Formulating High-Quality Supplements Can Be So Easy

The Basics of Liposomes

LIPOID Liposome Basic products are high-quality pre-formulated concentrates that can be combined with your nutrients of choice. Our liposomes are composed of 100 % natural phospholipids which self-organize in water as bilayer structures due to their amphiphilic properties. Liposomes can help to improve the bioavailability of nutrients and are the vehicle of choice when it comes to increased natural absorption of, e.g., vitamin C.

What is new?

In addition to the product based on non-GMO soybean phospholipids, we now launch a sunflower-based variant of our high-quality pre-formulated liposomes: LIPOID Liposome Basic H. LIPOID Liposome Basic H is the ideal solution for clean label supplements.

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.

Contact us here ^[1] for more information on our LIPOID Liposome Basic products.

What is Phosphatidylcholine?

Phosphatidylcholine is the fat-soluble form of the vitamin-like substance choline and an important phospholipid for the human body. The molecule consists of a water-soluble choline head and two fat-soluble fatty acids including polyunsaturated ones. Phosphatidylcholine exhibits antioxidative properties, can reduce inflammation and enhance cell membrane integrity.

Furthermore, positive hepatoprotective effects of these fatty acids could be demonstrated in several clinical studies.

Current Supply Situation in the Population

High phosphatidylcholine content can be found in animal-derived food such as meat, eggs, fish and milk or in breast milk. Plant-derived foods contain comparatively low amounts of phosphatidylcholine. The recommended daily intake of choline set by the FDA is 550 mg/day for men and 425 mg/day for women. Pregnant and lactating women have a further increased need for choline of 450 g/day and 550 mg/ day respectively. Nowadays, most population groups do not reach the recommended choline intake.

Choline occurs in various supplementation forms, including synthetic choline bitartrate and natural phosphatidylcholine. The natural form is widely present in animal and plant cells, as well as in breast milk. To provide this valuable form of choline, Lipoid offers high-quality phosphatidylcholine from natural sources like soybeans or sunflowers.

The benefits of natural phosphatidylcholine over artificial choline salts:

• Phosphatidylcholine can be efficiently processed by the body via natural pathways to form new cell structures
• Phosphatidylcholine has an enhanced bioavailability and faster absorption
• Due to the effective natural uptake, phosphatidylcholine does not reach the large intestine and therefore is not converted into transmethylamine-N-oxide (TMAO) by gut microbes
• In addition to choline, phosphatidylcholine provides essential unsaturated fatty acids that contribute to its health benefits

Lipoid offers a unique portfolio of high-grade phospholipids sourced from non-GMO sunflowers for nutraceutical applications. These phospholipids offer a natural and sustainable option, ensuring clean label compliance.

Rich in essential fatty acids and phosphatidylcholine, they can be used to support cognitive health, liver function, or as high-quality building blocks for liposomes and emulsions to enhance the performance of your active ingredient.

Get in contact with us to discuss which product is the best fit for your applications.

Safe and Endogenous Compounds for Pharmaceutical Applications

Phospholipids are ubiquitous, endogenous, and nutritional compounds. For pharmaceutical applications, phospholipids are safe and versatile excipients for any administration route. This is demonstrated by their long-standing use in several innovative pediatric drug products and their recognition by regulatory authorities. The excellent tolerability and safety profile of phospholipids is underscored by their presence in breast milk and infant formula, making them one of the first nutrients that infants ingest.

Excipient Selection for Pediatric Drug Products

Formulating drug products for children poses unique challenges.  Excipients are key components in the formulation of age-appropriate drug products that are suitable for the envisaged administration route, API, and target age group. In addition to functionality and quality, taste and palatability of the dosage form are typical aspects of drug formulation for children. Moreover, particular attention has to be paid to excipient safety.

As endogenous compounds with an established regulatory framework, phospholipids perfectly fulfill existing safety and quality requirements. Moreover, they provide versatile functionalities and are compatible with a wide range of age-appropriate dosage forms (Figure 1).

Figure 1: Selection of phospholipid-based formulation options and their conversion in oral dosage forms.

Concluding Remarks

Regulatory authorities require consideration of pediatric dosage forms early during the product development. The unique needs of children in terms of safety and efficacy must therefore be considered when selecting excipients. Because of their excellent safety profile, multifunctionality, and compatibility with a wide variety of dosage forms, phospholipids are ideally suited for this purpose. Moreover, they allow simultaneous development of pediatric and adult formulations, as well as conversion of adult formulations to pediatric ones without the need to exchange excipients. Various organizations have confirmed the safety of lecithin and phospholipids from a regulatory perspective including their suitability for pediatric formulations.

Lipoid provides phospholipids in cGMP quality from small to large scale to support your product development from pre-clinical to clinical and commercial stages.

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.