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Page 1: $TQWIJV VQ [QW D[source-1-global.com/wp-content/uploads/docs/coq10/...CSWGQWU EQTG (CV UQNWDNG CEVKXG UWDUVCPEGU ECP QPN[ DG UQNWDKNK\GF YKVJKP VJG DK NC[GT OGODTCPG VJWU VJG NQCFKPI

Brought to you by

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IntroductionThe worldwide launch of the VESIsorb® delivery system represents a unique solution to improving

the absorption and bioavailabilty of poorly water soluble natural ingredients and bio-actives.

The patented VESIsorb® delivery system is a naturally self-assembling colloidal delivery system that

has been clinically proven to increase absorption of nutritional supplements, food and beverage, and

cosmetic ingredients.

We are delighted by the number of questions we have received from the medical community, We are delighted by the number of questions we have received from the medical community,

scientists, and health and wellness focused individuals worldwide. The more one learns about this

sophisticated colloidal droplet delivery system, the more intrigued they are by the simplicity and

effectiveness of this naturally self-assembling VESIsorb® technology. Consequently, we have

developed this “white paper” for those interested in gaining a deeper and clearer understanding of

why natural actives like CoQ10 Ubiquinone and Kaneka QH™ Ubiquinol, Omega-3 EPA/DHA,

Vitamin D-3, Curcumin, Citrus Polymethoxylated Flavones, Resveratrol, Tocotrienols, and more are

better absorbed when delivered in these patented VESIsorb® capsules, drinks, stick packs, gels, better absorbed when delivered in these patented VESIsorb® capsules, drinks, stick packs, gels,

and gummies.

We have used a FAQ (frequently asked questions) style which provides a simple and easy to follow

format.

Q: I have read where you suggest that the VESIsorb® system mimics the body’s natural digestion process. CoQsource®, for example, is “BODY READY” when taken orally. Can you explain what you mean?A: We use “natural” in describing the VESIsorb® technology because it mimics the human fat

digestion and absorption process. It is known that poor water soluble drugs, e.g. fat soluble

vitamins, are better absorbed when administered after a meal containing fat. One of the reasons for

the improved absorption is the enhanced drug solubilization by bile salt mixed micelles which are

formed from the digestion products of dietary triglycerides (monoglyceride and fatty acids) and bile -

a nanotechnology tool developed by Mother Nature. The task of naturally formed bile salt-mixed

micelles, having a size below 10 nanometers, is to transport the lipophilic molecules through the

aqueous environment of the GI-tract and across the unstirred water layer to the absorptive aqueous environment of the GI-tract and across the unstirred water layer to the absorptive

epithelium. Individual lipid molecules, and not the micelles per se, are the species that enter the

absorptive membrane.

The precise manner by which lipophilic molecules cross the membrane of the enterocytes is

uncertain. Until recently it was generally thought that lipids simply diffuse, individually as monomers

through the lipid bilayer of the membrane into the cell. Now there is evidence that dietary fatty acids

may be transported across the enterocyte membrane by a specific transporter.

Once inside the enterocyte, dietary fatty acids and monoglycerides diffuse to the smooth

endoplasmic reticulum, where they are resynthesized into triglycerides. Finally, the resynthesized

triglycerides packaged into chylomicrons which are secreted into lymph.

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It is very important to understand that nano-size micelles are produced naturally in our bodies each

and every day.

On the other hand, there are methods used in nanotechnology that are “top down” which simply

means they use energy and force to decrease the size to less than 100 nanometers. They use

high-pressure homogenizers or micro-fluidizers. They are, in some cases, fundamentally milling

down crystals from microns to much smaller nano-sized hard particles. This never happens in the

body, and it is far from a natural occurrence.

Q: VESIsorb® improves the absorption and bioavailability of natural Q: VESIsorb® improves the absorption and bioavailability of natural ingredients poorly absorbed by the body in three steps. Could you explain? A: VESIsorb®, a lipid-based formulation that naturally self-assembles on contact with an aqueous A: VESIsorb®, a lipid-based formulation that naturally self-assembles on contact with an aqueous

phase into a colloidal system (so called "association colloid"), mimics this mixed micellar absorption

pathway. The improvement of oral drug or natural bio-active bioavailability by this technology is

broken down into three steps: Step 1: Formation of the colloidal delivery system containing the drug,

Step 2: Diffusion of the colloidal system across the unstirred water layer, Step 3: Dissociation of

single molecules from the colloidal system and transfer to the absorption epithelium and passive

diffusion of single molecules across enterocyte membrane. Since VESIsorb® mimics the naturally

occurring mixed micellar transport system of the human body it can be considered as a safe occurring mixed micellar transport system of the human body it can be considered as a safe

technology to improve the absorption of poorly water soluble drugs.

Step 1Formation of the colloidal delivery system. When mixed with an aqueous system (such as the GI-lumen), this unique lipid-based formulation naturally forms a self-assembling colloidal delivery system container solubilized bioactives. A colloidal droplet is typically less than 100nm in diameter and consists of a monolayer with the CoQ10 or other bioactives within its oil core.

Step 2Diffusion of the solubilized bioactives across the unstirred water layer.

Step 3Step 3Transfer of the solubilized CoQ10 or other bioactives to the absorptive surface of the intestine.

Q: The difference between micelles, liposomes and VESIsorb® naturally self-assembling colloids is confusing. Can you explain the differences?

VESIsorb® vs. MicellesMicelles are composed of a surfactant or surfactant mixture and the active substance to be Micelles are composed of a surfactant or surfactant mixture and the active substance to be

solubilized within the center of the micelle. A micelle is like an aggregate of surfactant molecules

dispersed in a liquid solution. A surfactant molecule has a hydrophilic part - called “head” - and a

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hydrophobic part - called “tail”. A typical micelle in an aqueous solution forms an aggregate with the

hydrophilic "head" regions in contact with surrounding water (solvent), sequestering the hydrophobic

tail regions in the micelle center. In this “hydrophobic tail center,” the active substance is dissolved.

A “classical” micelle system does not contain oil and is a surfactant-rich system. If a micelle contains

small amounts of oil, they are called “swollen” micelles.

Like micelles, VESIsorb® is an aqueous dispersion. However, the dispersed phase is composed of Like micelles, VESIsorb® is an aqueous dispersion. However, the dispersed phase is composed of

both surfactant AND oil and belongs, therefore, to the systemic group of micro-emulsions. The

dispersed phase of VESIsorb® can be envisioned as nano-droplets composed of an oily core (oil

components/active ingredients) surrounded by a hydrophilic shell (emulsifiers). Compared to a

micellar system, the VESIsorb® contains lower amounts of surfactant (which is highly desirable) and

high amounts of oil (lipophilic core/center where the active substance is dissolved).

Aqueous VESIsorb® dispersion, like micro-emulsions, act like real solutions that are in a Aqueous VESIsorb® dispersion, like micro-emulsions, act like real solutions that are in a

thermodynamic equilibrium and thus, cannot be accountable to the classical image of an emulsion.

It is a “colloidal” solution with extremely tiny (< 100nm), highly flexible associates.

VESIsorb® vs. LiposomesLiposomes are vesicles and composed of a phospholipid bi-layer membrane surrounding an

aqueous core. Fat-soluble active substances can only be solubilized within the bi-layer membrane,

thus the loading capacity is limited and lower compared to VESIsorb®.

Micelles vs. Liposome vs. Colloidal Delivery SystemMicelles vs. Liposome vs. Colloidal Delivery System

Q: Someone explained to me that the VESIsorb® delivery system is designed to work at “body temperature.” Please explain how this works.A: VESIsorb® has been designed to function and perform in the human body at body temperature

(37°C). This system ensures 100% active ingredient solubility at body temperature both in the

VESIsorb® fill mass and in the aqueous body environment. For example, the CoQ10 VESIsorb®

system has been designed to completely dissolve the CoQ10 at body temperature (37°C) but not

MicelleShell:

Hydrophilic surfactant head

Core: Hydrophobic surfactant tail

LiposomeShell:Bi-Layer

Core: Water

ColloidShell:

Mono-Layer

Core: Oil

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necessarily at room temperature (so called temperature dependent solubility). Thus, by cooling

down the system below body temperature, the clear solution may become oversaturated and the

system becomes semi-solid to solid. By re-warming the system to body temperature of 37°C, it

completely liquefies again and then rebuilds in contact with the gastric/GI fluids in the colloidal

delivery system.

Q: VESIsorb® is described as technologically-advanced delivery system. On what basis do you describe this system in this way?A: The patented VESIsorb® self-assembling colloidal droplet delivery system is technologically adA: The patented VESIsorb® self-assembling colloidal droplet delivery system is technologically ad-

vanced and more scientifically sophisticated than other so called “enhanced absorption systems.”

The superiority of the delivery system has consistently been demonstrated in well-designed pilot and

peer reviewed published pharmacokinetic absorption and bioavailability studies.

The colloidal droplet system must be customized to each active or combinations of actives. Suc-

cessful VESIsorb® formulations are optimized for droplet conversion performance using dynamic

light scattering analysis. The goal is 100% solubilized actives, in a completely homogeneous system

with mean droplet size of less than 100nm. Meeting these criteria confirms that the VESIsorb® self-

assembling colloidal droplet system is working.

What is also important to understand is that the system is not only built around the unique molecular

characteristics of the bio-active but designed for optimal performance in the body. When mixed with

an aqueous system, such as the GI-fluids, this unique lipid-based formulation naturally forms a self-

assembling colloidal droplet delivery system containing solubilized bio-actives.

The following photos are a VESIsorb® Coenzyme Q10 formulation compared to a leading brand that

claimed the product was formulated for improved absorption:

The VESIsorb® droplet conversion is initiated by both the temperature of the body and exposure to

an aqueous environment such as GI-fluids.

A simple demonstration provides perspective on how a “body ready” VESIsorb® formulation

self-assembles naturally in the body. See for yourself by following these simple instructions.

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SEEING IS BELIEVING

VESIsorb® CoQ10 Competing CoQ10 softgel

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Initially warm the capsule to “body temperature” in your hands for 3-4 minutes. Coenzyme Q10

and QH Ubiquinol VESIsorb® formulations are semi-solid at room temperature and will turn to

liquid inside the capsule at body temperature. Other VESIsorb formulas (e.g. Omega-3,

Resveratrol, PMF) are already in a liquid form at ambient temperature.

Pour water into a glass. The water should be body temperature (98.6°F/37°C) to provide

optimal conditions for droplet conversion.

Cut the end of the capsule with scissors (or poke a hole in it with a sharp tack) and gently Cut the end of the capsule with scissors (or poke a hole in it with a sharp tack) and gently

squeeze the contents of the capsule into the glass of water. The various formulations all

perform a little differently.

The VESIsorb® formulation will go into solution in seconds with a little stirring. Follow the same

steps with the competitive product and see the difference! Remember that each patented

VESIsorb® formulation is unique and may vary in appearance based upon concentration,

percent loading of the active, droplet size variation, etc.

Below is a popular Omega-3 fish oil compared to the same fish oil Below is a popular Omega-3 fish oil compared to the same fish oil in VESIsorb®:

Standard TG OMEGA-3 Product

Q: In the case of CoQ10, I understand that the crystals inhibit absorption. I’ve read about “crystal free” delivery systems so the CoQ10 is better absorbed. Is it that simple?A: It is simple to say that all one needs to do is dissolve the fat soluble active (CoQ10) in an applicable A: It is simple to say that all one needs to do is dissolve the fat soluble active (CoQ10) in an applicable

oil and just fill it into a soft gel capsule. Within the capsule (oil environment) it is indeed dissolved but

NOT in an aqueous environment. As soon as the oil, containing the active in a dissolved form, comes in

Oil Drops Sitting On Water

Does Not Go Into Solution

Separation Of Components(No Emulsification)

Colloidal Droplet Formation

100% In Solution! Completely Homogenous Colloidal Solution!

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contact with water, the solution medium (oil) gets diluted and is not stable or mixable with water

because the “linking molecules” (emulsifier) are missing. So, immediately upon losing its oil solubility

feature, the former solved active starts crystallizing in the water environment (e.g. GI-tract). When

this occurs, there is poor dissolution, poor absorption, and little effect.

Q: How does CoQsource® in the VESIsorb® natural colloidal droplet delivery system succeed where “crystal free” fails?A: VESIsorb® is a carrier system which keeps water-insoluble, respectively fat-soluble, molecules in A: VESIsorb® is a carrier system which keeps water-insoluble, respectively fat-soluble, molecules in

a hydrophilic environment (e.g. water, gastric fluids, etc.) in solution. It is a “colloidal”-scale

solubilized system. VESIsorb® does not change a molecule chemically. It is a solubilization vehicle

comprised of oils and monolayer forming agents (emulsifiers). Emulsifiers, due to their nature

(hydrophobic tail and hydrophilic head) - arrange in an aqueous environment at the interface

between oil and water. Without these linking molecules, it is not possible to get a stable oil/water

mixture (e.g. emulsion). A stable emulsion is able to keep fat-soluble molecules dissolved in a water

environment. Upon adding VESIsorb® to an aqueous environment, it naturally self-assembles into a environment. Upon adding VESIsorb® to an aqueous environment, it naturally self-assembles into a

“colloidal emulsion,” where no energy is required to build up the emulsion droplets. These “colloidal

droplets” are not static systems. They are dynamic, meaning their molecules (emulsifiers, oils and

actives) could move by a so-called perpetual “flip-flop” effect from one droplet to another or to other

membranes (e.g. enterocytes).

Q: Do you have pharmacokinetic studies that support the improved absorption and bioavailabilty?A: The peer-reviewed journal, “Alternative Therapies in Health and Medicine,” recently published the

results of a double-blind study comparing the bioavailability of patented CoQsource® (coenzyme

Q10 in a VESIsorb® formulation) Bio-Enhanced CoQ10 to that of other bio-enhanced formulations.

The study, entitled, “Relative Bioavailability Comparison of Different Coenzyme Q10 Formulations

with a Novel Delivery System,” appears in the March/April, 2009 issue, Volume 15, Number 2.

The graph below provides a vivid illustration of the difference in CoQsource® (the orange line) which is

coenzyme Q10 in the VESIsorb® delivery system versus the three other “bio-enhanced” coenzyme Q10

Pharmacokinetic ProfilePharmacokinetic Profile

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products in plasma concentration levels over time. CoQsource® (coenzyme Q10 in the VESIsorb®

delivery system) not only has higher plasma concentration levels after one hour, but continues to

increase dramatically before reaching Cmax at about 4 hours. The plasma concentration of

CoQsource® remains well above levels for the 3 other treatments throughout the 24 hour period.

Q: Has VESIsorb® successfully been applied to natural ingredients other than CoQ10?A: Yes, we have successfully developed VESIsorb® formulations with many other natural bio-active A: Yes, we have successfully developed VESIsorb® formulations with many other natural bio-active

ingredients including CoQ10 in both the Ubiquinone and KanekaQH™ Ubiquinol forms, Omega-3

EPA/DHA, Vitamin D-3, Resveratrol, Palm Tocotrienols, Gamma Tocopherols, Citrus

Polymethoxylated Flavones (PMFs), and more. PMFs are notoriously poorly absorbed, and we have

dramatically improved their absorption, solubility and application in food and beverages.

Kaneka QH™ Ubiquinol:A pharmacokinetic pilot study in humans comparing Kaneka QH™ Ubiquinol to the same Kaneka A pharmacokinetic pilot study in humans comparing Kaneka QH™ Ubiquinol to the same Kaneka

QH™ Ubiquinol in the VESIsorb® delivery system demonstrated an increase of 696% in peak blood

levels of Ubiquinol. The relative bioavailability calculated using the area under the curve was also

increased by 485%.

Omega Choice® concentrated Co2 critical extraction EPA:A pharmacokinetic pilot study in humans comparing OmegaChoice® 90 Concentrated Omega-3 A pharmacokinetic pilot study in humans comparing OmegaChoice® 90 Concentrated Omega-3

EPA to the same OmegaChoice® 90 in the VESIsorb® delivery system demonstrated an increase of

567% in peak blood levels of EPA. The relative bioavailability calculated using the area under the

curve was also increased by 487%.

Q: Are there other advantages to VESIsorb® solubilization technology besides bioavailability? On the manufacturing side/formulation – does it facilitate production? Or raise particular challenges?A: The advantages of the VESIsorb® Delivery System go well beyond absorption and bioavailability. A: The advantages of the VESIsorb® Delivery System go well beyond absorption and bioavailability.

We have been able to broaden the applications for certain bio-active ingredients into food products,

drink mixes, beverages, and personal care products. We have succeeded in this area by addressing

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issues such as water solubility, oxidative stability, shelf life and uniformity of dispersion in the

delivery medium. The VESIsorb® system is easy to work with in production and effectively improves

many production systems.

Q: Is there a spectrum of "natural" and safety concerns with nanotechnology – ranging from technology that is closer to natural processes vs. more highly engineered products? Can you give some examples along the spectrum?A: "Natural" is normally linked with purity and safety. Nanotechnology is a broad and complex field A: "Natural" is normally linked with purity and safety. Nanotechnology is a broad and complex field

that needs to be discussed under certain rules of nomenclature and distinguishing aspects. Experts

agree it is critically important to differentiate between solid “nano- particles” versus “nano-size” fluid

droplets as well as differentiating between those that disintegrate in vivo and those that do not.

The VESIsorb® naturally self-assembling association colloidal droplets disintegrate within the The VESIsorb® naturally self-assembling association colloidal droplets disintegrate within the

GI-tract into the single components; thus the formed droplets are of transient nature and considered

safe by the experts. In contrast, solid, non-disintegrating nano-particles such as carbon nano-tubes,

are an example of nanotechnology that has raised concerns about safety.

However, aside from the mentioned aspects, many other factors can influence the safety of However, aside from the mentioned aspects, many other factors can influence the safety of

nano-systems. Various scientific expert groups are discussing this complex issue and are trying to

establish guidelines for the safe use of nanotechnology. A recent and excellent report published by

the IRCG (International Risk Governance Council; “Risk Governance of Nanotechnology

Applications in Food and Cosmetics”) summarizes some of the activities regarding safety of

nanotechnology.

To learn more about VESIsorb®, take a virtual tour of the Vesifact AG facility To learn more about VESIsorb®, take a virtual tour of the Vesifact AG facility in Switzerland and view a VESIsorb® video, visit www.Source-1-Global.com.

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