As retailers, you are faced with a continual flow of new supplements—products featuring newly launched ingredients, new blends, and new flavors of gummies or powders. The abundance is exhilarating (customers just love new products!) and angst-inducing (how can I know the product will deliver the desired results?).
Considering what supplements to carry is challenging. You want customers to get what they pay for and to receive all the benefits the brand promises. In other words, you want to ensure your customers are receiving the product’s actives in a way they can be optimally absorbed. Technically speaking, do the product’s actives, as they travel through the small intestines into the bloodstream, lead to higher absorption and better performance in the target tissue?
The answer would be yes if the supplement is manufactured with authentic liposome technology.
Liposomes in General
Based on the concept that a fat helps transport a nutrient through absorption, a liposome is a lipid (fat) protective coating that encases the active ingredient. A true liposome is a precision-oriented structure that can deliver the bioactives (vitamins, minerals, phytonutrients, peptides and EFAs, to name a few) into the bloodstream where they can reach their targets in higher concentrations—with greater bioactivity and performance.
According to Liu et al. [Molecules 2022 Feb 17;27(4):1372)], in the pharmaceutical world, liposomes provide improved site-targeting and release and protection of the active ingredients compared to traditional delivery systems. In the nutraceutical world, this is equally true.
Functionally, a liposome is a high-performing workhorse. It is a tiny sphere-shaped structure, constructed of one or more lipid bilayers (typically comprised of phospholipids). The core of the liposome is the water-soluble/polar component, and the lipid/fat-soluble component is the second layer. The active ingredients may be housed in both sections of the liposome. The liposomal structure is such that it can hold both water- and fat-soluble active ingredients. This characteristic makes liposomes exceedingly flexible for use in a wide variety of formats that appeal to customers.
The strength of the liposomal delivery system is that it works in a way the body naturally prefers to absorb nutrients, with a lipid encasement that protects the payload as it moves through the gastrointestinal (GI) tract. This arrangement enables the nutrient to penetrate the epithelium of the small intestine for intact delivery into the bloodstream. The nature of an effective liposome is to optimize nutrient absorption through the GI tract, increasing its concentrations in blood plasma and optimizing bioavailability in the target tissue.
Key point: the liposome delivery system with the active ingredient within is more bioavailable than the ingredient itself. The liposome allows the active ingredient(s) it contains to be delivered with precision to the target inside the body.
Not all Liposomes Are Created Equally
There are significant differences between liposomes that are formed imprecisely and those that are created with the precision of advanced technology. When tested, many liposomes turn out not to even be liposomes! When we talk about the effectiveness of liposomes, we need to address the reality that most ingredients marketed as liposomal, when properly tested, are found to contain no liposomes whatsoever.
In the nutraceutical industry, there are several liposomes marketed in liquid form, which unfortunately, limits both their application and the ability to control size. Optimizing bioavailability depends on solubility and intestinal permeation, and size is critically important for both these factors. The size of the liposome should be between 100 and 200 nanometers to allow for optimal absorption by the small intestine.
Liposomes are usually made with phospholipids (e.g., phosphatidylcholine, phosphatidylserine, and phosphatidylethanolamine) from sunflower oil, soybean oil and others. That stated, four characteristics define an authentic liposome:
1. The liposomes must have well-defined bilayers and a smooth core surface.
2. They must be nano in size.
3. They must be evenly distributed.
4. They must have an optimal zeta potential correlating with improved stability and reduced possibility of the bioactive leaking out.
Technically speaking, only through advanced testing can a true liposome be identified. A high-powered Cryo Transmission Electron Microscope (CryoTEM) often reveals that many, if not most, contain no lipid bilayers, meaning it is not a liposome. If it has a single phospholipid layer, it is a micelle; if it has no protective layer, it is neither. CryoTEM testing can also show if the liposome is free of leakage, which would tend to occur if there is only one layer or none.
“Zeta potential” describes how tightly the liposome holds onto the ingredient(s) packaged within. A poor Zeta potential reading demonstrates that the liposome is unstable, weak, and can break apart before it reaches its destination, meaning the active ingredient is no longer protected by the liposome and therefore, not receiving its benefits. Zeta potential in the approximate range of -30 to -60 meV is optimal. At this level, the liposome has little chance of the active ingredient leaking out.
The Advantages of Powder Liposomes
The standout advantage of liposomes in powder form is that it allows for more control of the size of the liposome in contrast to the liquid form, which is a desirable attribute depending on the brand manufacturer’s application.
The patent pending LipoVantage process effectively dehydrates the liposome so that its structure and contents remain intact, and the hydrophilic polar core holds strong. To further protect the liposome, DualHydrogel Technology uses a proprietary blend of natural polar ingredients in and around the liposome structure to prevent potential collapse during the dehydration process. This technology also enhances stability in the body and improves bioavailability.
While many liposomes are limited in how they can be used, LipoVantage is versatile and can be used effectively in not only tablets and capsules but also in gummies, chews, functional foods, RTDs and more. The technology can also be used topically for skin care and cosmetic products.
Best in Class Vitamin C Clinical Study
Vitamin C, still the best-selling single vitamin, was made into liposomal form using LipoVantage technology. Specnova recently conducted a randomized, double-blind, placebo-controlled study that investigated absorption and bioavailability at different time points. It was found that there were higher levels of LipoVantage vitamin C in leukocytes, 20 percent more than non-liposomal vitamin C. This shows that higher levels of the vitamin are reaching their target. Higher levels of vitamin C in the blood doesn’t guarantee it’s reaching the location where it needs to be. Knowing that the vitamin C is actually making it to the leukocytes is essential.
To date, this is one of the best vitamin C studies available, measuring the absorption/bioavailability of both liposomal and non-liposomal vitamin C. The gold standard for clinical studies was employed, i.e., a double-blind, placebo-controlled, cross-over study. Other vitamin C studies use open-label designs with no control group or use unrealistically high vitamin C mega-doses of 4-36 g to bring about a better outcome.
Other research that looked at increased concentrations of vitamin C in leukocytes, showed no difference from standard vitamin C or placebo and/or no difference to standard vitamin C in blood plasma. To date, there is no therapeutic substitute for LipoVantage Vitamin C—as proven through clinical research and in-vitro studies.
In yet another test, a fasted and fed intestinal in-vitro model, LipoVantage vitamin C powder was shown to be 1.4 times more stable in the small intestines than non-liposomal vitamin C. Vitamin C is unstable in the 6.8 pH of the small intestine. The stability of a 500 mg dose of vitamin C as ascorbic acid was tested in simulated intestinal fluid for two hours, comparing non-liposomal USP vitamin C against a competitor liposomal vitamin C and Specnova LipoVantage vitamin C.
The degradation of LipoVantage liposomal vitamin C powder was 55 percent less than that of the non-liposomal USP reference standard and the competitor liposomal vitamin C. In the simulated intestinal fluid study, non-liposomal vitamin C and the competitor liposomal vitamin C had a 42 percent disintegration, leaving 58 percent (or 290 mg) available for absorption. LipoVantage vitamin C only had a 20 percent disintegration, with 80 percent (or 405 mg) ready and available for absorption.
There are true liposomes and those that claim to be. When reviewing liposomal supplements to add to your shelves, be sure to ask the manufacturer if the liposomes have well-defined bilayers shown via CryoTEM, as well as the Zeta potential of the liposomes in the formula and the particle size and distribution shown via DLS. You can also ask about the encapsulation efficiency of the liposomes. A manufacturer of true liposomes should be able to supply that information on request.
Customers are wide open to trying new supplements and new technologies that are proven to work. When they purchase these products, they trust they will deliver on marketing claims. Beyond the human clinical trials showing increased efficacy, customers will let you know if they’re getting results and feeling the difference. True liposomes, if they’re truly liposomal, will deliver results, and you’ll definitely hear that good news. VR
Sebastian Balcombe is the CEO and founder of Specnova, a biotech innovator in the nutraceuticals industry, based in Virginia.