Micellization is actually a complicated word for a fairly easy to understand process. It is simply taking a lage particle and breaking it down, sometimes to thousanths of it’s original size, so the body can easily absorb it. Think of an hourglass…. if I were to put a pebble in the glass, it wouldn’t flow through that little narrow hole in the middle. If that pebble were crushed up however, all the particles could flow through and get where they need to be. The same thing goes on inside our bodies. We have small pore like openings in our cell walls, called aquaporin. If a particle is too big, it is not absorbed into this little pore like opening. If however that particle is broken into thousands of little bits, well, it slips right through. Voila! 100% absorbsion. So when you buy a Micellized product, you get everything you are paying for. It will not end up in the toilet. Gross, huh? But really, if you take vitamins, notice the color of your urine. In large part, the bright color is all the vitamins you spent good money for that went straight on through to your bladder. Nice. With Biometics, you will notice a change. But not from vitimins absorbed, but it will be quite light because you are drinking more water. That’s about it.
Here’s the scientific version of what Micellization is:
Discover the Advantage of EMUSOL® MICELLIZATION
Understanding the Process of Drug or Nutrient Absorption
Understanding the Process of Drug or Nutrient Absorption
To understand how the micellization process improves the absorption of fat-soluble compounds,
one has to understand how drugs/nutrients act in order to have desired therapeutical/nutritional
effects.
Understanding the Process of Drug or Nutrient Absorption
1, 2
To produce its characteristic effects, a drug must be present in appropriate concentration at its
site of action. The extent to which a drug reaches its site of action is called bioavailability.
Although it is obviously a function of the amount of drug administered, the concentration at its site
of action also depends on the extent of its absorption, distribution and elimination. In order to
increase the bioavailability of a drug, one can formulate the dose form that will modify its
absorption and distribution process.
1, 2, 3
The absorption of a drug involves its passage across cell membranes. The basic structure of
biological membranes is a bimolecular leaf arrangement of lipids as shown in Figure 1, in which
the amphoteric lipids and cholesterol are oriented so that the hydrophobic portion of the
molecules interact minimizing their contact with water or other polar groups, and polar head
groups of the lipids are at the interface with the aqueous environment, as shown in Figure 2.
At the junction of membrane surface and body fluid, there is a double layer formation. This double
layer is aqueous in nature. For a drug to cross the membrane and arrive at its site of action, it
must cross this double layer before getting into the membranes. Absorption, regardless of the
site, is dependent upon drug solubility in the double layer. The higher the solubility, the higher the
absorption, therefore the higher the bioavailability.
How can micellized compounds have better absorption?
When amphoteric surfactant is dissolved in aqueous solution, the molecules of the compound
tend to aggregate and form a ball-like structure called micelle:
4
Big blue hydrophilic “heads” group towards the outside of the ball while little hydrophobic “tails”,
which are oil-like, group inside the ball “away” from the solution. Because of the nature of the
micellar structure, micellization can solubilize fat-soluble compounds inside the ball and increase
solubility of the compounds in the double layer dramatically, hence increasing their bioavailability.
EMUSOL® MICELLIZATION
Recognizing the advantages of aqueous preparation of fat-soluble nutrients over oil forms,
research during the past years has concentrated on improving the design of new dosage forms
that substantially increase the effectiveness of such formulations. Much of this activity has
focused on the development of micro-emulsion systems in which an oil is divided into very small
droplets (< 0.1 micron) referred to as “micelles”.
4
The use of micellar technology not only improves the efficacy of the product but allows a
reduction in the total dose. One of the breakthroughs in nutritional delivery systems is the unique
EMUSOL® MICELLIZATION PLUS process. The uniqueness of this process is easily
demonstrated by observing the resulting transparent solution when a micellized nutrient is added
to water. There is abundant evidence in the scientific literature that fat-solubles are more
effectively absorbed from aqueous preparations than from oily forms.
3
However, the real
advantage is the increase in amount and rate of absorption.
ENHANCED BIOAVAILABILITY
Several studies have been conducted on the EMUSOL® micelle vitamin preparations to
determine the effectiveness of this delivery system when compared with both standard oil forms
and other emulsified forms. The studies were conducted in a random crossover fashion with
normal healthy individuals varying in sex and age. The following information is a summary of the
results:
VITAMIN E
FIVE TIMES GREATER ABSORPTION
Platelets play an important role in thrombus formation in arterial vascular walls which may lead to
vascular disease. It has been suggested in the scientific literature that vitamin E exhibits antiplatelet
activity.
5
However, the plasma level of vitamin E in oil form is found to be very low. The
absorption of Vitamin E in oil form is lower than 25% in normal humans.
6
Dosage of 500 IU of d-alpha-tocopheryl acetate were administered to the 12 subjects and the
plasma levels were measured as an increase over baseline levels (19.8 micromoles/liter) at 4 and
24 hours. Figure 3 shows the results of the comparative absorption increases of vitamin E plasma
levels of the oil, emulsified and EMUSOL® form at 4 and 24 hours. Table 1 indicates the relative
increases in absorption.
The data indicates that the EMUSOL® form of vitamin E showed a 4.8 times increase over the oil
form at 4 hours and 5.0 times increase at 24 hours. It also showed that the EMUSOL® form
increased plasma levels more than twice that of the emulsified form.
OVER FOUR TIMES FASTER ABSORPTION
In a separate study, the rate of the absorption (micromole/liter/hour) was compared using 500 IU
of the oil, emulsified and EMUSOL® forms of d-alpha-tocopheryl acetate. Figure 4 shows the
results of this study. Table 2 indicates the comparative rates of absorption observed.
The data indicates that the EMUSOL® form of vitamin E is absorbed 4.5 times faster than the oil
form. It was also absorbed nearly twice as fast as the emulsified form.
VITAMIN A
FIVE TIMES GREATER ABSORPTION
Human subjects were given 50,000 IU vitamin A palmitate in either an oil, emulsified or
EMUSOL® form. The blood plasma levels were measured as an increase over baseline levels
(2.675 micromoles/ liter) at 4 and 8 hours. Figure 5 illustrates results while Table 3 provides a
summary of the relative increases.
The data indicates that the EMUSOL® form of vitamin A showed a 5.4 times increase over the oil
form at 4 hours and a 4.7 at 8 hours. It also showed that the EMUSOL® form increased plasma
levels more than twice that of the emulsified form.
EMUSOL® is a registered trademark of Micelle Laboratories, Inc.
References:
1. Goodman and Gilman’s “The Pharmacological Basis of Therapeutics”, Eighth Edition, pp
1-83, McGraw-Hill, 1990
2. Thomas M Devlin “Biochemistry with Clinical Correlations” Third Edition, pp 1059-1091,
Wiley-Liss, 1993
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excretion and storage of oily and aqueous preparations of vitamin A. J Paediatr
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rat: the effect of different carriers and different dose levels. Int J Vit Nutr Res 42,
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Paediatr 85, 753-759 (1974);
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h. Sokol RJ, Heubi JE, Butler-Simon N, et al. Treatment of vitamin E deficiency
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12(3), 46-54 (1987)
5.
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aggregation and thrombocythemia in the rat. ProcSocExp Biol Med 149, 275-277
(1975);
b. Steiner M, Anastasi J. Vitamin E: an inhibitor of the platelet release reaction. J
Clin Invest 57, 732-737 (1976);
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incorporation of 14 c-arachidonate into platelet lipids of rabbits. J Nutr III, 1839-
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supplementation on platelet aggregation in man. J Am Col N 3, 244-249 (1984)
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excretion of vitamin E in man. J Lab Clin Med 39, 802-807 (1952