Learn More About Liposomal Delivery

About Liposomal Delivery
liposome research
The Liposome Advantage
THE BENEFITS OF LIPOSOMES
About Our LIPOSOMAL CAPSULES
About Our Lipo Gel Products
Real Image of a Liposome

Liposomes are a revolutionary way of encapsulating active ingredients in a phospholipid “bubble” to protect and deliver them directly to the cells of your tissues, which are reached via the bloodstream.⑴ This allows for the ingredients to be absorbed and utilized rather than being destroyed in the stomach.

The aim of taking any supplement is to ensure its transport into the bloodstream. However, due to the low absorption and bioavailability rates of traditional oral capsules, active ingredients lose most of their potency while passing through the gastrointestinal tract or are simply not absorbed in the small intestine at all. The majority is excreted unused via the intestines or kidneys. ⑵

Liposomal delivery offers a targeted and complete absorption of active ingredients with a delayed‑release effect, unlike all other nutrient delivery methods. This increased circulation time of key nutrients in the bloodstream significantly improves bioavailability. The higher the bioavailability of an active substance, the more effect it has on the body.

RESEARCH ON LIPOSOMES FOR INCREASED BIOAVAILABILITY

With our Liposomal products, approximately 90% of the payload reaches the bloodstream intact, regardless of what the payload is.

For example, with our Liposomal Green Tea Extract around 90% of the EGCG reaches the bloodstream.

With regular Green Tea extract, around 9% of EGCG reaches the bloodstream.

Hence the study below shows it is about 10x more bioavailable.

Regular Apigenin is around 30% bioavailable, so you can expect our Liposomal Apigenin to be approximately 3x more bioavailable than regular Apigenin.

Although we don't have research on bioavailability of all our Liposomal products, below we show research that demonstrates increased bioavailability of 3 to 40x when using liposomes in some of the most popular supplements we produce.

Liposomal Green Tea Extract 10x More Bioavailable

(This is the product we use in our Lipo Green Tea)

A study was conducted at the North-West University in South Africa, assessing the bioavailability of the green tea extract used in the production of Origine 8™ compared to a standard commercially available extract of green tea commonly found in green tea supplements.

Origine 8™ delivered an average concentration of catechins of 11,630 ng/ml compared to a concentration of 930 ng/ml delivered by the standard green tea extract. A 12 fold greater average concentration was delivered by Origine 8™.

Origine 8™ offered complete absorption of all 8 catechin found in green tea. With the exception of EGCG standard green tea extract provided insignificant levels of the other 7 catechin in comparison to Origine 8™ as demonstrated in figure 1 .

The average concentration of Epigallocatechin Gallate (EGCG) delivered by Origine 8™ was 6120 ng/ml compared to an average concentration of 612 ng/mlEGCG delivered by the standard green tea extract. EGCG is regarded as a key catechin and Origine 8™ delivers a 10 fold greater total concentration.

Origine 8™ resulted in a far greater half-life compared to the standard green tea extract.
Catechins delivered by Origine 8™ were still found to be present in the plasma after 24 hours whereas standard green tea was cleared from the body after only 6 hours. This means that Origine 8™ could be used as a once per day dose whilst standard green tea would require multiple doses of far greater size throughout the day to deliver the same levels of catechins achieved through a single dose of a far smaller size of Origine 8 TM.

Liposomal Fisetin 1.6 to 27x More Bioavailable

This study in mice found a 2.7-fold increase (in Cmax) with Liposomal Fisetin, with a dose 10 times lower than that of the free fisetin when given by IP.

With IV, the Cmax of liposomal fisetin was 10, vs 6 for free fisetin.

Liposomal Vitamin B-12 Formulas 3-5x More Bioavailable Than Tablet.

Route and Type of Formulation Administered Influences the Absorption and Disposition of Vitamin B₁₂ Levels in Serum

This study compared five formulations for bioavailabilty in humans over 6 hours.A standard table (iii) was compared against an emulsion (ii), a chewabletablet (iv), an oral spray comprised of larger liposomes (v) and an oral spray comprised of very small (20 nanometer) liposomes.

(i) Nanocelle 1000ug -28% - A nano liposomal formulation of B₁₂ sublingual spray with an average particle size of about 20 nm
(ii) Emulsion 1000ug - 10% -An emulsion formulation of B₁₂ sublingual
(iii) Tablet 1000ug - 5% - A standard tablet formulation of B₁₂ that is absorbed through the gastrointestinal tract.
(iv) Chewable 5000ug - 27% - A dissolvabletablet of B₁₂ that is absorbed through the sublingual mucosa
(v) Liposome 1000ug - 14% - A liposome oral spray of B₁₂ with particle sizes of approximately 100 nm.

The chewable showed similar increase as nano liposomal, but a 5x higher dosage was used. The standard liposomal product was 3x more bioavailable than tablet.

The nano liposomal spray exhibited sustained release with more than 5x increased bioavailability over standard tablets.

Liposomal Berberine Increases Circulation Time 23-46x

Preparation, Pharmacokinetics and Tumour-Suppressive Activity of Berberine Liposomes (Zheng, 2017)

Administration of standard Liposomal Berberine increased retention time in circulation from .42 to 10 hours. Use of PEG modified Liposomes further increased retention to to 14 hours.

Administration of Berberine solution injection is hindered by unsatisfactory pharmacokinetics and, more importantly, the risk of lethal cardiovascular adverse reactions due to rapid uptake into heart and lung. This study validated common and long-circulating liposomes as safe and effective method for sustained release of Berberine.

Liposomal Curcumin & Resveratrol Capsules 10-20x More Bioavailable in Circulation and Prostate Tissue vs Standard Capsules

Liposome encapsulation of curcumin and resveratrol in combination reduces prostate incidence in PTEN knockout mice.

Liposome capsules of resveratrol and curcumin may inhibit prostate problems by increasing their bioavailability synergistically.

In this study, we determined the bioavailability of liposome encapsulated curcumin and resveratrol, individually and in combination and evaluated the inhibitory effects of these agents against prostate growth and progression.

Serum and prostate tissue samples harvested at different time points of 30 min to 12 hr with plain liposome (0.1%), curcumin (50 mg/kg/bw), lipo-curcumin (50 mg/kg/bw), lipo-resveratrol (50 mg/kg/bw) and lipo-curcumin administered with lipo-resveratrol (25 mg/kg/bw for each).

figure a - Levels of curcumin and resveratrol recorded in the serum.

figure b - Levels of curcumin and resveratrol recorded in the prostate.

figure d - Quantification of tumor growth inhibition. Total number of adenocarcinomas observed under 10 high-power fields of control vs. treatment groups.

Liposomal Glutathione More Effective

Clinical research aiming to improve glutathione concentration requires sufficient glutathione absorption and delivery.Researchers turn to liposomal glutathione to achieve sustained bioavailability.

Results from two recent studies showed that liposomal nanoformulation absorption is more effective for raising blood glutathione levels in humans than non-liposomal glutathione. ¹

Both studies report a very rapid decline in bioavailability of non-liposome-encapsulated glutathione compared to liposomal glutathione.

Liposome Encapsulated Glutathione Elevates Body Stores

The results of a recent study demonstrated increased body stores of Glutathione (GSH) after oral administration of Liposomal GSH humans. ²

Since GSH is subject to destruction in the acid environment of the stomach, researchers tested that oral liposomal GSH might be an effective means of GSH delivery in vivo.

In addition, liposomal GSH had positive effects on several GSH-related parameters including decreases in biomarkers of oxidative stress and enhancements in immune functions.

Finally, liposomal GSH was highly tolerated and its administration was not associated with any signs of adverse effects. ³

The results from this study provide support for the potential use of oral liposomal Glutathione as an intervention strategy for enhancing tissue Glutathione levels for use in disease therapy or prevention.

Liposomal Glutathione effects were often greater that previously observed for non-liposomal Glutathione . ⁴

Enhanced Efficacy of Apigenin Liposomes

A recent study focusing on establishing apigenin as a potential chemotherapeutic agent for alleviating colorectal cancer reports the development of a stable liposomal nanocarrier with high encapsulation of the hydrophobic flavone apigenin for enhanced chemotherapeutic effects.

"Apigenin liposomes bypass the hurdles posed by apigenin as a chemotherapeutic due to its high hydrophobicity. The enhanced pharmacological activity of apigenin has been assigned to its ability to interact and subsequently influence membrane properties which also resulted in optimal yield of a stable, rigidified, non-leaky nano-carrier with ideal release kinetics."

Research demonstrates the chemo-preventive properties of apigenin against colorectal cancer and the enhanced efficacy of its liposomal formulation both at the in vitro and in vivo level.

Liposomal Quercetin: Prolonged Circulation Time in Vivo

New research using Quercetin liposomes demonstrates higher quercetin concentrations in plasma than non-encapsulated quercetin and prolonged circulations time in the blood.

"The effect of quercetin liposomes was stronger than quercetin alone. This formulation provides characteristics such as high drug encapsulation ratio, low in vitro release rate and slow drug clearance and prolonged circulation time in vivo. This provides an alternative solubilization vehicle for administration of quercetin."

Liposomal Nanoparticles Improve the Solubility and Bioavailability of Quercetin in Liver

Liposomal nanoparticles may improve the solubility and bioavailability of quercetin in liver. A 2020 study on the protective and therapeutic effects of nanoliposomal quercetin found liposomal quercetin could effectively protect rats against acute liver injury and may be a new hepatoprotective and therapeutic agent for patients with liver diseases.

Fig. 1:Effect of nanoliposomal quercetin on histopathological changes in rat liver tissues. (Scale bar: 50 μm; HE staining). a Normal control; b-d hepatic-injured rats with b saline treatment; c quercetin treatment; and d nanoliposomal quercetin treatment.

"Interestingly, nanoliposomal quercetin was more effective on decreasing liver index and interstitial inflammatory infiltration of hepatic-injured rats than pure quercetin, which indicated that the protective effect of nanoliposomal quercetin in the injured liver was stronger than that of pure quercetin."

"Liposomes are valued for their biological and technological advantages, and are considered to be the most successful drug-carrier systems known to date." - International Journal of Nanomedicine, Liposomes As Nanomedical Devices

Depending on the molecule, with Liposomes 90% of the ingredients can typically make it to the bloodstream.

Many common supplements are digested by enzymes and bacteria in the stomach. If they make it past the intestines to the liver, they are seen as a foriegn body and are mostly filtered out.

Studies show nearly all NAD+ boosters do not escape the liver at all, but are converted to NAM which is released into the bloodstream.

Liposomes protect ingredients from digestion. As they are composed of phospholipds that are very similar to the membrane of every cell in our body, they are seen as native and are not filtered out by the liver, which released them intact into the bloodstream where they dissolve after a few hours and release the payload where it can be taken up by cells.

Liposomes protect ingredients through the GI tract, merging their contents into cells to improve the biodistribution of compounds.

LIPOSOMES DEMONSTRATION

WHY LIPOSOMES

BIOAVAILABILITY ISSUES

"Liposomes are valued for their biological and technological advantages, and are considered to be the most successful drug-carrier systems known to date."

International Journal of Nanomedicine

Depending on the molecule, with Liposomes 90% of the ingredients can typically make it to the bloodstream.

Many common supplements are digested by enzymes and bacteria in the stomach. If they make it past the intestines to the liver, they are seen as a foriegn body and are mostly filtered out.

Studies show nearly all NAD+ boosters do not escape the liver at all, but are converted to NAM which is released into the bloodstream.

Liposomes protect ingredients from digestion. As they are composed of phospholipds that are very similar to the membrane of every cell in our body, they are seen as native and are not filtered out by the liver, which released them intact into the bloodstream where they dissolve after a few hours and release the payload where it can be taken up by cells.

Liposomes protect ingredients through the GI tract, merging their contents into cells to improve the biodistribution of compounds.

LIPOSOMES DEMONSTRATION

WHY LIPOSOMES

BIOAVAILABILITY ISSUES

The aim of taking any supplement is to ensure its transport into the bloodstream. However, due to the low absorption and bioavailability rates of traditional oral capsules, active ingredients lose most of their potency while passing through the gastrointestinal tract or are simply not absorbed in the small intestine at all. The majority is excreted unused via the intestines or kidneys. ⑵

Liposomal delivery offers targeted and complete absorption of active ingredients with a delayed‑release effect, unlike all other nutrient delivery methods.

This increased circulation time of key nutrients in the bloodstream greatly improves bioavailability.

Ingredients are absorbed & utilized rather than being destroyed in the stomach.

The higher the bioavailability of an active substance, the more effect it has on the body. ⑶

This means greater efficacy & smaller doses needed to achieve better results.

IT SOLVES THE BIOAVAILABILITY PROBLEM

The aim of taking any supplement is to ensure its transport into the bloodstream. However, due to the low absorption and bioavailability rates of traditional oral capsules, active ingredients lose most of their potency while passing through the gastrointestinal tract or are simply not absorbed in the small intestine at all. The majority is excreted unused via the intestines or kidneys. ⑵

Liposomal delivery offers targeted and complete absorption of active ingredients with a delayed‑release effect, unlike all other nutrient delivery methods.

This increased circulation time of key nutrients in the bloodstream greatly improves bioavailability.

Ingredients are absorbed & utilized rather than being destroyed in the stomach.

The higher the bioavailability of an active substance, the more effect it has on the body. ⑶

This means greater efficacy & smaller doses needed to achieve better results.

Liposomes are absorbed through the oral mucosal lining and through lymphatic mechanisms in the gut, bypassing first-pass metabolism and breakdown in the liver ensuring the retention of liposome integrity.

The phospholipids in the liposomes closely resemble the structure of your cell membranes, and as a result the body recognizes them as safe and friendly substances which are biocompatible.

Many nutraceutical supplements have been shown to cause problems in the liver at higher dosages. The risk of liver damage greatly limits the dosage that can safely be used, which diminishes the effectiveness. The liver does not filter out molecules delivered by liposomes, so the risk from toxicity is greatly diminished.

BIOCOMPATIBILITY & SAFETY

Liposomes are absorbed through the oral mucosal lining and through lymphatic mechanisms in the gut, bypassing first-pass metabolism and breakdown in the liver ensuring the retention of liposome integrity.

The phospholipids in the liposomes closely resemble the structure of your cell membranes, and as a result the body recognizes them as safe and friendly substances which are biocompatible.

Many nutraceutical supplements have been shown to cause problems in the liver at higher dosages. The risk of liver damage greatly limits the dosage that can safely be used, which diminishes the effectiveness. The liver does not filter out molecules delivered by liposomes, so the risk from toxicity is greatly diminished.

Liposomes were first discovered in 1965 and soon after were proposed as drug delivery systems. For the last five decades, advancements in this field have led to numerous clinical trials on liposomes for delivery of anti-fungal, antibiotic drugs, delivery of gene medicines, anesthetics and anti-inflammatory medications. This is an established technology, with a variety of types of liposomes being brought to market. (Source)

For the last five decades, advancements in this field have led to numerous clinical trials on liposomes for delivery of anti-fungal, antibiotic drugs, delivery of gene medicines, anesthetics and anti-inflammatory medications.

This is an established technology, with a variety of types of liposomes being brought to market. (Source)

Protects against the harsh environment of the GI tract and increases oral uptake and absorption
Provides superior stability of active ingredients, allowing for higher absorption and greater efficacy
Timing of the dose does not require accompaniment or exclusion of food as the absorption via the liposome avoids the digestive processes
Provides a larger nutrient payload per particle
The dose is slowly released so the supplement's concentration level can stay fairly constant in the body

KEY ADVANTAGES OF LIPOSOMAL DELIVERY

Protects against the harsh environment of the GI tract and increases oral uptake and absorption
Provides superior stability of active ingredients, allowing for higher absorption and greater efficacy
Timing of the dose does not require accompaniment or exclusion of food as the absorption via the liposome avoids the digestive processes
Provides a larger nutrient payload per particle
The dose is slowly released so the supplement's concentration level can stay fairly constant in the body

More Economical - Manufacturing liposomes does add cost to the finished product, however, a 2x increase in cost is vastly outweighed by the 5-20x or greater increase in effectiveness of liposomal delivery.

More Effective - Many popular supplements such as Curcumin, Resveratrol, Berberine, Apigenin, Quercetin and others are well documented to have extremely poor bioavailability. When you're taking a supplement that has 5% or less bioavailability, it is not possible to achieve high blood saturation levels safely. Liposomes deliver much higher quantities of the target molecules to the bloodstream.

Safer - Many nutraceutical supplements have been shown to cause problems in the liver at higher dosages. The risk of liver damage greatly limits the dosage that can safely be used, which diminishes the effectiveness.

The liver does not filter out molecules delivered by liposomes, so the risk from toxicity is greatly diminished. The phospholipids in the liposomes closely resemble the structure of your cell membranes, and as a result the body recognizes them as safe and friendly substances which are biocompatible.

Our LIPO Caps™ are used in our liposomal capsule products. The process involves encapsulating nanosized particles in liposomes, which are then freeze-dried to remove the aqueous phase. It’s a bit like grapes that are dehydrated to raisins, except that liposomes re-inflate in the body. This ensures maximum bioavailability and stability, protecting the ingredients against degradation.

This encapsulation technology is clinically proven through safety, absorption and blood glucose studies to maximize nutrient bioavailability. ^⑶

We use natural non-hydrogenated sunflower phosphatidylcholine in our manufacturing process, derived from non-GMO certified sunflower oil from Europe. It undergoes a multi-step, purification and filtration process during liposome manufacturing to ensure the utmost purity.

LIPO Gel products are ideal for people who have trouble swallowing pills and prefer a liquid gel. Just put two pumps under the tongue and let it absorb for 30-60 seconds before swallowing.

If swallowed, liposomes do protect the active ingredients from digestion in the stomach, but it is preferable to let the gel absorb under the tongue or elsewhere in the oral cavity as much as possible.

The liposomes are derived from non-GMO certified sunflower oil from Europe. It undergoes a multi-step, purification and filtration process during liposome manufacturing to ensure the utmost purity.

Powdered Liposome under Electron Microscope

Trans-Resveratrol Pure Powder

Berberine

Trans-Resveratrol

CardioMAX