DEFENDER – Liposomal CaAKG, Berberine, HLA Capsules
$49.95
Defender is a unique combination of supplements formulated to reduce systemic inflammation to minimize NAD⁺ consumption, prevent cellular senescence, slow the rate of age-related DNA methylation, and increasing levels of NAMPT which is responsible for the conversion of nicotinamide to NAD.⁺
Each Capsule Contains ▸110 mg Liposomal CaAKG ▸60 mg Liposomal Berberine ▸60 mg Liposomal Hyaluronic Acid (HLA)
About Defender
Defender is a unique combination of supplements formulated to reduce systemic inflammation. Decreasing systemic inflammation will minimize NAD⁺ consumption so that it’s available for other purposes.
Liposomal Berberine, CaAKG, and HLA work together to help prevent cellular senescence and slow the rate of age-related DNA methylation, which may help to prevent some of the many “diseases of old age”.
Defender may also elevate levels of NAD⁺ by increasing an important enzyme responsible for the conversion of nicotinamide to NAD,⁺ called NAMPT.
Berberine Found to Increase NAD⁺ Levels, Lower Inflammation
In a study examining the effects of Berberine on NAD⁺ levels, it was found that Berberine increases an important enzyme responsible for the conversion of nicotinamide to NAD,⁺ called NAMPT.
“Berberine increases NAD+/NADH ratio through induction of NAMPT expression in C2C12 cells.” (1)
Berberine Induces Autophagy
As you age, you accumulate senescent cells that secrete toxins which are inflammatory. Berberine is one of the most promising interventions to slow the accumulation of senescent cells and the inflammation they secrete by inducing autophagy, the body’s way of clearing out dead and damaged cells to make way for new ones.
“Mechanistic studies exhibit that berberine induces autophagic death in ALL cells by inactivating AKT/mTORC1 signaling.” (2)
It has also been shown to increase NAD⁺ levels through its activation of the AMPK enzyme.
“Berberine has been shown to enhance AMPK activation (one of the few chemicals that does), enhance autophagy and mitigate apoptosis (cell death) induced by high glucose levels.” (3)
CaAKG Slows Effects of Aging and Reduces Inflammation
CaAKG works by slowing the rate of age-related DNA methylation and reducing the inflammation caused by senescent cells: two proposed reasons why we age.
“AKG suppresses chronic inflammation and induces secretion of IL-10 in T cells of female mice.” (4)
CaAKG also contributes to metabolism, providing energy for cellular processes. It helps stimulate collagen and protein synthesis and influences age-related processes including stem cell proliferation.
HLA Promotes New Cell Growth and Reduces Inflammation
Hyaluronic acid (HLA) is important for promoting the growth of new cells and tissues in the joint’s cartilage and bone, which thereby may reduce joint inflammation caused by injuries or tissue degeneration.
“The studies reviewed here show promising results for the use of HA in the treatment of inflammatory pathologies.” (5)
About Liposomal Delivery
Our process encapsulates and delivers our products intracellularly in its complete form where it can be absorbed and utilized rather than being destroyed in the stomach. Learn More About Improved Bioavailability with Liposomes.
Powdered Liposome under Electron Microscope
Testing
About Liposomes
Liposomes protect ingredients through the GI tract, merging their contents into cells to improve the biodistribution of compounds.
Liposomes Demonstration
Why Liposomes
Bioavailability Issues
Solves the Bioavailibility Problem
Targeted Delivery
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 bioavailability. The higher the bioavailability of an active substance, the more effect it has on the body. 3
Advanced Absorption
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. A synthesis takes place which allows vitamins, minerals or micronutrients to be transported more easily. This higher absorption, means greater efficacy and with smaller doses needed to achieve better results. 4Biocompatibility
Phospholipids, which are found throughout the body in the membranes of body cells, are so naturally-occurring, that the body recognizes these as body-compatible and does not treat them as ‘toxic’ or ‘foreign’—and, so, does not mount an immune attack on the liposome. 5Masking
Liposomes shield nutrients from detection by the body’s immune system, mimicking biological membranes and giving the active ingredients more time to reach their intended destination. Phospholipids mask the active ingredients so that larger amounts can be absorbed and escape the selective function of the small intestine. Osmotic (hydrophilic) side effects of some high-dose vitamins and minerals can thus be reduced. 6Crosses the Blood Brain Barrier
Liposomes have demonstrated the ability to cross this barrier, giving the liposomes the ability to deposit the supplement directly into the cells and enhance circulation of nutrients by your lymphatic system. 7Nanoscale Power
This profound effect of liposome size on complement recognition can also affect liver uptake. Generally, large unmodified liposomes are eliminated more rapidly than small liposomes, which is why our Fluidizing Liposomes™ are very small—less than 100 nm to prevent their uptake by macrophages of the liver and the spleen. 8What are Liposomes made of?
What does phosphatidylcholine do?
Phosphatidylcholine is required for many vital functions in the cardiovascular, reproductive, immune, and nervous systems. PC and its components are needed for the synthesis of important messenger molecules called prostaglandins which, among other functions, regulate the contraction and relaxation of muscles. Choline is required for the synthesis of intracellular messenger molecules including the neurotransmitters that allow nerve cells to communicate with muscles and each other, and are essential for proper heart and brain function. At birth up to 90% of cellular membranes are made up of PC. As you age, the percentage of PC in your cellular membranes can decrease to about 10%. This fact leads many to recommend consistent supplementation with this essential phospholipid. 10
How do Liposomes work?
Liposomes release bioactive nutrients by membrane fusion. They delay the clearance and increase the intravascular circulation time of encapsulated nutrients and prolonging retention time. At the first stage of liposome-cell interaction, liposomes adhere to the cell surface. Following such binding, the liposome is internalized into the cell by the mechanism of endocytosis (or phagocytosis). This is followed by the enzymatic digestion of the liposome in the intracellular compartment, accompanied by the intracellular distribution. The active nutrient encapsulated in the liposome is protected from metabolism and the molecule becomes active only after release from liposome. These encapsulating phospholipids bond with cell membranes to facilitate intracellular delivery. They are successful in this because they are able to bypass the digestive processes that normally degrade foreign substances. Liposomes ensure safe delivery of encapsulated cargo retain it in tissues and cells.References
1. Potential of Liposomes for Enhancement of Oral Drug Absorption 2. Nanocarriers for oral drug delivery 3. Composition design and medical application of liposomes 4. Liposomal Delivery Systems: Design Optimization and Current Applications 5. Oral Bioavailability: Issues and Solutions via Nanoformulations 6. Spontaneous In Situ Formation of Liposomes from Inert Porous Microparticles for Oral Drug Delivery 7. Stabilization of liposomes during drying 8. Powdered lipid nano and microparticles: production and applications. Lipid nanoparticles as vehicles for macromolecules: nucleic acids and peptides 9. Scalable solvent-free production of liposomes 10. Membrane lipids: where they are and how they behave
Key Advantages of Liposomal Delivery:
- Protects against the harsh environment of the GI tract and increases transmucosal (oral) uptake and absorption.
- Optimizes both hydrophilic and hydrophobic, unstable compounds.
- 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.
- Offers higher bioavailability and absorption compared to conventional capsules.
- Increases increase peak plasma concentration.
Liposome Research
RESEARCH ON LIPOSOMES FOR INCREASED BIOAVAILABILITY
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
WATER SOLUBILITY
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.
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.
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 B12sublingual 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.
Read moreLiposomal 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.
Read moreLiposomal Curcumin & Resveratrol Capsules 10-20x More Bioavailable in Circulation and Prostate Tissue vs Standard Capsules
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 to12 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.
Read more
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.
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
Read More
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."
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."
