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If you’ve been in the dietary supplement industry for the past 20 years, no doubt you’re familiar with liposomes as a delivery system for nutraceuticals. In fact, today there are a range of different nutraceuticals available in liposomal form with claims of improved bioavailability. However, since multiple raw material suppliers offer liposomes, it is important to establish if the raw material being offered is, in fact, a true liposome that can deliver promised benefits. To understand this better, let’s start this article with an introduction to liposomes.
Introduction to Liposomes
Liposomes are a technology for transporting substances into the body effectively by way of promoting absorption directly in the mouth or by preventing breakdown by stomach acid. Starting in the 1970s, liposomes were investigated for their appeal as a potential drug delivery system. That appeal was due to the fact that liposomes offered biocompatibility and the ability to incorporate both hydrophilic (i.e., mixes well with water) and hydrophobic (i.e., doesn’t mix well with water) agents. Nevertheless, it wasn’t until the late 1990s that that liposomal technologies were sufficient to be utilized successfully in commercial products. Part of this is due to the availability of quality phospholipids needed to create liposomes and reliable homogenization and sizing equipment have become routinely available.1 Nutritional industry use of liposomes will grow rapidly in the next five to 10 years. High-quality products with more complex mixtures of pure compounds and complex botanical mixtures will offer clinicians less-invasive options for dosing and delivery of these actives.
Structure of Liposomes
Liposomes are one of several types of lipid-based delivery systems. The most common of these is an emulsion, such as that used in a skin cream or foods like mayonnaise. In these, oil and water are brought together in a stable form for a limited time. Emulsions use surfactants, which can interact with both water and oil, such as lecithin, to stabilize drops of oil in water or vice versa.
Liposomes are different. Rather than using a surfactant to stabilize oil in water, the phospholipids are arranged into spherical cell membrane where lipid bilayers with their water-loving “heads” face toward the aqueous medium and their fatty “tails” tuck toward each other. This creates pockets of entrapped water along with water soluble compounds and potentially protect them from harsh digestive conditions while helping to facilitate gastrointestinal uptake.
In addition, the hydrophobic fatty acid core of the bilayers is able to provide hydrophobic compounds, whereby a small spherical package is created that could carry both hydrophilic and hydrophobic compounds. Interactions between the liposome membrane and cell membranes further offer the potential of enhanced cellular uptake.2,3 Essentially, liposomes pass through the digestive tract without much nutrient loss and travel directly into the bloodstream where they can be delivered directly into the body’s cells. As a result, liposomes maximize ingredient absorption.
Real Liposomal Technology
Unfortunately, some raw materials sold as liposomes are actually fatty acids blended with nutraceuticals, and not a true liposome. In addition, the liposomal ingredient market is saturated with products that rely on “thin film dispersion” or “double freeze-dried emulsions,” which are methods that produce volatile liposomal delivery capsules where the nutrients disperse before making it into the cell.
Based upon my research, one particularly good liposomal technology is Liposomax, a liposomal encapsulation method that improves ingredient absorption as well as efficacy. Here’s what I found.
Independent laboratory analysis at Australia National University4 was conducted on Liposomal Pureway-C (which uses Liposomax liposomal technology) two TEM (Transmission Electron Microscopy) test methods (Cryo-TEM & Negative Staining TEM) to confirm the liposomal nature of the start material and the finished compressed tablet. TEM is the most frequently used imaging method for the validation and evaluation of the structure of a liposome, and is imaging is necessary because the liposomes are sub-microscopic in size, so a normal microscope is not strong enough to detect the liposomes.
Results showed: “Single and multilamellar vesicles could be observed. Mainly round liposomes were observed but elongated shapes were not uncommon. The size range of liposomes found in our analysis was between 20 nm and 1 um.” In other words, Liposomax liposomes were found to be the real deal. The graphics below show the results of the TEM analysis.
In addition, subsequent TEM analysis was conducted on other nutraceuticals using Liposomax liposomal technology. This includes liposomal glutathione, liposomal melatonin, liposomal quercetin and liposomal vitamin D3. Included are the images confirming that true liposomes were also formed with these nutraceuticals.
By contrast, certain other such liposome materials currently offered on the marketplace have not been shown to be true liposomes via TEM analysis:
Absorption With Liposomes
To assess cellular absorption of liposomal vitamin C (Liposomax), human epithelial cells were collected and starved for 24 hours and then treated with 0.5 mM of ascorbic acid that was either in liposomal form (blue line with circles) or non-liposomal ascorbic acid (red line with squares). An analysis of variance demonstrated that the liposomal vitamin C showed four times better absorption than non-liposomal vitamin C as early as 10 minutes after treatment of the cells and at all time points tested.
Efficacy With Liposomes
Efficacy with liposomal vitamin C (Liposomax) was also demonstrated in other cellular studies.5 In one, human kidney epithelial cells were grown in a single layer. A wound was produced using a sterile pipett tip, and the cells were thee immediately treated with ascorbic acid, non-liposomal vitamin C or liposomal vitamin C and inculated for 24 hours. The results clearly demonstrated that the wound healed more quickly and effectively with liposomal vitamin C.
Neurogenesis is the process by which nervous system cells, the neurons, are produced by neural stem cells. Neuritogenesis, or the sprouting of neurites from a cell, is the first step in the development of a mature neuron. An experiment5 was conducted in which neuron cells were treated with non-liposomal and liposomal vitamin C and observed over six hours for neuritogenesis. Results showed that liposomal PureWay-C was superior in supporting neuronal cell differentiation and function as measured by neuritogenesis.
Conclusion
Liposomes may serve as a delivery system for nutraceuticals, although it is important to establish if liposomal raw materials being offered are true liposomes. Independent laboratory analysis using TEM have demonstrated that Liposomax liposomal technology produces true liposomes. Furthermore, these same liposomes have been shown to have improved absorption and improve efficacy in wound healing and neuritogenesis as demonstrated with a liposomal preparation of Pureway-C. VR
References
1 Shade CW. Liposomes as Advanced Delivery Systems for Nutraceuticals. Integr Med (Encinitas). 2016 Mar;15(1):33-6.
2 Lelkes PI, Friedman JE. Interaction of French-pressed liposomes with isolated bovine adrenal chromaffin cells. Characterization of the cell-liposome interactions. J Biol Chem. 1985 Feb 10;260(3):1796-803. PMID: 3838175.
3 Lelkes PI, Friedman JE. Interaction of French-pressed liposomes with isolated bovine adrenal chromaffin cells. Characterization of the cell-liposome interactions. J Biol Chem. 1985 Feb 10;260(3):1796-803. PMID: 3838175.
4 Rug M. Report: TEM analysis of 2 samples provided. PureWay-C Liposomal Vitamin C 70% Fine Powder (Lot # 792-LPFP70-062121-A1). PureWay-C Liposomal Vitamin C 70% Tablets (# EX21074/1). Australian National University. 16 February 2021.
5 Personal communication with Dr. Pedro Perez, One Innovation Labs.
Gene Bruno, MS, MHS, the provost for Huntington University of Health Sciences, is a nutritionist, herbalist, writer and educator. For more than 40 years he has educated and trained natural product retailers and health care professionals, has researched and formulated natural products for dozens of dietary supplement companies, and has written articles on nutrition, herbal medicine, nutraceuticals and integrative health issues for trade, consumer magazines and peer-reviewed publications. He can be reached at gene.bruno@hchs.edu.
If you’ve been in the dietary supplement industry for the past 20 years, no doubt you’re familiar with liposomes as a delivery system for nutraceuticals. In fact, today there are a range of different nutraceuticals available in liposomal form with claims of improved bioavailability. However, since multiple raw material suppliers offer liposomes, it is important to establish if the raw material being offered is, in fact, a true liposome that can deliver promised benefits. To understand this better, let’s start this article with an introduction to liposomes.
Introduction to Liposomes
Liposomes are a technology for transporting substances into the body effectively by way of promoting absorption directly in the mouth or by preventing breakdown by stomach acid. Starting in the 1970s, liposomes were investigated for their appeal as a potential drug delivery system. That appeal was due to the fact that liposomes offered biocompatibility and the ability to incorporate both hydrophilic (i.e., mixes well with water) and hydrophobic (i.e., doesn’t mix well with water) agents. Nevertheless, it wasn’t until the late 1990s that that liposomal technologies were sufficient to be utilized successfully in commercial products. Part of this is due to the availability of quality phospholipids needed to create liposomes and reliable homogenization and sizing equipment have become routinely available.1 Nutritional industry use of liposomes will grow rapidly in the next five to 10 years. High-quality products with more complex mixtures of pure compounds and complex botanical mixtures will offer clinicians less-invasive options for dosing and delivery of these actives.
Structure of Liposomes
Liposomes are one of several types of lipid-based delivery systems. The most common of these is an emulsion, such as that used in a skin cream or foods like mayonnaise. In these, oil and water are brought together in a stable form for a limited time. Emulsions use surfactants, which can interact with both water and oil, such as lecithin, to stabilize drops of oil in water or vice versa.
Liposomes are different. Rather than using a surfactant to stabilize oil in water, the phospholipids are arranged into spherical cell membrane where lipid bilayers with their water-loving “heads” face toward the aqueous medium and their fatty “tails” tuck toward each other. This creates pockets of entrapped water along with water soluble compounds and potentially protect them from harsh digestive conditions while helping to facilitate gastrointestinal uptake.
In addition, the hydrophobic fatty acid core of the bilayers is able to provide hydrophobic compounds, whereby a small spherical package is created that could carry both hydrophilic and hydrophobic compounds. Interactions between the liposome membrane and cell membranes further offer the potential of enhanced cellular uptake.2,3 Essentially, liposomes pass through the digestive tract without much nutrient loss and travel directly into the bloodstream where they can be delivered directly into the body’s cells. As a result, liposomes maximize ingredient absorption.
Real Liposomal Technology
Unfortunately, some raw materials sold as liposomes are actually fatty acids blended with nutraceuticals, and not a true liposome. In addition, the liposomal ingredient market is saturated with products that rely on “thin film dispersion” or “double freeze-dried emulsions,” which are methods that produce volatile liposomal delivery capsules where the nutrients disperse before making it into the cell.
Based upon my research, one particularly good liposomal technology is Liposomax, a liposomal encapsulation method that improves ingredient absorption as well as efficacy. Here’s what I found.
Independent laboratory analysis at Australia National University4 was conducted on Liposomal Pureway-C (which uses Liposomax liposomal technology) two TEM (Transmission Electron Microscopy) test methods (Cryo-TEM & Negative Staining TEM) to confirm the liposomal nature of the start material and the finished compressed tablet. TEM is the most frequently used imaging method for the validation and evaluation of the structure of a liposome, and is imaging is necessary because the liposomes are sub-microscopic in size, so a normal microscope is not strong enough to detect the liposomes.
Results showed: “Single and multilamellar vesicles could be observed. Mainly round liposomes were observed but elongated shapes were not uncommon. The size range of liposomes found in our analysis was between 20 nm and 1 um.” In other words, Liposomax liposomes were found to be the real deal. The graphics below show the results of the TEM analysis.
In addition, subsequent TEM analysis was conducted on other nutraceuticals using Liposomax liposomal technology. This includes liposomal glutathione, liposomal melatonin, liposomal quercetin and liposomal vitamin D3. Included are the images confirming that true liposomes were also formed with these nutraceuticals.
By contrast, certain other such liposome materials currently offered on the marketplace have not been shown to be true liposomes via TEM analysis:
Absorption With Liposomes
To assess cellular absorption of liposomal vitamin C (Liposomax), human epithelial cells were collected and starved for 24 hours and then treated with 0.5 mM of ascorbic acid that was either in liposomal form (blue line with circles) or non-liposomal ascorbic acid (red line with squares). An analysis of variance demonstrated that the liposomal vitamin C showed four times better absorption than non-liposomal vitamin C as early as 10 minutes after treatment of the cells and at all time points tested.
Efficacy With Liposomes
Efficacy with liposomal vitamin C (Liposomax) was also demonstrated in other cellular studies.5 In one, human kidney epithelial cells were grown in a single layer. A wound was produced using a sterile pipett tip, and the cells were thee immediately treated with ascorbic acid, non-liposomal vitamin C or liposomal vitamin C and inculated for 24 hours. The results clearly demonstrated that the wound healed more quickly and effectively with liposomal vitamin C.
Neurogenesis is the process by which nervous system cells, the neurons, are produced by neural stem cells. Neuritogenesis, or the sprouting of neurites from a cell, is the first step in the development of a mature neuron. An experiment5 was conducted in which neuron cells were treated with non-liposomal and liposomal vitamin C and observed over six hours for neuritogenesis. Results showed that liposomal PureWay-C was superior in supporting neuronal cell differentiation and function as measured by neuritogenesis.
Conclusion
Liposomes may serve as a delivery system for nutraceuticals, although it is important to establish if liposomal raw materials being offered are true liposomes. Independent laboratory analysis using TEM have demonstrated that Liposomax liposomal technology produces true liposomes. Furthermore, these same liposomes have been shown to have improved absorption and improve efficacy in wound healing and neuritogenesis as demonstrated with a liposomal preparation of Pureway-C. VR
References
1 Shade CW. Liposomes as Advanced Delivery Systems for Nutraceuticals. Integr Med (Encinitas). 2016 Mar;15(1):33-6.
2 Lelkes PI, Friedman JE. Interaction of French-pressed liposomes with isolated bovine adrenal chromaffin cells. Characterization of the cell-liposome interactions. J Biol Chem. 1985 Feb 10;260(3):1796-803. PMID: 3838175.
3 Lelkes PI, Friedman JE. Interaction of French-pressed liposomes with isolated bovine adrenal chromaffin cells. Characterization of the cell-liposome interactions. J Biol Chem. 1985 Feb 10;260(3):1796-803. PMID: 3838175.
4 Rug M. Report: TEM analysis of 2 samples provided. PureWay-C Liposomal Vitamin C 70% Fine Powder (Lot # 792-LPFP70-062121-A1). PureWay-C Liposomal Vitamin C 70% Tablets (# EX21074/1). Australian National University. 16 February 2021.
5 Personal communication with Dr. Pedro Perez, One Innovation Labs.
