LIPOSOMAL TECHNOLOGY
INTRODUCTION
Are your patients reaping the full benefits from the supplements you recommend? Even people that follow supplement protocols to the letter don't always get the full dosage of essential nutrients that they need.
Liposomal delivery offers a method of getting certain nutraceuticals into the body that's more effective than regular encapsulation. Liposomes are hollow lipid vesicles that can be packed with nutrients and act a vehicle to deliver minerals and nutrients to specific parts of the body for faster absorption and less potential for irritation.
Now, let's explore how liposomal technology works.
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How Liposomal Technology Improves Your Practice
Delivering medications or nutraceuticals with liposomes offers these advantages1:
- Accelerated intestinal absorption.
- Better protection and stability than other encapsulation technologies (prevents degradation).3
- Greater bioavailability of the active ingredient.
- Can incorporate both fat- and water-soluble compounds into the liposomes. 3
- Uniformly disperse and provide controlled release of the active ingredient.3
- Protection of the gut from irritating ingredients.
- Low allergenicity and low toxicity. 2
Liposomes are hollow spheres, composed of phospholipids.1,2 Similar to an animal cell, the lipids arrange as a bilayer and surround an aqueous compartment.3
However, unlike an animal cell, they may have many layers of lipids and aqueous compartments. Liposomal vesicles can be as small as <0.1 mm to 1 mm.
Water-soluble agents can be loaded into the center of the liposome while fat-soluble agents can be incorporated into the lipid bilayer.2
Keller. Trends in Food Science & Technology 12 (2001) 25–31
Liposomal delivery is widely recognized as an improved delivery route for pharmaceuticals. There are a number of medications on the market that utilize liposomal delivery and there are several hundred clinical trials in progress.1
When taken orally, liposomal intestinal absorption is far better than the absorption of the same nutrient in a standard encapsulation.1
Liposomes have therapeutic potential because they can gain entry to the cell, thereby raising intracellular levels of the nutrient, and are retained longer inside the cell.2
Liposomal nutritional supplements have been available on the market for more than 15 years: vitamins A, B2, B12, E, CoQ10, melatonin, and zinc.3
The liposome bilayer protects vitamins, extends the half-life, and facilitates their uptake into cells.3 Liposomal antioxidant formulas have benefits on target tissues by increasing intracellular antioxidant levels and extending the time antioxidants are retained in the cell.2
Stability
The gastrointestinal tract is acidic, propulsive, and constantly mixes the contents of the lumen. This harsh environment can degrade active ingredients. Liposome entrapment has been shown to stabilize encapsulated, bioactive materials against a range of environmental and chemical changes, including:
- Enzymatic
- Chemical modification
- Changes in pH
- Temperature fluctuation
- Ionic strength changes
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Mechanism of Delivery: Mucoadhesion
The GI tract is coated with a thick aqueous layer of mucus. However, mucus retards the adhesion of molecules and can therefore interfere with the oral delivery of nutrients and medications.3 While it is necessary for healthy gastrointestinal function, it makes nutrient delivery difficult.
One way to improve the efficiency in nutrient delivery is to improve adhesion of a substance to the mucosal layer of the gastrointestinal tract.
Mucoadhesion improves contact and adhesion of an active ingredient to the mucus layer of the GI tract.3 Because mucus is an aqueous and lipid mixture, liposomes are ideally suited to diffuse molecules through the mucosal layer and into circulation.
A mucoadhesive formulation offers advantages over traditional delivery including:3
- More contact time between the active ingredient and mucus
- Better, more intimate, contact between the active ingredient and mucus
- Protection of the active ingredients from
Kirby, et al. International Journal of FoodScience and Technology. 1991 26, 437-449.
Research on Liposomal Nutrients
Liposomal nutritional formulas are more bioavailable, more stable, and are more clinically effective than other forms of delivery. CoQ10, which typically has poor solubility, was more bioavailable (absorbed twice as fast) in a liposomal spray than in a gelatin capsule.
Liposomal delivery improved the water solubility of quercetin, prolonging its circulation times and accumulation in lung tissue.4 Liposomal bromelain increased the stability and bioavailability of the enzyme.3
Melatonin in a liposomal spray was 50% more bioavailable and raised circulating levels of melatonin more quickly, than a compressed melatonin tablet.
Liposomal nutrients not only raise circulating levels of nutrients but they also improve functional markers. Vitamin C is highly unstable and liposomal encapsulation led to three times longer half-life.
Vitamin C also has a notoriously slow pattern of absorption but this is accelerated when it is encapsulated within a liposome.1 Liposomal vitamin C led to greater circulating levels than unencapsulated vitamin C1 and protected against ischemia-reperfusion injury, a measure of oxidative damage.1
Liposomal GSH was given to patients with HIV for 13 weeks and intracellular GSH levels significantly increased, as measured by peripheral blood mononuclear cells (PBMCs). Likewise, markers of oxidant stress, blood malondialdehyde, were significantly reduced.5
Liposomal formulations are used in animal and cell studies because of superior stability, bioavailability, and uptake into cells. Liposomal quercetin protected lungs from radiation-induced oxidant damage in an animal study.
Liposomal quercetin was so much more bioavailable than free quercetin, that a lower dose was necessary for injections.4 Pretreatment of cells with liposomal NAC increased intracellular glutathione and reduced the oxidant damage caused by a poisonous herbicide called paraquat, more than free NAC.2
LIPOSOMALs FROM DAVINCI®
Pioneers in nutraceutical science believe liposomal delivery is the next step in advancing supplementation. Doctors are also starting to favor this delivery method because their patients see results and reap more benefits than traditional delivery.