Liposomes

“Liposomes are small ball-like structures that are used to encapsulate active content, in the case of CannAMP, palmitoylethanolamide. Their cores are filled with water, while their membranes consist of phospholipids, which can hold fat-soluble molecules.” “Liposomes are very small bubbles which have a membrane consisted of the same phospholipid bilayer that the cell membrane is consisted of.”
“lipo = fat: soma = body so a minute spherical sac of phospholipid molecules enclosing a water droplet”

 
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Liposomes consist of the same material as what makes up our cells, phospholipids, with hydrophobic (water fearing) tail and hydrophilic (water loving) heads. Hydrophobic tails align in lipid bilayer to escape from aqueous environment, so hydrophilic heads point outward. Edges still exposed to aqueous environment so folds into sphere to form 3D liposome.
“Phospholipids are consisted of a head and two tails. The heads are hydrophilic, which means that they turn towards water, while the two tails are hydrophobic, which means they turn away from water. If two phospholipids are connected within an aqueous environment, due to this relationship of their parts with water, they will position themselves in a way that their tails are connected (facing inwards to each other), while their heads face outwards, towards the water environment. When this phospholipid bilayer is formed into a spherical structure like a ball (the bubble we mentioned) it has an aqueous core which can carry drugs or vitamins which are water soluble – hydrophilic – and the middle of its membrane (the part with phospholipid tails) can carry drugs and vitamins which are fat soluble – hydrophobic.”

 
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“Liposomes are small balls with a membrane that is made of phospholipid bilayers. These phospholipids consist of one head that seeks to be in touch with water and two tails which always turn towards a fatty environment. When two layers of these phospholipids are put together in an aqueous environment, their tails turn towards each other, leaving the heads of the two layers in touch with water. When this bilayer sheet is formed into a ball, the core of the ball is filled with water and the membrane consists of lipophilic tails, which means that liposomes can carry both hydrophilic and lipophilic content.”

 

How liposomes work

Due to their dual nature, can encapsulate water and fat soluble ingredients, water-soluble in cavity and fat soluble in membrane. CannAMP’s active ingredient, is fat soluble, so in membrane
A liposome approaches a cell. The liposome closes in. The liposome has attached itself to the cell and is releasing the active ingredients.
Versatility (can have water or fat soluble drugs) – So active in aqueous cavity (water soluble, hydrophilic active) or lipid bilayer (fat soluble or lipophilic active) (or even both)

 
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The benefits of liposomes

Problems with conventional drug delivery. Issues with conventional drug delivery: Limitations associated with oral dosage forms (Unsuitable in patients who are uncooperative, strictly “nil by mouth”, are vomiting profusely or have ileus), most nutrients excreted and slow and unpredictable absorption. Stomach acid breaks down the active and very little of it is absorbed. Liposomal drug delivery addresses these and more.

Main advantages

The mechanism behind liposomes offers several benefits. First of all, there is the protection of the active content (drugs, supplements, vitamins…). Most of any active content taken orally gets digested in the stomach and intestines, or destroyed by enzymes before it actually reaches the cells where it is needed. Not with liposomes! The phospholipid membrane of the liposomes is the same as the cell membrane, so all the things that cannot penetrate the cells also fail to damage the active content inside the liposome. This means that, under perfect conditions, the active content is protected and virtually all of it gets exactly where it is needed. Having in mind the price difference and wastage of the active content during non-liposomal oral use, liposomal use can actually prove to be more price-efficient, as well as more beneficial. Liposomal vitamin C is a very good example. Bioavailability of vitamin C is not great and much of it gets wasted, but we all know how beneficial vitamin C is. Making use of liposomal vitamin C is the solution. “This phospholipid membrane is the main reason behind the benefits of the liposomal delivery system. Its most important feature is the fact that is consisted of the same material as the cell membrane. The same way that enzymes do not degrade cells in the body, they do not degrade the CannAMP inside a liposome. This means that CannAMP is protected from the stomach acids and enzymes and not degraded before it reaches cells. “Before that, let’s see how liposomes protect CannAMP from the enzymes. It is thanks to the phospholipid membrane. It is actually the same as our cell membranes, so it protects the inside of the liposome efficiently.” Secondly, by choosing different sizes and lamellarities of liposomes, manufacturers can customize the delivery routes and the time of the release.

Another huge advantage of liposomes is the fact that the cell membrane and the liposome membrane are consisted of the same phospholipid bilayer. This biocompatibility makes the targeted cells readily available to accept the active content inside the liposome. When a liposome reaches a cell, its membrane integrates itself into the cell membrane and its content is released inside the cell. This way, the last obstacle in the voyage of the active content to the interior of the cell is surmounted.” Lastly, because the cell and liposome membranes are biocompatible and because the heads of phospholipids tend to keep together and the tails do the same, cell membranes openly accept liposomes, fusing with their membranes to let the active content inside. The result of this delivery system is an incredible increase in bioavailability because CannAMP is not degraded before it reaches the cells and it is entirely released into the cell thanks to the biocompatibility of cell and liposome membranes.” “Lastly, the fact that the liposome membrane is made of the same phospholipid bilayer that the cell membrane is made from means that there is no problem with membrane permeability. Due to this biocompatibility of membranes, phospholipids of the cell membranes literally open to take in the phospholipids of the liposome, effectively releasing the entire amount of active content into the cell.”

Further advantages

Benefits of liposomal delivery: Biocompatible, biodegradable, can encapsulate water and fat soluble ingredients, improved pharmacokinetic effects, increase in efficacy, multiple administration routes (oral, sublingual and intravenous), non-immunogenic, protects ingredient from digestive enzymes, reduced dosage, reduced toxicity, sustained ingredient release and targeted delivery. More benefits: cutting edge delivery system, natural composition (readily absorbed by body), can incorporate and release both water soluble and fat soluble components, controlled pharmacokinetics, enhanced activity (shield active from stomach acids) and decreased toxicity (targeted release). Even more benefits: “Protect active from stomach acid, increased bioavailability, enable timed release, targeted delivery, improved absorption (because of the biocompatibility of cell and liposome membranes) and Successfully crosses the blood-brain barrier” (Stability, Bioavailability, Targeted release) “Multiple administration routes (oral, sublingual and intravenous), Protects active from degradation, Increased efficacy (increases bioavailability), Targeted delivery, Carries both fat and water soluble actives (tunable), Reduced dosage, Lower toxicity, Bio-degradable, bio-compatible and non-immunogenic” Secondly, many drugs that we use to treat one condition are detrimental to our body. Side effects from many drugs are all too common and especially so for drugs used to deal with pain and inflammation. However, liposomes do not only protect the active content from the outside perils; they also protect other cells and tissues from the detrimental effects of any damaging active content. The active content gets delivered exactly where needed and it does not damage anything else on the way. For example, many drugs damage stomach and intestines before they are released into the bloodstream. Liposomes encapsulate the drugs and do not let them exert any of the negative effects.

“The liposomal delivery is the way to get intravenous absorption and efficacy, but without having to endure the invasive procedure. It makes it effortless for prolonged use. Thirdly, liposomes can vary in sizes. Making use of different sizes means that they can reach different places and use different routes to get there. There is no need to explain why this is beneficial, but many people don’t actually know how important this is for cancer patients. Namely, it is usually very difficult to distinguish which cells are tumor and which are healthy ones. This is why many cancer treatments are very bad for the healthy cells. However, tumor cells have a noticeably higher permeability and retention when compared to normal cells. This means that using larger liposomes prevents the active content from entering healthy cells, but allows it into the ones affected by tumor. This is known as passive targeting and it is a huge benefit of liposomes for cancer treatment.