The Liposomal Difference: A Breakthrough in Nutrient Delivery
Josh Rimany, RPh., FACA, IFMCP
Clinical Benefits
• High bioavailability and absorption
• Protecting nutrients against the harsh environment of the GI tract
• Increased uptake into cells
• Liposomes can be formulated to hold both water & fat soluble nutrients
• Enhanced compliance for those who have trouble swallowing large tablets
• Less drug-nutrient interactions
Overview
In today’s health and wellness landscape, supplements are widely used and consumed. Two out of three Americans take some kind of supplement everyday. Whether its a vitamin, mineral, or herbal product, it is clear that we perceive benefits from taking various different supplements. However, just because we consume vitamins and nutrients on a regular basis, does not necessarily mean we are absorbing them. Orally administered vitamins (and drugs) typically show low absorption, or bioavailability, due to their degradation by enzymes in the gastrointestinal (GI) tract, the difficulty of absorbing them in the small intestine, and thefirst-pass metabolism in the liver.
In order to offer health benefits, vitamins and minerals need to reach the target tissue of action.Bioavailability is key for vitamins and supplements to reach their full potential and efficacy. Many factors affect bioavailability—including digestive problems, low stomach acid, or lowuptake of a nutrient. In reality, traditional oral vitamins and micronutrients lose the majority of their potency through digestion, metabolism and excretion, prior to reaching the cells in our body.
Liposomes: A breakthrough in medication delivery
Every cell in our body has a membrane composed of a lipid bilayer. This membrane performs many kinds of functions in our body like protecting the inside of the cell, allowing nutrients to pass through it, and expelling wastes and toxins. Mostly composed of phospholipids, the cell membrane is not
only protective, it is highly active.
In the 1960’s, scientists discovered using liposomal delivery of medications. Liposomes are tiny phospholipid bubbles with a bilayer structure very similar to that of our cell membranes. By encapsulating a drug around a phospholipid, they become highly biocompatible, delivering small amounts of therapeutic substances to the specific tissues of the body, without affecting any other part of the body.
Taking pharmaceutical science to nutrition…..
Until very recently, the use of liposomes were primarily directed at targeted drug delivery.However, the versatile abilities of liposomes are now being discovered in other settings. Liposomes are presently being implemented for the specific oral delivery of certain dietary and nutritional supplements.
A very small number of dietary and nutritional supplement companies are currently pioneeringthe benefits of this unique science towards this new application. This new direction and employment of liposome science is in part due to the low absorption and bioavailability rates of traditional oral dietary and nutritional tablets and capsules. The low oral bioavailability and absorption of many nutrients is clinically well documented. Therefore, the natural encapsulation of lipophilic and hydrophilic nutrients within liposomes has made for a very effective method of bypassing the destructive elements of the gastric system and aiding the encapsulated nutrient to be delivered to the cells and tissues.
Several different healthy substances, such as vitamins, minerals and other supplements, can be encapsulated within these liposome membranes. Liposomes are very specific ‘vesicles’ or bubbles modified to carry either fat-soluble or water soluble molecules. Their likeness to our living bilayer lipid cell membranes is remarkable. If a vitamin or nutrient is placed inside the liposome, it will not readily pass through the bilayer. Yet when the liposome merges with the lipid bilayer of the cell membrane, it can deliver its contents directly to the cell. Liposomes are designed not only to protect the nutritional supplement from degrading and absorbing in the harsh environment of the gut terrain, but also to deliver the nutrients in a targeted manner to specific tissues and areas of the body.
Size matters…..and smaller is best
In order for liposomes to be effectively and efficiently absorbed into the cell, they need to be a certain size. If the liposome matrix is too large, it will not be absorbed and will get excreted. By utilizing nanotechnology and reducing particle sizes to sizes typically less than 150ng, nutrients can be absorbed properly into the cell for maximum efficiency.
Not all liposomes are the same
There is an art and science to creating liposomal delivery in dietary supplements. Many factors come into play in proper liposomal nutritional
manufacturing. This process and technology is complicated and involves many steps to ensure proper stability, potency, compatibility and
consistency. Not all manufacturers standardize, research, validate, or test these processes. There is no standardization or specific labeling requirements for liposomal manufacturers, so it can be. difficult as a consumer to know what you are actually getting. Asking the right
questions and validating these processes with nutritional companies is a good first step in understanding a quality product.
Factors in making liposomes
• The actual manufacturing method and preparation of the liposomes themselves
• The constitution, quality, and type of raw phospholipid used in the formulation and manufacturing of the liposomes
• The ability to create homogeneous liposome particle sizes that are stable and hold their encapsulated payload
• The physicochemical characteristics of the material to be entrapped and those of the liposomal ingredients
• The nature of the medium in which the lipid vesicles are dispersed
• The effective concentration of the entrapped substance and its potential toxicity
• Additional processes involved during application/delivery of the vesicles
• Optimum size, polydispersity and shelf-life of the vesicles for the intended application
• Batch-to-batch reproducibility and possibility of large-scale production of safe and efficient liposomal products
Liposomal nanotechnology = higher bioavailability
Liposomes are thought to be absorbed through different mechanisms than traditional oral dosage forms. Traditional oral dosage forms are absorbed through first pass metabolism in the liver, where the nutrient (or drug) is metabolized and broken down before it goes into circulation, where it is then delivered to the tissue. Liposomes are absorbed through the oral mucosal lining and through lymphatic mechanisms in the gut, therefore bypassing first pass metabolism and breakdown in the liver. This higher absorption means greater efficacy with smaller doses needed to achieve better results.
FAQ: The many clinical benefits of Liposomal nutrient delivery
Higher bioavailability and absorption
By using liposomal nanotechnology, dietary supplements can achieve up to 5-10 times more bioavailability than standard oral supplements. Liposomes are primarily absorbed through the oral mucosal lining and through lymphatic mechanisms in the gut, rather than first pass metabolism in the liver. This higher absorption means greater efficacy with smaller doses needed to achieve better results.
Protecting nutrients against the harsh environment of the GI tract
Encapsulating a phospholipid around a dietary supplement with liposomes protects the nutrient from being degraded and broken down by the body, thus allowing more nutrients to be utilized.
Increased uptake into cells
Liposomes likeness to our living bilayer lipid cell membranes has a clear advantage for absorbing dietary supplements. Creating this molecular mimicry allows our body to use its own mechanisms to directly absorb the targeted nutrients into the tissue where these nutrients function and work.
Liposomes can be formulated to hold both water & fat soluble nutrients
Liposomes can now be used in a wide variety of dietary supplements and formulations. By having the technology and experience, we now can formulate many different and efficacious products, unique in the industry.
Enhanced compliance for those who have trouble swallowing large tablets
In today’s health and wellness landscape, it is easy to create a “pill burden” when it comes totaking multiple medications, dietary supplements, and nutritional products. By utilizing small amounts of liquids, we can obtain greater compliance and therefore better outcomes.
Less drug-nutrient interactions
Many dietary supplements interact with numerous medications and can present significant complications if not addressed properly. Bypassing first pass metabolism with liposomes has its pharmacological clinical advantages. Lymphatic absorption of liposomes are absorbed through different mechanisms than most medications, thereby decreasing the likelihood of drug-nutrientcomplications and more consistent outcomes.
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