What Is Liposomal Delivery?

You may have heard about the latest “trend” in the health and wellness world – liposomal delivery. But what does it mean, and why is it so important? What is liposomal technology used for, and why should you keep an eye on this marvel delivery system? Let’s take a look!

While many people use liposomal and liposomes synonymously, they’re two separate things entirely.

We’ll get into both on a much deeper level further in the article, but for now, here’s a basic differentiation of the two terms:

Liposomes

These are the microscopic particles that contain and protect active ingredients prior to targeted delivery.

Liposomal

This technology is the delivery system that makes liposomes able to be used for so many applications.

Before we get into what liposomal delivery is, we’ll need to take a closer look at liposomes. We’ll discuss what they are, how they work, and why they’re an essential part of this marvel of a drug delivery system.

Liposomes are artificially made vesicles (small cellular containers) that have been uniquely designed to safely deliver a variety of bioactive compounds from point A to point B.

Liposomes are capable of transporting both hydrophilic (water-soluble) and hydrophobic (water-repelling) substances, making them applicable in a variety of fields, from agriculture to pharmaceuticals.

To understand how liposomes work, we’ll need to take a closer look at the structural design of these microscopic cellular marvels.

Liposomes are composed of two molecules

that form a sturdy cellular container. When phospholipids (fatty-acid-like lipids) are combined with water, they become spherical in shape with a self-sealing aqueous (water-like) core.3

A variety of vitamins, minerals, and/or plant extracts can then be placed into the core of liposomes for maximum bioavailability.

The two layers of phospholipids allow liposomes to target specific cells while maintaining structural integrity during their journey through the body. Nutrients arrive where they need to go without prematurely breaking down.

Liposomes are a simple, yet superior drug delivery system (DDS). They’re the ideal transport method for otherwise volatile nutrients like antioxidants and antimicrobials.

Are There Different Types of Liposomes?

Yes – Liposomes are classified according to the structure of lipid bi-layers and the size of the cellular container. While we won’t get too deep into the different types of liposomes, it can be important to understand the unique qualities of each.

There are 4-types of liposomes:

Size plays a big role in liposome efficacy and the molecule’s overall half-life (the time it takes for the amount of a drug’s active substance in your body to reduce by half).

LUV (Large Unilamellar Vesicles) –
These are the most commonly used liposomes for drug delivery.

SUV (Small Unilamellar Vesicles) –
Candidate carrier for oral application.

MLV (Multilamellar Vesicles) –
Candidate carrier for oral delivery.

MVV (Multivesicular Vesicles) –
These liposomes are not viable for oral drug applications.

Size plays a big role in liposome efficacy and the molecule’s overall half-life (the time it takes for the amount of a drug’s active substance in your body to reduce by half).

Liposomes for Oral Drug Delivery (ODD)

Liposomes have been on the radar for medical applications since their discovery in 1961 by Alec D. Bangham. However, until recently, there have been some set-backs with the use of liposomes in oral drug delivery.

On their own, liposomes can be problematic for oral application. Researchers noticed that liposomes tended to have instability in the gastrointestinal (GI) tract as well as the inability to easily cross certain cell membranes.5

Additionally, the process of creating liposomes can be tedious at best and expensive at worst. Mass production of liposomes just wasn’t in the picture. Yet.

Research showed the potential capabilities of liposomes in drug delivery but until recently, there were too many set-backs for oral methods. That’s where liposomal delivery comes in.

Liposomal is a 100% DNA-free process that allows for maximum benefits with very few known drawbacks.⁴

Liposome encapsulation efficiency increases with liposome size and decreases with the number of bi-layers. The ideal liposome for drug delivery has 2 bi-layers and is sized anywhere from 50 nm to 150 nm. These are usually the LUV liposomes we mentioned above.

Liposomal is a critical discovery for optimal drug delivery. Liposomal technology allows the active ingredient it’s carrying to get from Point A to Point B without breaking down in the mouth or stomach. Absorption is primarily done in the small intestines where nutrients are most beneficial.

Liposomal technology can uniquely be used for both hydrophilic (water-absorbent) and hydrophobic (water-resistant) delivery methods. That’s because liposomes are comprised of bi-layers.

Researchers have found that water-absorbing layers seem to interact with only tissues with water-based membranes. Meanwhile, water-resisting layers will not interact with water-based membranes at all. Instead these layers engage chemically with “hydrophbic” substances.

Liposomes may be the ideal method for transporting active ingredients that both are and aren’t water-soluble. This means manufacturers can use more complex mixtures of pure compounds for enhanced efficacy.⁸

The liposomal delivery system has a wide range of varying uses – many of which are still yet to be discovered. In fact, the nutritional industry use of liposomal technology is expected to grow rapidly in the next 5 to 10-years.

Doxil®

A chemotherapy medication used to treat cancer.

LipoDox®

Used to treat breast cancer, bladder cancer, Kaposi’s sarcoma, lymphoma, and acute lymphocytic leukemia.

Myocet®

A medication used for treating women with breast cancer that has spread to other parts of the body.

ThermoDox®

Primarily treats liver cancer and recurrent breast cancer.

As more and more research is done on liposomal and the benefits, we’re seeing a variety of products hitting the shelves.

One of the largest-growing markets for liposomes is within the supplement niche. Dietary supplements often contain nutrients like essential vitamins, minerals, amino acids, and other plant extracts that can be volatile to stomach acid. With the ability to by-pass stomach acid intact, dietary supplements can be absorbed directly in the small intestines – where the benefits are highest.

This allows a manufacturer to use higher-quality raw products at smaller doses while maintaining maximum efficacy. The structure of active ingredients can be much more complex than with traditional drug delivery systems (DDS).

You’re likely to see an uptick in health supplements that use liposomal delivery in the near future. The current drugs containing liposomes are just the tip of the iceberg for the health industry.

Liposomes are the ideal companion for dietary supplements. Manufacturers can utilize more natural ingredients that are known to be volatile once introduced into the body’s system. Because liposomes have a protective layer, these pure ingredients can get to where they’ll be most effective without prematurely breaking down.

Vitamin C

A uniquely beneficial vitamin that helps maintain healthy skin cells, blood vessels, bones, and cartilage.

Magnesium

A powerful chemical element that is beneficial for protein synthesis.

Glutathione

A substance made from amino acids that’s essential for tissue building and repair.

Curcumin

A therapeutic compound derived from turmeric known for anti-inflammatory properties.

NAD+

An essential anti-aging coenzyme affecting cellular function.

Liposomal technology can improve the body’s ability to absorb a wide range of nutrients. In fact, manufacturers are able to create more complex formulas thanks to liposomes and their ability to contain both water-soluble and water-resistant ingredients.

Liposomal delivery allows for more effective formulas. Complex botanical mixtures can be made using various raw compounds without risk of them being prematurely absorbed and thus destroyed before the body can reap the benefits.

Liposomal technology is at the forefront of drug delivery. There are a plethora of parameters that make a liposome-based formula more effective. Let’s take a look.

We know that liposomes are able to encapsulate an active ingredient for transport throughout the body. These nourishing marvels are enhanced with liposomal technology that allows them to travel with ease across cell membranes that traditional DDS wouldn’t be able to pass through.

The stomach can be a harsh environment for active ingredients in traditional pills. Nutrients can prematurely be broken down and destroyed by harmful acids before they’re put to good use. For maximum absorbency, those nutrients will need to make it all the way to your small intestines unscathed. That’s where liposomal delivery comes in.

Think of liposomes as a suit of armor designed to surround and protect active ingredients as they make their way to where they’ll be best absorbed – your small intestines. Nutrients get to where they’re supposed to go without breaking down in the mouth or stomach. Thus active ingredients are better utilized within the body.

Liposomes are biocompatible, biodegradable, non-toxic, and non-immunogenic carriers. Compared with traditional drug delivery systems, liposomes have been shown to exhibit better properties, including; site-targeting, sustained or controlled release, protection of drugs from degradation and clearance, superior therapeutic effects, and lower toxic side effects.

While more market research needs to be done surrounding individual products, there are over 20 medicines currently on the market using liposomal delivery. These medicines have been shown to be safe and effective by regulatory agencies such as the United States Food and Drug Administration.

Many of the drugs that utilize liposomal delivery have a shortened, unprotected lifespan when delivered without such liposomal protection. Due to the drug’s rapid uptake in the reticuloendothelial system (RES), they’re often limited in what they can accomplish without extremely high dosages. With liposomal delivery, a drug’s half-life is significantly improved – making an ineffective drug more productive.

In fact, liposomes have been clinically shown to significantly prolong circulation times.7 This allows manufacturers to offer a broader range of therapeutic applications that were not possible prior to liposomal drug delivery.

Liposomal delivery allows for advanced release methods other drug delivery systems can’t. Because liposomal allows for complex combinations of active ingredients, manufacturers are able to maximize formulas to suit almost any need.

Let’s say there are two active ingredients known to have anti-aging benefits. One is water-soluble, while the other is water-resistant.

Normally, a manufacturer would need to explore methods that would make a poorly soluble ingredient absorbable and therefore usable, along with the water-resistant one(s).11 With liposomal technology that problem is all but eliminated. Pure ingredients can be delivered intact, for maximum efficacy, without the need to improve their oral bioavailability.

There’s a lot of questions surrounding liposome delivery. Intense research on the technology continues to this day – with greater and greater advancements. Here, we’ll break down some of the touch questions surrounding liposomes and they’re delivery system – liposomal.