Nano coenzyme q10 or bioavailable Ubiquinone is markedly different from Coenzyme q10 (CoQ10), which is difficult to make available to cellular physiology.  As we know from our cell biology and biochemistry, Coenzyme q10 or Ubiquinone is highly lipophilic and therefore it must be co-administered with a high fat meal or drink.   Even then the bioavailability is marginal at best.  In more recent years nanotechnology has introduced methods to enhance bioavailability of Coenzyme q10 in the gut for greater absorption.  But, does it really help mitochondrial processing?  In many studies deficient Ubiquinone levels have been associated with cardiovascular disease, diabetes, neurodegenerative disorders, statin-associated myopathy, and some cancers (Zhou, Liu, Zhang, et al., 2014).  Consequently, we should transmit our knowledge of nano coenzyme q10 benefits to our patient population to aid them in their self-healing efforts.

Coenzyme Q10 (CoQ10) is part of the mitochondrial respiratory chain of all living cells, used for necessary processing energy reactions along the inner mitochondrial membrane. CoQ10 is one of the Quinone’s, and is structurally similar to vitamin K or menaquinone (Alban, Muralikrishnan & Ebadi, 2002). CoQ10, when in its reduced form, Ubiquinol, has effective antioxidant properties, which means it lowers free radicals and lipid peroxidation buildup that would otherwise contribute to oxidative stress. It performs its antioxidant function in the biological membranes protecting mitochondrial inner-membrane proteins and DNA.   Ubiquinone has an amphipathic property owing to its dual structural features, notably its hydrophilic benzoquinone ring and its polyisoprenoid side chain that gives it a lipophilic capacity.  Ubiquinone’s amphipathic property facilitates electron transport chain activity by transferring electrons between redox components in the chain establishing a proton gradient across the inner mitochondrial membrane, which makes the energy in ATP. Ubiquinone in tissues is normally up-regulated in the presence of oxidative stress such as physical exercise, encounters with cold weather, and thyroid hormone therapy.  Increasing age tends to counter the normal levels of Ubiquinone (Alban, Muralikrishnan & Ebadi, 2002).  As stated, CoQ10 deficiencies contribute to a number of illnesses that can be ameliorated with supplementation.  Sadly, the quest for bioavailability has been the issue, until the advent of nano Coenzyme Q10. 

Initial attempts at increasing bioavailability of Coenzyme Q10 involved using an oil solution and suspension system.  Later, a lipid and surfactant based emulsion system was tried, followed by a solid dispersion system, but water solubility of the Coenzyme Q10 agent remained low (Zhou, Liu, Zhang, et al., 2014).  Instead, a nanoemulsion method was needed to enhance the bioavailability of CoQ10 that was not based on the earlier lipid-based delivery systems.  The nanoemulsion method allowed a water-insoluble agent, Coenzyme Q10, transit across a water-soluble environment.  Then, Sharma, et al. (2012) reported that while there were complications to the mitochondrial apparatus in certain study subjects, a reversal of their impaired function was demonstrated when given nano Coenzyme Q10 in adequate quantities.  The authors used multifunctional nanocarriers based on “ABC miktoarm polymers” (A = poly(ethylene glycol (PEG), B = polycaprolactone (PCL), and C = triphenylphosphonium bromide (TPPBr)).  This was combined using click chemistry with ring-opening polymerization that were self-assembled into nanosized micelles and used for delivery of the Ubiquinone.  The authors reported this nano delivery system achieved full bioavailability to the mitochondria without losing continuity of the Ubiquinone.

Kwong et al. (2002) was concerned about the benefits of Coenzyme Q (CoQ10) administered orally assisting the mitochondrial electron transport chain and deploying its in-vivo antioxidant properties.   The research team subjected rats to CoQ10 (150 mg/kg/d) in their diets for 4 and 13 weeks.  Using HPLC to follow half-life levels of CoQ10, the team found CoQ10 added to the rat’s diet resulted in an elevation of equivalent CoQ10 levels in rat heart, brain, and skeletal muscle mitochondrial tissues.  Additionally, they found lower levels of protein oxidative damage with commensurate increases in antioxidative capabilities.

Sanbe, Tanonaka, Niwando & Takeo (1994­), studied heart failure (CHF) in rats and did not find significant improvement in the survival of CHF animals using Coenzyme Q10.  However, in the right ventricle of CoQ10-treated animals, a significant increase was noted in the levels of creatine, inorganic phosphate, and mitochondrial oxygen consumption rates.  Additionally, the team noted slight increases in creatine phosphate, but not in adenosine-5′-triphosphate, suggesting the right ventricle had the capacity to recover its energy functions. 

Ullmann, Metzner, Schulz, Perkins, & Leuenberger (2005), studied commercial formulations of Coenzyme Q10.  The team was interested in comparing the bioavailability of the different products.  They studied DSM Nutritional Products Ltd. (Kaiseraugst, Switzerland) CoQ10 10% TG/P (all-Q®), a new tablet-grade formulation, with CoQ10 Q-Gel® Softsules® based on the Bio-Solv® technology (Tishcon Corp., Salisbury, MD; marketed by Epic4Health™, Smithtown, NY) and Q-SorB® (Nature’s Bounty™, Bohemia, NY). The team took plasma CoQ10 levels at trough through 36 hours using 12 healthy male subjects in a randomized, three-period crossover bioequivalence study.  Highest C max or bioavailability values were seen after Q-Gel application.  However, the time to reach maximum bioavailability was identical across all samples.  A test for bioequivalence revealed Q-Gel and all-Q to be bioequivalent.  Additionally, both Q-Gel and all-Q had better bioavailability than Q-SorB. It was noted that a discriminator of the two bioequivalent agents, all-Q and Q-Gel, is that all-Q is available in tablets, but not Q-Gel.

In summary, it appears the nano formulation of Coenzyme Q10 is needed to supply adequate amounts of Ubiquinone to the tissues for inner mitochondrial activity.  Given the lipid boundary and bioavailability when supplying merely the product in a high-lipid diet, it seems prudent to recommend the nano formulation of Coenzyme Q10 to achieve therapeutic response.  There are numerous patient groups that can benefit from this agent.  In addition to the illnesses of cardiovascular disease, diabetes, neurodegenerative disorders, statin-associated myopathy, and some cancers, the elderly seem to derive benefit.

 

References:

Albano, C. B., Muralikrishnan, D., & Ebadi, M. (2002). Distribution of coenzyme Q homologues in brain. Neurochemical research, 27(5), 359-368.

Bentinger, M., Dallner, G., Chojnacki, T., & Swiezewska, E. (2003). Distribution and breakdown of labeled coenzyme Q< sub> 10</sub> in rat. Free Radical Biology and Medicine, 34(5), 563-575.

Kwon, S. S., Nam, Y. S., Lee, J. S., Ku, B. S., Han, S. H., Lee, J. Y., & Chang, I. S. (2002). Preparation and characterization of coenzyme Q< sub> 10</sub>-loaded PMMA nanoparticles by a new emulsification process based on microfluidization. Colloids and Surfaces A: Physicochemical and Engineering Aspects, 210(1), 95-104.

Kwong, L. K., et al. (2002). Effects of coenzyme Q10 administration on its tissue concentrations, mitochondrial oxidant generation, and oxidative stress in the rat. Free Radical Biology and Medicine.  33 (5) 1, pp. 627–38. doi: 10.1016/S0891-5849(02)00916-4.

Lipshutz, B. H., Mollard, P., Pfeiffer, S. S., & Chrisman, W. (2002). A short, highly efficient synthesis of coenzyme Q10. Journal of the American Chemical Society, 124(48), 14282-14283.

Sanbe, A., Tanonaka, K., Niwano, Y., & Takeo, S. (1994). Improvement of cardiac function and myocardial energy metabolism of rats with chronic heart failure by long-term coenzyme Q10 treatment. Journal of Pharmacology and Experimental Therapeutics, 269(1), 51-56.

Sharma, A., Soliman, G. M., Al-Hajaj, N., Sharma, R., Maysinger, D., & Kakkar, A. (2011). Design and evaluation of multifunctional nanocarriers for selective delivery of coenzyme Q10 to mitochondria. Biomacromolecules, 13(1), 239-252. doi: 10.1021/bm201538j.

Ullmann, U., Metzner, J., Schulz, C., Perkins, J., & Leuenberger, B. (2005). A new coenzyme Q10 tablet-grade formulation (all-Q®) is bioequivalent to Q-Gel® and both have better bioavailability properties than Q-SorB®. Journal of medicinal food, 8(3), 397-399.

Xia, S., Xu, S., & Zhang, X. (2006). Optimization in the preparation of coenzyme Q10 nanoliposomes. Journal of agricultural and food chemistry, 54(17), 6358-6366.

Zhou,H., Liu, G., Zhang, J., et al. (2014). Novel Lipid-Free Nanoformulation for Improving Oral Bioavailability of Coenzyme Q10. BioMed Research International. Article ID 793879, 9 pages. doi:10.1155/2014/793879.

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