Considerable research has gone into developing alternative delivery methods for medicines and nutraceutical products, with liposomes emerging as one of the more promising avenues. In this article, Natalie Gerhardt of Multichem Sourcing explores the technology and its benefits.
In today’s world, we anticipate swift and effortless delivery of our needs and desires. This applies to everything from ecommerce purchases to the medicines and supplements we administer to maintain optimum health.
When it comes to medicines and nutraceutical products, conventional delivery methods may be painful (injections or IVs). There is also the issue of sub-optimal bioavailability. That is, the active ingredients in the medicine or supplement may become diluted or degraded during interaction with the human body, or their action may be slowed down. In the case of tablets and capsules, excipients, binders, fillers and flow agents can contribute to poor disintegration rates, leading to poor absorption. This can happen even when the active ingredients are delivered at the right dose.
For a formulator, the most pressing challenge is to ensure that the active ingredients move into the bloodstream and reach the cells where they are needed.
The technology at a glance
In a liposome, active ingredients are surrounded by a sphere of phospholipids (the same fat molecules that make up cell walls). This protects the active ingredients and allows them to better survive the digestive process and enter the intestines. Here, the liposome fuses with the cell walls and the active ingredients are released.
Depending on the ingredient, absorption may increase by a factor of up to 20 – a positive result that has been supported by many scientific studies worldwide. More recently, the liposome delivery method has been used more frequently in natural health applications and nutritional supplements.
In an article entitled Curing The Incurable, author Thomas E Levy MD states that, “a much smaller oral dose of liposome encapsulated vitamin C, (5g to 10g), often results in a clearly superior clinical response than a much larger dose of vitamin C given intravenously (25g to 100g).”
Benefits of liposomes
The primary advantage of liposomes is that they increase the bioavailability of their ‘payloads’ – that is, of the substances they contain. Enhanced bioavailability has multiple ancillary benefits, including more precise doses, and reduced costs, as smaller quantities are required to achieve the same outcome. This helps avoid reduced impacts associated with under-delivery, as well as toxicity risks caused by over-delivery.
In a nutraceutical context, liposomes ensure efficient delivery to target cells and enhanced absorption rates of nutrients, with multiple physical health benefits including support for healthy cell structures and maintenance of healthy liver tissue.
Liposomes are biocompatible and biodegradable (the phospholipids used are derived from seed oils eg, sunflower oil). Liposome-enabled delivery allows for adjustable and incremental dosing and avoids the need for IVs and injections.
Solving the challenges of liposomal delivery
Many studies exist on the efficacy of medicinal liposomal delivery systems, both liquid and dry. Indeed, their efficacy is no longer in question. There are also multiple studies showing that liposomes are an effective delivery system for vitamins and other supplements. However, liquid liposomes (whether delivered by injection or orally) are imperfect; they degrade quite quickly and have a short half-life. They are also more likely to break down in the stomach. This is not to say that they are ineffective, but rather that they are less stable. Liquid liposomes tend to demonstrate low solubility and can be prone to leakage of the encapsulated molecules.
Innovative and promising methods developed to address these issues include the use of so-called proliposomes. Work on pharmaceutical applications for these dry liposomes began in the 1980s and soon showed that their stability is far superior to that of regular liquid liposomes. They are a dry, free-flowing granular material (powder), which immediately forms a liposomal dispersion on contact with water or biological fluids within the body. When the dry powders are hydrated and gently mixed (as occurs in the stomach), the contents rapidly disperse to create a liposomal suspension in the aqueous solution.
Ensuring quality
In today’s world, ingredient fraud is a major issue. Most manufacturers are not able to test the exact purity and stability of the liposomes they purchase. While many suppliers offer these products, only a handful can genuinely produce the stable form.
Multichem Sourcing, a SAHPRA licensed importer, rigorously vets suppliers and can confidently offer a wide range of the high-quality liposomal ingredients. The company’s current liposome range includes ascorbic acid (vitamin C), glutathione, vitamin B complex, curcumin, NMN, PEA and omega derivatives, among others.
The future of liposomes
The increased use of liposomes in nutraceuticals has been linked to the growth in the use of pure compounds and complex botanicals – a trend that is aligned with intensified consumer focus on all aspects of wellness.
The future looks bright for liposomes, with new and advanced production methods allowing for smaller and more stable liposomes and consequently, faster absorption rates and increased circulation time within the body.
About the author
Natalie Gerhardt (BSc. Hons. in Biochemistry and Microbiology) is the managing director of Multichem Sourcing, a raw materials and chemicals sourcing specialist based in South Africa. The SAHPRA licensed company focuses on sourcing and supplying APIs and raw materials required for API synthesis. Multichem Sourcing supports the pharmaceutical, nutraceutical, cosmetics, agricultural and veterinary industries.
