madman
Super Moderator
Coenzyme Q10 supplementation: Efficacy, safety, and formulation challenges
Abstract
World population growth and aging are posing unprecedented challenges in sustaining the health of 9.1 billion people that will be occupying the planet by 2050. Although non-communicable diseases such as cardiovascular and neurodegenerative diseases, cancer, and diabetes are among the top 10 global causes of death, they can be prevented by risk factor reduction, early detection, and adequate treatment. Since a healthy diet along with dietary supplementation could play an important role to reduce morbidity and cut off its associated health care costs, research in the food and nutrition area is required to find solutions to global challenges affecting health.
As a result of the healthy living trend, the dietary supplements category is growing fast, leading to an urgent need for dietitians, physicians, and policymakers to broaden the scientific evidence on the efficacy and safety of a wide range of active ingredients. Coenzyme Q10 (CoQ10), as the third most consumed dietary supplement, and as a potential candidate for the treatment of various non-communicable diseases that are among the global top 10 causes of death, has gained interest over years. Scientific evidence regarding mainly CoQ10 efficacy and safety, as well as formulation challenges, is addressed in this review.
1 INTRODUCTION
When it comes to coenzyme Q10 (CoQ10), which is not an FDA-approved drug, but yet sold as a food supplement (DrugBank, 2019), it is currently the third most consumed nutritional supplement after fish oil and multivitamins (Kapoor & Kapoor, 2013). In addition, thanks to its strong antioxidant activity, and physiological key role in mitochondrial bioenergetics (Nelson & Cox, 2017), it has also been considered as a potential candidate for the treatment of various diseases where oxidative stress plays a significant role such as cardiovascular diseases, neurodegenerative disorders, cancer, and diabetes, which are among the top 10 global causes of death (Dhanasekaran & Ren, 2005; Villalba, Parrado, SantosGonzalez, & Alcain, 2010; WHO, 2018a). For this reason, considering that CoQ10 supplementation has gained interest over years and has an expanding consumer base, a review of the current scientific evidence regarding CoQ10 supplementation is needed. The aim of this review is to provide researchers, dietitians, physicians, formulators, and regulators with a breadth of evidence on CoQ10 efficacy, safety, and formulation challenges. In order to meet these objectives, this review is organized in the following sections: CoQ10 overview sources and deficiency, and supplementation, which includes pharmacokinetics and bioavailability, therapeutic indications, safety and precautions, and formulation.
2 OVERVIEW OF COQ10
3 COQ10 SOURCES AND DEFICIENCY
4 COQ10 SUPPLEMENTATION
4.1 Pharmacokinetics and bioavailability of the dietary supplement CoQ10
4.2 Therapeutic indications
4.2.1 Cardiovascular diseases
4.2.2 Statin-induced myopathy
4.2.3 Neurodegenerative diseases
4.2.4 Cancer
4.2.5 Diabetes
4.2.6 Treatment of CoQ10 deficiencies
4.2.7 Migraine
4.2.8 Athletic performance
4.2.9 Male infertility
4.3 Safety and precautions
4.4 Formulation
5 CONCLUSION
CoQ10 not only plays an essential role in the synthesis of cellular energy in the form of ATP but it is also a strong lipophilic antioxidant. Despite being endogenously synthesized in the human body and found in plant and animal tissues that are part of our diet, different factors can lower its physiological concentrations. While CoQ10 deficiencies have been reported in certain diseases and conditions where oxidative stress plays a significant role, whether the deficiency is a cause or consequence remains unknown. However, since a number of clinical trials have observed that its oral administration provided beneficial effects on different disorders that have been associated with low CoQ10 levels and high oxidative stress, it has been suggested as a promising therapeutic agent to prevent and slow the progression of these diseases that include cardiovascular diseases, statins-induced myopathy, neurodegenerative diseases, cancer, diabetes, CoQ10 deficiencies, migraine, athletic performance, and male infertility.
These findings on the potential health benefits of CoQ10 supplementation have led to increased consumer demand. In addition, in the context of population aging and the healthy living trend, consumers are becoming more aware than ever of ingredients in their food and their properties, and an increasing number of consumers are seeing food as a medicine. For this reason, dietary supplements stand out as one of the fastest-growing healthcare categories. Consumer base expansion has led to an urgent need for researchers, dietitians, physicians, and regulators to broaden the scientific evidence on the efficacy and safety of a wide range of active ingredients found in food supplements, including CoQ10. This review intended to provide them with a breadth of evidence on CoQ10 efficacy, safety, and formulation challenges. However, further studies must be carried out in order to clarify the role of CoQ10 and the optimal therapeutic regimen in the management of different health conditions. Additional investigation on physicochemical properties, pharmacokinetics, stability, and efficacy is also needed to deepen the knowledge on CoQ10 and to allow formulators to improve CoQ10 properties by means of different techniques. This is especially relevant since solubility, but especially stability and bioavailability concerns hinder its use in food supplements and medicinal products. For this reason, further research is needed to overcome these issues. Finally, although there is insufficient evidence to conclude its efficacy on different therapeutic indications, it is worth highlighting that CoQ10 supplementation is safe and well-tolerated at doses much higher than usual, with few drug interactions and minor side effects. However, people with certain health conditions and under treatment should consult with a health care professional before using CoQ10.
Abstract
World population growth and aging are posing unprecedented challenges in sustaining the health of 9.1 billion people that will be occupying the planet by 2050. Although non-communicable diseases such as cardiovascular and neurodegenerative diseases, cancer, and diabetes are among the top 10 global causes of death, they can be prevented by risk factor reduction, early detection, and adequate treatment. Since a healthy diet along with dietary supplementation could play an important role to reduce morbidity and cut off its associated health care costs, research in the food and nutrition area is required to find solutions to global challenges affecting health.
As a result of the healthy living trend, the dietary supplements category is growing fast, leading to an urgent need for dietitians, physicians, and policymakers to broaden the scientific evidence on the efficacy and safety of a wide range of active ingredients. Coenzyme Q10 (CoQ10), as the third most consumed dietary supplement, and as a potential candidate for the treatment of various non-communicable diseases that are among the global top 10 causes of death, has gained interest over years. Scientific evidence regarding mainly CoQ10 efficacy and safety, as well as formulation challenges, is addressed in this review.
1 INTRODUCTION
When it comes to coenzyme Q10 (CoQ10), which is not an FDA-approved drug, but yet sold as a food supplement (DrugBank, 2019), it is currently the third most consumed nutritional supplement after fish oil and multivitamins (Kapoor & Kapoor, 2013). In addition, thanks to its strong antioxidant activity, and physiological key role in mitochondrial bioenergetics (Nelson & Cox, 2017), it has also been considered as a potential candidate for the treatment of various diseases where oxidative stress plays a significant role such as cardiovascular diseases, neurodegenerative disorders, cancer, and diabetes, which are among the top 10 global causes of death (Dhanasekaran & Ren, 2005; Villalba, Parrado, SantosGonzalez, & Alcain, 2010; WHO, 2018a). For this reason, considering that CoQ10 supplementation has gained interest over years and has an expanding consumer base, a review of the current scientific evidence regarding CoQ10 supplementation is needed. The aim of this review is to provide researchers, dietitians, physicians, formulators, and regulators with a breadth of evidence on CoQ10 efficacy, safety, and formulation challenges. In order to meet these objectives, this review is organized in the following sections: CoQ10 overview sources and deficiency, and supplementation, which includes pharmacokinetics and bioavailability, therapeutic indications, safety and precautions, and formulation.
2 OVERVIEW OF COQ10
3 COQ10 SOURCES AND DEFICIENCY
4 COQ10 SUPPLEMENTATION
4.1 Pharmacokinetics and bioavailability of the dietary supplement CoQ10
4.2 Therapeutic indications
4.2.1 Cardiovascular diseases
4.2.2 Statin-induced myopathy
4.2.3 Neurodegenerative diseases
4.2.4 Cancer
4.2.5 Diabetes
4.2.6 Treatment of CoQ10 deficiencies
4.2.7 Migraine
4.2.8 Athletic performance
4.2.9 Male infertility
4.3 Safety and precautions
4.4 Formulation
5 CONCLUSION
CoQ10 not only plays an essential role in the synthesis of cellular energy in the form of ATP but it is also a strong lipophilic antioxidant. Despite being endogenously synthesized in the human body and found in plant and animal tissues that are part of our diet, different factors can lower its physiological concentrations. While CoQ10 deficiencies have been reported in certain diseases and conditions where oxidative stress plays a significant role, whether the deficiency is a cause or consequence remains unknown. However, since a number of clinical trials have observed that its oral administration provided beneficial effects on different disorders that have been associated with low CoQ10 levels and high oxidative stress, it has been suggested as a promising therapeutic agent to prevent and slow the progression of these diseases that include cardiovascular diseases, statins-induced myopathy, neurodegenerative diseases, cancer, diabetes, CoQ10 deficiencies, migraine, athletic performance, and male infertility.
These findings on the potential health benefits of CoQ10 supplementation have led to increased consumer demand. In addition, in the context of population aging and the healthy living trend, consumers are becoming more aware than ever of ingredients in their food and their properties, and an increasing number of consumers are seeing food as a medicine. For this reason, dietary supplements stand out as one of the fastest-growing healthcare categories. Consumer base expansion has led to an urgent need for researchers, dietitians, physicians, and regulators to broaden the scientific evidence on the efficacy and safety of a wide range of active ingredients found in food supplements, including CoQ10. This review intended to provide them with a breadth of evidence on CoQ10 efficacy, safety, and formulation challenges. However, further studies must be carried out in order to clarify the role of CoQ10 and the optimal therapeutic regimen in the management of different health conditions. Additional investigation on physicochemical properties, pharmacokinetics, stability, and efficacy is also needed to deepen the knowledge on CoQ10 and to allow formulators to improve CoQ10 properties by means of different techniques. This is especially relevant since solubility, but especially stability and bioavailability concerns hinder its use in food supplements and medicinal products. For this reason, further research is needed to overcome these issues. Finally, although there is insufficient evidence to conclude its efficacy on different therapeutic indications, it is worth highlighting that CoQ10 supplementation is safe and well-tolerated at doses much higher than usual, with few drug interactions and minor side effects. However, people with certain health conditions and under treatment should consult with a health care professional before using CoQ10.
