Coenzyme Q10 oral bioavailability: effect of formulation type

Barakat, Abdulwahab; Shegokar, Ranjita; Dittgen, M; Müller, Rainer H.

doi:10.1007/s40005-013-0101-4

Cited by 28 publications

(17 citation statements)

References 132 publications

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“…Palamaluka (2004b) reported high CoQ10 permeability values through Caco-2 cell monolayer and categorized it as a Class II compound in the BCS. However, this categorization is questionable based on the extremely low absorption (Fa% 51%) (Barakat et al, 2013) and apparent permeability coefficient (P app ) values (51 Â 10 À7 cm/s) of CoQ10 (Xia et al, 2009). As such, CoQ10 should be sorted as a Class IV compound.…”

Section: Strategies For Surmounting Permeability Barriersmentioning

confidence: 99%

“…With such essential role, it steers cellular machinery and synthesis (Baker & Tarnopolsky, 2003). To the best of our knowledge, previous reviews on this wonder nutrient ($97 reviews) mainly focused on the therapeutic uses (Kawasaki, 1992;Palazzoni et al, 1997;Soja & Mortensen, 1997;Al-Hasso, 2001;Gürkan & Bozdaǧ-Dündar, 2005;DiMauro et al, 2006;Frankovic, 2006;Pepe et al, 2007;Singh et al, 2007;Storch, 2007;Dos Santos et al, 2009;Spindler et al, 2009;Quinzii & Hirano, 2010;Janicki & Buzała, 2012;Cordero et al, 2013), formulations Villalba et al, 2010;Bank et al, 2011;Ž mitek et al, 2011;Barakat et al, 2013), clinical or preclinical trials (Mortensen et al, 1990;Hargreaves et al, 2005;Marcoff & Thompson, 2007;Littarru & Tiano, 2010), pharmacokinetics Ž mitek & Ž mitek, 2009;Villalba et al, 2010;Ž mitek et al, 2011) as well as deficiency and its consequences (Hargreaves, 2003;Naini et al, 2006;Land et al, 2007;Quinzii et al, 2007;Quinzii & Hirano, 2010;Trevisson et al, 2011). Nevertheless, oral absorption and targeting to mitochondria remain a major challenge for optimum antioxidant effect and hence need to be evaluated in light of the multiplicity of barriers that hinder the effective delivery of CoQ10 as a nutraceutical product.…”

Section: Introductionmentioning

confidence: 99%

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Strategies for oral delivery and mitochondrial targeting of CoQ10

Zaki

2014

Drug Delivery

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Coenzyme Q10 (CoQ10), also known as ubiquinone or ubidecarenone, is a powerful, endogenously produced, intracellularly existing lipophilic antioxidant. It combats reactive oxygen species (ROS) known to be responsible for a variety of human pathological conditions. Its target site is the inner mitochondrial membrane (IMM) of each cell. In case of deficiency and/or aging, CoQ10 oral supplementation is warranted. However, CoQ10 has low oral bioavailability due to its lipophilic nature, large molecular weight, regional differences in its gastrointestinal permeability and involvement of multitransporters. Intracellular delivery and mitochondrial target ability issues pose additional hurdles. To maximize CoQ10 delivery to its biopharmaceutical target, numerous approaches have been undertaken. The review summaries the current research on CoQ10 bioavailability and highlights the headways to obtain a satisfactory intracellular and targeted mitochondrial delivery. Unresolved questions and research gaps were identified to bring this promising natural product to the forefront of therapeutic agents for treatment of different pathologies.

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Section: Strategies For Surmounting Permeability Barriersmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Strategies for oral delivery and mitochondrial targeting of CoQ10

Zaki

2014

Drug Delivery

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“…In spite of having protective role against toxicities induced by xenobiotics, CoQ10 represents significant lipid solubility and low bioavailability that limit its clinical applications; therefore, higher doses are needed to be administered orally for clinical applications . It is worth noting that researches have achieved obvious therapeutic effectiveness in humans only in the long term and high dose CoQ10 administration, which forces researchers to seek strategies for overcoming these limitations…”

Section: Introductionmentioning

confidence: 99%

Protective effects of coenzyme Q10 nanoparticles on dichlorvos‐induced hepatotoxicity and mitochondrial/lysosomal injury

Eftekhari

Ahmadian

Azami

et al. 2017

Environmental Toxicology

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Development of biocompatible antioxidant nanoparticles for xenobiotic-induced liver disease treatment by oral or parenteral administration is of great interest in medicine. In the current study, we demonstrate the protective effects of coenzyme Q10 nanoparticles (CoQ10-NPs) on hepatotoxicity induced by dichlorvos (DDVP) as an organophosphate. Although CoQ10 is an efficient antioxidant, its poor bioavailability has limited the applications of this useful agent. First, CoQ10-NPs were prepared then characterized using dynamic light scattering (DLS) and transmission electron microscopy (TEM). In DDVP-treated and non-treated hepatocytes in the presence of CoQ10-NPs, cell viability, the level of reactive oxygen species (ROS), lipid peroxidation (LPO), mitochondrial membrane potential (MMP), lysosome membrane integrity, and cellular glutathione (GSH) content were measured. The prepared CoQ10-NPs were mono-dispersed and had narrow size distribution with average diameter of 54 nm. In the in vivo study, we evaluated the enzymes, which are involved in the antioxidant system for maintenance of normal liver function. In comparison to nonparticulate CoQ10, the CoQ10-NPs efficiently decreased the ROS formation, lipid peroxidation and cell death. Also, particulate form of CoQ10 improved MMP, GSH level and lysosome membrane integrity. In the in vivo, study, we revealed that CoQ10-NPs were better hepatoprotective than its nonparticulate form (P < .05). Altogether, we propose that the CoQ10-NPs have potential capability to be used as a therapeutic and prophylactic agent for poisoning that is induced by organophosphate agents, especially in the case of DDVP. Furthermore, these positive remarks make this nanoparticle amenable for the treatment of xenobiotic-induced liver diseases.

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“…However, while it used to be incorporated as a simple crystalline powder or dispersed in oil, different novel delivery systems have been recently tested to improve its bioavailability. Thus, different formulation approaches, such as self‐emulsified drug delivery systems, nanoemulsions, or cyclodextrin complexes, have been used and combined to improve CoQ10 bioavailability when incorporated into different pharmaceutical dosage forms (Barakat, Shegokar, Dittgen, & Müller, ; Schulz, Obermüller‐Jevic, Hasselwander, Bernhardt, & Biesalski, ). The suggested daily dose varies depending on the indication but is usually around 30 to 100 mg for healthy people, reaching up to 60 to 1,200 mg when used in some medical conditions (Pravst et al., ).…”

Section: Coq10 Supplementationmentioning

confidence: 99%

“…Solubilized formulas have shown higher absorption and bioavailability, and thus plasmatic levels were significantly higher when compared to nonsolubilized CoQ10 powder (Bhagavan & Chopra, ; Miles, ). For this reason, different formulation approaches including novel delivery systems such as self‐emulsified drug delivery systems (SEDDS), nanoemulsions, or cyclodextrin complexes have been tested to improve CoQ10 bioavailability when it is incorporated into softgels, capsules, and tablets (Barakat et al., ; Schulz et al., ). By way of example, different formulation approaches will be briefly reviewed below.…”

Section: Coq10 Supplementationmentioning

confidence: 99%

Coenzyme Q10 supplementation: Efficacy, safety, and formulation challenges

Arenas-Jal

Suñé-Negre

García-Montoya

2020

Comp Rev Food Sci Food Safe

142

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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 noncommunicable 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, dietary supplements category is growing fast, leading to an urgent need for dietitians, physicians, and policy makers 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 noncommunicable 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.

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Coenzyme Q10 oral bioavailability: effect of formulation type

Cited by 28 publications

References 132 publications

Strategies for oral delivery and mitochondrial targeting of CoQ10

Strategies for oral delivery and mitochondrial targeting of CoQ10

Protective effects of coenzyme Q10 nanoparticles on dichlorvos‐induced hepatotoxicity and mitochondrial/lysosomal injury

Coenzyme Q10 supplementation: Efficacy, safety, and formulation challenges

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