What is a liposome?Liposomes are vesicles comprised of phospholipid molecules – the same molecules that comprise cell membranes. The phospholipid molecule consists of a hydrophilic phosphate head and two hydrophobic fatty acid tails. These features enable liposomes to be the carriers of hydrophobic and hydrophilic compounds. Due to low absorption and bioavailability rates of traditional oral dietary capsules, the encapsulation of hydrophilic and hydrophobic nutrients within liposomes allows the active ingredient to bypass the destructive elements of the gastric system. To release the protected molecules to a site of action, the lipid bilayer fuses with other bilayers such as the cell membrane, delivering the liposome contents directly into the cells and tissues intact.
What is phosphatidylcholine?One of the most important and prominent phospholipids in cell membranes is called phosphatidylcholine (PC) [pronounced FOSS-fah-tide-al-KOH-lean]. 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.
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.
Increases BioavailabilityLiposomes release drug molecules by membrane fusion. They delay the clearance and increase the intravascular circulation time of encapsulated drugs, decreasing digestion of liposomes by macrophages in the reticulo-endothelial system (RES), and enhancing the retention of drugs. The drug encapsulated in the liposome is protected from metabolism and the drug molecule becomes active only after release from liposome (r). 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.
Crosses the Blood Brain BarrierHave you ever heard of the blood-brain barrier? This is a filtering mechanism in our circulation system that allows blood to be carried to the brain but blocks numerous other substances from passing through. Nanoliposomes 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.
Research on Lipsomes for increased bioavailabilityLiposomes protect products from digestion in the GI tract, but that is only the first step. The improved bioavailability varies greatly, depending on the molecule itself and the quality of the liposome. 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. Liposome Stability. Liposomes need modification to increase stability so they do not break apart and release their payload when exposed to the GI tract and bloodstream. Recent advances in Liposomal technology enables skilled manufacturers to adjust the stability so the payload is protected for several hours. Different manufacturing techniques result in significant variation in stability and bioavailability. Liposome size. As noted above, size of the liposome is crucial. Larger Lipsomes are quickly filtered out by the liver and other parts of the RES. Smaller liposomes (below 50 nanometers) can circulate much longer. The study on B-12 below shows the larger size liposome formula increased bioavailability of 3xvs 5x for the smaller sized liposomal formula.
Liposomal Fisetin 1.6 to 27x more bioavailableThis 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.(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) Liposome1000ug - 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 exhibitedsustained release with more than 5x increased bioavailability over standard tablets. Read more
- (i)Nanocelle 1000ug -28% - A nano liposomal formulation of B12sublingual spray with an average particle size of about 20 nm
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. Read more
Liposomal Curcumin & Resveratrol capsules 10-20x more bioavailable in circulation and prostate tissue vs standard capsulesLiposome 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 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 co 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