The Secret To Effective Liposomal Delivery

Sponsored by Quicksilver Scientific

By Christopher Shade, PhD

April 09, 2017

The future is here. The nutritional industry now has access to pharmaceutical-grade liposomes that can provide the power of intravenous therapy in the convenience of oral supplements. This is exciting, for sure, but are the claims made by all companies that offer liposomal supplements true? Not necessarily. “Liposomal delivery” is a pretty broad term and certainly not all liposome products are created equal.

There are definitely key advantages with liposome products but as with anything, there are two sides of this coin. Below is a list of advantages, as well as potential disadvantages, of liposomal delivery and the production of liposomal supplements.

Advantages Disadvantages
Increased bioavailability Manufacturing issues (high particle size, poor ingredients)
Increased cellular delivery Instability of some products
Able to deliver both hydrophilic and hydrophobic compounds Higher cost
Increased oral uptake and lymphatic absorption  
Convenient for the patient  

There is no question that correctly-made liposomal products provide improved systemic and cellular absorption of nutrients. Biocompatible liposomes have intraoral and lymphatic absorption, impacting systemic circulation in a way that until now only intravenous therapies could achieve. Additionally, lymphatic delivery via liposomes bypasses the first-pass metabolism in the liver, which also increases oral bioavailability.1

This is all very exciting in theory, but the critical step along the way to make this happen, and where some of the companies are lacking, is in the manufacturing process. Many companies produce liposomes that are instable, and are too large in size for the body to optimally absorb and utilize them. For liposomal supplement delivery, size really does matter.

Until recently, nutritional manufacturers have used low-to-medium shear methods with large lecithin loads, producing gel-phase products with very large diameter particles and a wide range of sizes, typically 400 to 1000 nm.2 Alternately, they are produced with rotor-stator dispersion devices that create a milky liposomal solution with particles ranging from 200 to 400 nm in size.

Smaller liposomal spheres and emulsions are the result of refined chemistry and high-shear equipment, which of course, comes at a cost in terms of production. But in the end, those larger-sized spheres are not as bioavailable as the smaller liposomes, leaving the consumer with a less effective, yet still a high-cost product.

Smaller liposomes are far more efficient at intracellular delivery. In one study, cellular intake increased 9-fold as the liposome size was decreased from 236 nm to 97 nm, and cellular intake was increased 34-fold at 64 nm.3 In addition, the therapeutic capabilities of a liposomal delivery system are also related to how fast the body clears the liposomes from the blood. It’s not surprising that clearance is inversely related to size, with the smaller liposomes and micronized emulsions circulating in the blood the longest.4 Larger liposomes are recognized by the macrophages of the immune system as foreign invaders, and cleared from the blood more rapidly.

Manufacturers of liposome products have a responsibility to tightly control purity with a focus on sphere size. The optimal range is 50 to 100 nm and should be verified using Laser Dynamic Light Scattering technology.5

A properly manufactured liposomal product will fuse with cell membranes and facilitate efficient intracellular delivery. The lipid membranes of the liposome, usually comprised mostly of phosphatidyl choline, fuse with the cell membrane, supporting effective cell membrane function and signaling throughout the body. To claim that a liposomal product can be as effective as intravenous therapy, manufacturers must emphasize with their production and quality control process the liposomal purity, quality, and size. And in this case, the smaller the better.

This information was brought to you by Quicksilver Scientific. All practitioners who register will receive wholesale pricing on all Quicksilver Scientific products.

About the Author

Christopher Shade, PhD, obtained bachelor of science and masters of science degrees from Lehigh University in environmental and aqueous chemistry, and a PhD from the University of Illinois where he studied metal-ligand interactions in the environment and specialized in the analytical chemistries of mercury. During his PhD work, Shade patented analytical technology for mercury speciation analysis and later founded Quicksilver Scientific, LLC, to commercialize this technology. Shortly after starting Quicksilver Scientific, Shade turned his focus to the human aspects of mercury toxicity and the functioning of the human detoxification system. He has since researched and developed superior liposomal delivery systems for the nutraceutical and wellness markets and also specific clinical analytical techniques for measuring human mercury exposure. He used his understanding of mercury and glutathione chemistry to design a unique system of products for detoxification that repairs and then maximizes the natural detoxification system.

References

  1. Ahn H, Park JH. Liposomal delivery systems for intestinal lymphatic drug transport. Biomater Res. 2016 Nov 23;20:36.
  2. Shade C. Liposomes as advanced delivery systems for nutraceuticals. Integr Med. 2016;15(1):33-36.
  3. Klibanov AL, Maruyama K, Beckerleg AM, et al. Activity of amphipathic poly(ethylene glycol) 5000 to prolong the circulation time of liposomes depends on the liposome size and is unfavorable for immunoliposome binding to target. Biochim Biophys Acta – Biomembranes. 1991;1062(2):142–148.
  4. Kraft JC, Freeling JP, Wang Z, Ho RJ. Emerging research and clinical development trends of liposome and lipid nanoparticle drug delivery systems. J Pharm Sci. 2014 Jan;103(1):29-52.
  5. Laouini A, Jaafar-Maalej C, Limayem-Blouza I, et al. Preparation, characterization, and applications of liposomes: State of the art. J Colloid Sci Biotechnol. 2012;1:147–168.