposome Basic

LIPOID Liposome Basic can be mixed with a wide range of hydrophilic nutrients without the use of expensive technical equipment. It can be utilized pure or diluted and is compatible with many types of
applicators.