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The PhytoSolve®-Technology: PhytoSolve® C, PhytoSolve® Lutein D3, PhytoSolve® Omega D3: Unleashing their Full Potential with Natural Phospholipids

Boosting the Immune System

A healthy immune system contributes to overall health. It is an efficient integrated network of cellular elements and immune modulators to prevent certain diseases. Several natural nutrients are well known for supporting the immune system in various ways. These so-called immunostimulants comprise e.g. Vitamin C, Vitamin D3, and carotenoids like Lutein. They can be used as part of integrative, complementary, and preventive measures. Unfortunately, many of the immunostimulants do not have optimal properties to get absorbed effectively after oral intake. This can be greatly improved by using certain delivery technologies and excipients.

Natural Phospholipids

Key excipients to achieve this goal are natural phospholipids. Phospholipids are amphiphilic molecules and appear as part of the membrane of every living cell. Non-GMO plant-derived phospholipids are suitable to generate lipid globules like emulsion droplets and liposomes. Lipophilic nutrients are solubilized and/or emulsified, whereas hydrophilic nutrients can be encapsulated in the lipid globules. In addition, phospholipids act as a source of essential fatty acids and may protect the stomach from acidic substances. PhytoSolve® from Lipoid is a unique and natural technology to formulate lipophilic as well as hydrophilic nutrients.

PhytoSolve® C, PhytoSolve® Lutein D3, PhytoSolve® Omega D3:

These types of natural products are self-preserving and therefore free of preservatives, can be mixed with other dietetic products, and exhibit an excellent shelf life. They show a very pleasant taste and a smooth mouthfeel.

PHOSAL® H 50: Liquid Phospholipids Derived from Sunflower

The Natural All-Rounder

Lipoid’s PHOSAL® H 50 is a liquid formulation of purified phosphatidylcholine (PC) and oil from 100 % sunflower. This unique, pure and natural liquid formulation can serve as a solubilizer for lipophilic actives and can help to disperse lipid phases into aqueous systems by forming emulsion droplets.

In addition, the natural unsaturated phospholipids show various health benefits, including improving fat digestion, and are beneficial for colon and liver health. Moreover, the PC serves as the main natural dietary source of choline.

Increased Bioavailability

Phosphatidylcholine, the major phospholipid of bile, contributes physiologically to the digestion and absorption of fats and lipophilic nutrients. 

During digestion, PC together with bile salts emulsifies these fatty components into an emulsion of small fat droplets. This leads to a larger surface area of the oil phase and therefore to a much better absorption and enhanced bioavailability of the oil and components dissolved therein.

Schematic illustration of emulsion-forming properties by PHOSAL® formulations.

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Phospholipid-Based Delivery Systems: Phospholipids as Excipients in Advanced Veterinary Drugs

Phospholipids are excellent natural excipients for veterinary applications. They are essential components of the membrane of any biological cell. They accommodate membrane proteins, creating membranes with highly selective permeability properties necessary for cell survival. Thanks to this natural versatility, phospholipids are multipurpose excipients for pharmaceutical applications in a wide range of drug products. Their unique physicochemical properties and their crucial physiological role, biocompatibility, biodegradability, and safety, predestine them for use in veterinarian products. These natural, biocompatible and non-toxic excipients extracted from, e.g., soybean or egg yolk, show excellent performance and meet the increasingly stringent regulatory requirements for veterinary products.

Phospholipids are multipurpose excipients that can contribute many functions to veterinary formulations. They are suitable for all routes of administration. Besides their technical use as a wetting agent, solubilizer, emulsifier, depot former, and liposome builder, they can also functionally improve drug products as a penetration enhancer, bioavailability enhancer, moisturizer, and texturizer.

Furthermore, they are physiologically occurring components and therefore irrelevant for residue testing in milk and meat. Phospholipids are odorless or have a characteristic, slightly nutlike odor and a bland taste while synthetic emulsifiers mostly have a bitter taste. They are even able to suppress bitter taste without affecting other taste qualities and therefore perfectly suitable for taste-sensitive animals like cats. When administered by injection, phospholipids are known to have an excellent safety profile, without any risk of inducing allergic reactions or anaphylactic shocks, unlike other, potentially harmful, synthetic detergents.

PhytoSolve® C: Immune Health Booster that Unleashes Vitamin C’s Full Potential with Natural Phospholipids

Boosting the Immune System

A healthy immune system contributes to overall health. It is an efficient integrated network of cellular elements and immune modulators to prevent certain diseases. Several natural micronutrients, especially Vitamin C, are used for supporting the immune system. However, to unfold its full potential, to get high oral dosing and optimal absorption, Vitamin C needs the aid of functional formulations and excipients.

Purified and Plant-Derived Phospholipids

Key excipients to achieve optimal absorption are phospholipids. Phospholipids, from non-GMO soybean, can be used to generate tiny lecithin globules like emulsions and liposomes.PhytoSolve® is a proprietary and natural technology of Lipoid GmbH, with globules containing phospholipids as the main component. Micronutrients can be mixed with and/or encapsulated within these globules. In addition, phospholipids act as a source of essential fatty acids and may protect the stomach from acidic substances like Vitamin C.

PhytoSolve® C:

PhytoSolve® C is a natural product and contains a high concentration of Vitamin C. It is self-preserving and can be applied in various dosage forms, e.g. as sticks, sachets, shots, dispensing devices, or beverages.

PhytoPoor®: Soybean Oil & Olive Oil with Lowered Phytosterol Content for Parenteral Applications

Refined Oils with Reduced Phytosterol Content for Parenteral Application

Lipid emulsions, with a high content of essential polyunsaturated fatty acids, are used as a source for energy and nutrients in parenteral nutrition. Especially the polyunsaturated fatty acids linoleic acid (LA) and α-linoleic acid (ALA) are important as a source of calories and to prevent essential fatty acid deficiency.

Soybean oil has a high content of both fatty acids, whereas olive oil is a source for LA and oleic acid. Therefore lipid emulsions based on soybean oil or mixtures of soybean and olive oil are commonly used in parenteral nutrition.

A possible complication of long-term parenteral nutrition is the occurrence of parenteral nutrition-associated liver disease (PNALD ), affecting 15 – 40 % of adults and 30 – 60 % of children. There are indications that PNALD is related to parenteral uptake of phytosterols (PS). PS are natural minor components of vegetable-derived oils and parts of dietary intake. The absorption of dietary PS by the oral route is very limited (5 – 10 %) and the concentration in the blood is thereby low. This protective barrier is not given during parenteral administration while the ability of the human body to metabolize PS is limited. Elevated serum concentrations of PS, especially Stigmasterol, are associated with the deregulation of bile salt metabolism and liver injury. 

The PS content of common soybean oil is 2500 – 4000 ppm and of olive oil 1000 – 1800 ppm, respectively. With PhytoPoor® Lipoid is offering PS reduced soybean and olive oils for parenteral application.

As assessed by a rapid GC method, the refined soybean oil contains n.m.t. 600 ppm phytosterol and the refined olive oil contains n.m.t. 300 ppm PS.
The stigmasterol content, considered as the most critical PS, is more than 10-times reduced in these oils with only β-sitosterol as the major remaining PS.

 

Tab. 1: Comparison of the calculated typical phytosterol content of the oil phase of parenteral nutrition emulsion products made with standard oil grade or oil with reduced phytosterol content

Liposomes and Emulsions: Innovative Encapsulation Systems for Bioavailability Enhancement

Phospholipids from Lipoid are the ideal natural choice for the development of innovative products with numerous advantages.

Firstly, they can naturally improve the delivery and bioavailability of nutrients. An example of the enhancement of bioavailability by liposomal formulations is vitamin C. The superior delivery of liposomal encapsulated vitamin C could be shown in a study, where the oral delivery of the vitamin, (encapsulated with phospholipids), resulted in higher circulating levels – compared to pure vitamin C.

Secondly, formulations with phospholipids protect labile compounds from premature degradation in the gastrointestinal tract and therefore help to maintain the health benefits of sensitive ingredients. In pharmaceutical applications, the combination of nonsteroidal anti-inflammatory drugs with phospholipids helps to attenuate side effects related to gastrointestinal irritation. Likewise, formulations with phospholipids contribute to the maintenance of the gastrointestinal mucosa.

Thirdly, the major phospholipid phosphatidylcholine (naturally present in cell membranes of humans, animals, and plants) is also the natural source of the vitamin-like nutrient choline. Therefore, liposomal formulations with phospholipids provide the human body with choline and essential fatty acids, providing several additional benefits.

Depiction of phospholipids in an aqueous environment, an emulsion (phospholipid monolayer encapsulation of lipophilic ingredients), and a liposome (phospholipid bilayer encapsulation of hydrophilic ingredients).

Formulations with Phospholipids – Diverse Possibilities, Numerous Advantages

PHOSAL® Curcumin: The Superior Formulation for Bioavailable Curcumin

PHOSAL® Curcumin – The Natural Bioavailable Choice

PHOSAL® Curcumin is a liquid formulation of curcumin extract, purified phosphatidylcholine (PC) from sunflower lecithin, and plant oil. Curcuminoids are almost insoluble in water. Phosphatidylcholine with its combination of hydrophilic and lipophilic properties can disperse fat-soluble nutrients in an aqueous environment. PC is an important part of the micelles naturally formed during digestion and enhances the uptake of curcuminoids in the intestine.

Moreover, the formation of micelles protects sensitive components from degradation in the gastrointestinal tract [2], so that the curcuminoids can exert their full potential. The improvement of bioavailability of curcuminoids by formulation with natural phosphatidylcholine from sunflower and without any chemical additives was verified in an in vitro study.

PHOSAL® Curcumin contains about 7 % curcuminoids and approximately 50 % sunflower phosphatidylcholine. Phosphatidylcholine is the natural form of the vitamin-like substance choline that is related to different health claims by the EFSA.

Curcuminoids and Phosphatidylcholine – The Synergistic Combination

Curcuminoids and phosphatidylcholine (Fig. 2) have many health benefits. The combination of both sub-stances could lead to synergistic effects, for example against inflammatory, liver, or heart diseases.

Glycerophosphocholine (GPC): The PRO-Phospholipid with Natural Power to Reinforce Mind and Body

Glycerophosphocholine (GPC) also known as Alpha-Glycerophosphocholine is a substance derived from lecithin of vegetable sources.

We call it a “PRO” phospholipid because it is not a phospholipid, but a phospholipid-derived substance due to its lack of lipophilic fatty acids. It is a multifunctional nutrient present in all mammalian cells.

After oral consumption, LIPOID GPC-PRO is rapidly absorbed because of its high hydrophilicity. It is an acetylcholine (ACh) precursor,  which has a promising potential for the treatment of cholinergic dysfunctions.

LIPOID GPC-PRO passes easily through the blood-brain barrier providing a source of choline for ACh and phosphatidylcholine biosynthesis. The optimal phospholipid and acetylcholine levels promote cognitive, mental, and cerebrovascular health. Furthermore, a balanced GPC along with ACh concentration promotes physiological processes and body power.

ACh is involved in muscle contraction, as it is the major neurotransmitter regulating the physiological response to exercise. It can be assumed that since all muscle movements are related to contraction, and contraction is related to available cellular ACh concentration, maximizing ACh levels should optimize muscular performances. In comparison to other common cholinergic precursors, LIPOID GPC-PRO raises blood and brain choline levels safely and more efficiently. Cytidine 5-diphosphocholine or citicoline is one different choline source. However, the higher hydrophilicity and deviating roles in physiological pathways make the application of LIPOID GPC-PRO more favorable and effective. Numerous research studies explain the multifunctional benefits of GPC and suggest that oral supplementation plays a significant role in enhancing neurological function, physical performance, and memory.

Die Verwendung natürlicher Phospholipide als pharmazeutische Hilfsstoffe

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In pharmazeutischen Formulierungen werden aus pflanzlichen oder tierischen Quellen gewonnene Phospholipide und synthetische Phospholipide als Hilfsstoffe verwendet. Natürliche Phospholipide werden z.B. aus Sojabohnen oder Eigelb mit Hilfe von Extraktionsverfahren mit nicht toxischen Lösungsmitteln- und Chromatographieverfahren mit geringem Energieverbrauch und möglichst wenig Abfall gewonnen. Aufgrund der Verwendung validierter Fraktionierungsverfahren und der Beschaffung von Rohstoffen mit gleichbleibender Qualität weisen die resultierenden Produkte mit unterschiedlichen Phosphatidylcholingehalten eine ausgezeichnete Reproduzierbarkeit von Charge zu Charge hinsichtlich der Phospholipid- und Fettsäurezusammensetzung auf. haben. Die natürlichen Phospholipide sind in Arzneibüchern und relevanten Richtlinien der Zulassungsbehörden beschrieben. Synthetische Phospholipide werden vorzugsweise aus Glycerophosphocholin (GPC) natürlichen Ursprungs hergestellt. Synthetische Phospholipide spielen im Vergleich zu natürlichen Phospholipiden in der pharmazeutischen Technologie eine untergeordnete Rolle. Natürliche Phospholipide werden gegenüber synthetischen bevorzugt, da sie aus erneuerbaren Quellen stammen und mit nachhaltigen umweltfreundlichen Verfahren hergestellt werden. Im Vergleich zu synthetischen Phospholipiden sind die natürlichen Phospholipide in größerem Maßstab und zu relativ niedrigen Kosten verfügbar.