Benefits and importance of CoQ10 for the human health:
Coenzyme Q10 (CoQ10) is an endogenously produced lipid-soluble molecule of the human organism
that is considered an essential component of the mitochondrial electron transport chain where
it is the electron acceptor for complexes I and II. In this context, CoQ10 plays a key role
in mitochondrial oxidative phosphorylation and ATP production and therefore it is essential
for all energy-dependent processes in the body, enhancing the immune-system and acting as a
free radical scavenger. In addition to its abundant presence in the mitochondrion, CoQ10 is
found in other organelles such as endoplasmic reticulum, peroxisomes, lysosomes and vesicles.
It is a membrane stabilizer, preserves myocardial sodium-potassium ATPase activity, and
stabilizes myocardial calcium-dependent ion channels. Several factors such as ageing, poor
eating habits, stress and infection, are known to affect the organism's ability to continue
synthesizing and providing the adequate amounts of CoQ10. With age, the human organism begins
to develop a CoQ10 deficiency due to its inability to synthesize it from food where it is
present in beef, poultry, broccoli, soya oil and peanuts. In this context, several
researchers have advised using CoQ10 supplements alone or in combination with other
nutritional supplements to alleviate this deficiency and help maintain health of elderly
people or treat some of the health problems or diseases. Due to these functions, CoQ10 finds
its application in different commercial branches such as food, cosmetic, or pharmaceutical
industries. The antioxidant activity of CoQ10 surpasses both in the amount and in efficiency
other antioxidants. The protective effect is extended to lipids proteins and DNA mainly
because of its close localization to the oxidative events and the effective regeneration by
continuous reduction at all locations. CoQ10 in its reduced form as a hydroquinone
(ubiquinol) is a potent lipophilic antioxidant that has a great importance as a free radical
scavenger. CoQ10 protects the stability of the cell membranes, protects DNA from free radical
induced oxidative damage, and is capable of recycling and regenerating other antioxidants,
such as tocopherol and ascorbate. Other important functions of CoQ10 as e.g. cell signaling
and gene expression have also been described.
Absorption and Transport of CoQ10:
Taking its lipophilic nature, the absorption of CoQ10 is enhanced in the presence of lipids
with the main role attributed to the intestinal secretions from the pancreas and bile that
are known to facilitate emulsification and micelle formation required for the fats
absorption. Either during or following its absorption in the intestine, CoQ10 is reduced to
ubiquinol, incorporated into chylomicrons and then transported via the lymphatics to the
circulation where about 95% of CoQ10 in circulation exists in its reduced form as ubiquinol
in human subjects. Plasma CoQ10 concentrations are highly dependent on plasma lipoproteins
where CoQ10 redistributes possibly to protect lipoproteins from oxidation. Several factors
have highlighted the poor absorption of orally administered CoQ10 such as its insolubility in
water, limited solubility in lipids, and relatively large molecular weight. A preclinical
study has reported that only about 2-3% of orally-administered CoQ10 was absorbed.
Additionally, the absorption of CoQ10 and its bioavailability have been shown to be dependent
on other factors such as the nature of the formulation of CoQ10 with solubilized formulations
been reported to have an advanced effect on the bioavailability.
Tissue distribution of CoQ10 in humans and animals:
Upon its presence in the circulatory system, CoQ10 is distributed in all the tissues in
varying amounts with high concentrations been reported to be present in organs with high
metabolic activities such as the heart, kidney, liver and muscle. Additionally, and due to
its lipophilic nature, the lipid content of the body organ do play a role in the CoQ10
distribution. At the subcellular level, data have shown that a large portion of CoQ10
(40-50%) is localized in the mitochondrial inner membrane, with smaller amounts in the other
organelles and in the cytosol. At the blood level, about 95% of CoQ10 is present in the
ubiquinol-reduced form. Among blood cells, lymphocytes and platelets contain significant
amounts of CoQ10 whereas red blood cells contain only a tiny amount due to their lack of
mitochondria.
Pharmacokinetics of CoQ10:
In a pharmacokinetic study conducted on sixteen healthy subjects, and using deuterium-labeled
CoQ10 (100 mg), a Tmax of 6.5 h along with an elimination half-life of about 33 hours and a
mean plasma levels around 1 µg/ml have been reported. Similar results have been also found
when unlabeled CoQ10 has been used in another study. It is worth to mention that powder-based
CoQ10 products were used in both of these studies. To compare the bioavailability of several
CoQ10 formulations, three different solubilized formulations of CoQ10 were compared to a
powder-based formulation. Results have shown that two of the solubilized formulations along
with the powder product have showed a Tmax of about 6 h whereas the remaining solubilized
formulation had a Tmax of about 8 h. These results were similar and in accordance to other
results. The Tmax value of about 6 h or longer indicates that CoQ10 is absorbed slowly from
the gastrointestinal tract and this is attributable to both its hydrophobicity and high
molecular weight. In the different pharmacokinetic studies conducted on CoQ10, a second
plasma CoQ10 peak has been observed at about 24 h following oral ingestion, which may be due
to both enterohepatic recycling and redistribution from the liver to circulation.
Bioavailability of CoQ10 / Delivery systems:
Although CoQ10 has been reported to be useful for the treatment of several diseases such as
ageing, fatigue, irregular heartbeat, high blood pressure, and immune system impairment among
others, its efficacy has been always hindered by its high lipophilicity and poor solubility
in water, which leads to decreased absorption into the systemic circulation. Several
conventional formulations of CoQ10 are available in the form of soft gel capsules, oral spray
and tablets. Despite these, the idea of delivery of CoQ10 to the body remains a challenge. To
overcome the slow absorption of CoQ10, various bioavailability enhancement methods have been
developed such as liposomes, polymeric nanoparticles, polymeric micelles, solid lipid
nanoparticles, nanostructured lipid carriers, self-emulsifying systems, nanoemulsions and
solid and aqueous dispersions have been explored and developed to improve the solubility, the
absorption and the bioavailability of CoQ106. Based on purified phospholipids as the key
component and with a dose of 100 mg of CoQ10, NanoSolve has shown to increase the
bioavailability of CoQ10 fivefold in comparison to pure CoQ109. Using cyclodextrin as a
carrier, a novel patented formulation known as Q10Vital® has demonstrated its ability to
increase the bioavailability of CoQ10 when two Q10Vital formulations (liquid and powder) were
compared to regular CoQ10/soybean oil softgels. Although no difference in the Tmax was
observed between the three tested products, both Q10Vital formulations have reported a higher
Δcmax (32 % for the liquid formulation and 25% for the powder formulation) in comparison with
the regular softgel product.
Rationale of this study:
Although several technologies and delivery systems have been used to improve the absorption
of CoQ10 and increase its bioavailability, the carriers used to deliver CoQ10 are based on
synthetic products with no health benefits attributed to them. In alignment with its mission
and vision to deliver wellness products, Biodroga Neutraceuticals Inc has decided to develop
a new product (MaxSiQ10) aiming to increase the absorption and the bioavailability of CoQ10
by using omega-3 fatty acids as a vector delivery system and a carrier for CoQ10. The
benefits of omega-3 fatty acids to the human health have been well documented and reported in
several studies20-22. Because the human body does not efficiently produce fish-derived
omega-3 fatty acids (EPA and DHA) from its precursor alpha-linolenic acid, it is necessary to
obtain adequate amounts through fish and fish-oil products. Studies have shown that EPA and
DHA have been associated with better fetal development, including neuronal, retinal, and
immune function. Additionally, EPA and DHA may affect many aspects of cardiovascular function
including inflammation, peripheral artery disease, major coronary events, and
anticoagulation. Promising results have been attributed for EPA and DHA in weight management,
and prevention of cognitive decline. To differentiate themselves from the other products and
technologies already existing on the market, Biodroga Neutraceuticals Inc will be using its
MaxSimil® technology as the vector delivery system for CoQ10. MaxSimil is a new-patented
delivery technology that intrinsically enhances the absorption of omega-3 fatty acids (EPA
and DHA) of a given fish oil by modifying its glyceride composition to simulate digestion.
This technology delivers "absorption-ready" formulations enriched with "self emulsifing"
monoglycerides (MAG) and have the potential to be better absorbed when compared to the more
traditional ethyl ester (EE) and reconstituted triglycerides (rTG) fish oil forms available
on the market today. What differentiates MaxSimil relies in being a completely natural health
product with a demonstrated ability to increase the absorption of omega-3 fatty acids whereas
other carriers are synthetic chemical surfactants with detrimental effects on human cells.
Therefore, this project will test a MAG-Omega-3 formulation enriched with CoQ10, since it was
hypothesized that this formulation will be the most absorbed and bioavailable with the lowest
side effects in men and women without any disease such as intestinal lipid absorption issues.