Learn More About Liposomal Delivery
Liposomes, vesicles enclosed by phospholipid bilayers, can solubilize water-insoluble drugs into the lipid domain of the liposomal membrane. In addition to their solubilizing capacity and biocompatibility, the structural and compositional similarity of liposomes with bio-membranes has also encouraged their application for non-invasive oral delivery of poorly-permeable nutrients. 2 Liposomes are non-toxic, biocompatible, biodegradable, and have the following advantages as carriers in drug delivery: first, liposomes can reduce toxicity; second, hydrophilic and lipophilic agents can be incorporated into liposomes; third, liposomes control the drug release; and fourth, the liposome delivery system increases bioavailability. 3 Molecules with very poor water solubility usually have the worst bioavailability and can benefit the most from liposomal delivery. Fisetin is one example shown below up to 27x more bioavailable. 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. 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. 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. 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. 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. 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. 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. 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. 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 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." 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 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."RESEARCH ON LIPOSOMES FOR INCREASED BIOAVAILABILITY
WATER SOLUBILITY
Study Shows Liposomal Green Tea Extract 12x More Bioavailable Than Regular Green Tea
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
Liposomal Vitamin B-12 Formulas 3-5x More Bioavailable Than Tablet.
Liposomal Berberine Increases Circulation Time 23-46x
Liposomal Curcumin & Resveratrol Capsules 10-20x More Bioavailable in Circulation and Prostate Tissue vs Standard Capsules
Liposomal Glutathione More Effective
Liposome Encapsulated Glutathione Elevates Body Stores
Enhanced Efficacy of Apigenin Liposomes
Liposomal Quercetin:Prolonged Circulation Time in Vivo
Liposomal Nanoparticles Improve the Solubility and Bioavailability of Quercetin in Liver
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 "Liposomes are valued for their biological and technological advantages, and are considered to be the most successful drug-carrier systems known to date." 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. 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.
LIPOSOMAL DELIVERY PROTECTS INGREDIENTS
Liposomes protect ingredients through the GI tract, merging their contents into cells to improve the biodistribution of compounds.
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
HOW LIPOSOMES WORK
A liposome is made up of a spherical vesicle with the inner contents containing the active ingredients, which are protected by an outer layer comprised of tiny fat-like particles, called the phospholipid layer.
BIOCOMPATIBILITY & SAFETY
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)
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
OUR ENCAPSULATION PROCESS
Our LIPO Caps™ powdered liposomes technology encapsulates 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. Our peak particle size is less than 50 nm (nanometers).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.
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.
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.
Our peak particle size is less than 50 nm (nanometers). 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 20-40 nanometers in size, and 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
