Formation of CoQ10 reduced form by mixing CoQ10 oxidized form γCD complex and vitamin C in powder

Uekaji, Yukiko; Nakata, Daisuke; Shiga, Hirokazu; Jo, Ayako; Tachi, Iwao; Fukumi, Hiroshi; Urano, Akihito; Terao, Keiji

doi:10.1007/s10847-010-9912-3

Cited by 8 publications

(6 citation statements)

References 6 publications

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“…CoQ10 in pharmaceutical products undergo appreciable degradation (Uekaji et al, 2010). The formulation strategies adopted to promote thermal and photostabilization CoQ10 include: nanoliposomes encapsulation (Xia et al, 2006), selfemulsifiable systems (Nazzal et al, 2002c) (using limonene rather than essential oils with a capsule formulation) , solid dispersion formation (Nazzal et al, 2002a), addition of ascorbic acid and chelation by EDTA (Kommuru et al, 1999) and cyclodextrin (CD) complexation (Prosek et al, 2008).…”

Section: Strategies For Surmounting Stability Barriersmentioning

confidence: 99%

“…The stability CoQ10-CDs complexes and vitamin C co-formulations was investigated at drastic storage conditions: 60 C and 75% relative humidity. The free radical scavenging efficacy was tested using 1,1-diphenyl-2-picrylhydrazyl (DPPH) (Uekaji et al, 2010). Analysis of the oxidized and reduced CoQ10 by high-performance liquid chromatography (HPLC) revealed a significantly more ubiquinol (80%) formed in the g-CD inclusion complex compared to the noncomplexed CoQ10 (only 30%).…”

Section: Complexesmentioning

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 Stability Barriersmentioning

confidence: 99%

Section: Complexesmentioning

confidence: 99%

Strategies for oral delivery and mitochondrial targeting of CoQ10

Zaki

2014

Drug Delivery

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“…The in vitro antioxidative ability was evaluated using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay method [17] with slight modifications. In brief, 200 µmol/L of DPPH solution was prepared in 75% ethanol before use and kept away from light.…”

Section: In Vitro Antioxidant Abilitymentioning

confidence: 99%

Coenzyme Q10-Polyethylene Glycol Monostearate Nanoparticles: An Injectable Water-Soluble Formulation

Banshoya¹,

Nakamura²,

Tanaka³

et al. 2020

Antioxidants

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Therapeutic applications of coenzyme Q10 (CoQ10) are greatly limited by its lack of solubility in aqueous media. In this study, polyethylene glycol monostearate (stPEG) was used to construct micelles containing CoQ10 as a new formulation. The micellar formulations (stPEG/CoQ10) were prepared using five types of stPEG with 10, 25, 40, 55, and 140 PEG repeat units, respectively. The micellar preparation was simple, consisting of only stPEG and CoQ10. Next, we compared the physical properties and blood circulation of these micelles. The CoQ10 load of this formulation was approximately 15 w/w%. Based on the dynamic light scattering method, the average molecular size of the stPEG/CoQ10 micelles was approximately 15 to 60 nm. The zeta potentials of these micelles were approximately −10 to −25 mV. The micelles using stPEG25, 40, and 55 demonstrated high solubility in water. Furthermore, these micelles had in vitro antioxidant activity. On comparing the blood circulation of micelles using stPEG25, 40, 55, and 140, micelles using stPEG55 had a significantly higher circulation in blood. The stPEG55/CoQ10 micelle demonstrated a protective effect against acetaminophen-induced liver injury in mice. In conclusion, these data indicate that the intravenous administration of the stPEG/CoQ10 micellar aqueous formulation is of great value against oxidant stress.

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“…An additional advantage of rCoQ10 supplementation is its genuine antioxidant activity, while oCoQ10 requires enzymatic reduction before acting as an antioxidant [43]. The enzymatic activities of coenzyme Q reductases change according to physiological and pathological conditions and decrease with age, use of some medications, and after intense physical activities [44][45][46]. Supplementation with rCoQ10, therefore, seems advantageous over oCoQ10, especially in the above-mentioned cases.…”

Section: Introductionmentioning

confidence: 99%

“…The stability issues associated with CoQ10 are more pronounced with the use of rCoQ10, which is quickly oxidized, when in contact with air or after light exposure [44,47,48]. Providing quality rCoQ10 products is therefore quite demanding in terms of obtaining a stable formulation [28,47].…”

Section: Introductionmentioning

confidence: 99%

Stability of Reduced and Oxidized Coenzyme Q10 in Finished Products

2021

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The efficiency of coenzyme Q10 (CoQ10) supplements is closely associated with its content and stability in finished products. This study aimed to provide evidence-based information on the quality and stability of CoQ10 in dietary supplements and medicines. Therefore, ubiquinol, ubiquinone, and total CoQ10 contents were determined by a validated HPLC-UV method in 11 commercial products with defined or undefined CoQ10 form. Both forms were detected in almost all tested products, resulting in a total of CoQ10 content between 82% and 166% of the declared. Ubiquinol, ubiquinone, and total CoQ10 stability in these products were evaluated within three months of accelerated stability testing. Ubiquinol, which is recognized as the less stable form, was properly stabilized. Contrarily, ubiquinone degradation and/or reduction were observed during storage in almost all tested products. These reactions were also detected at ambient temperature within the products’ shelf-lives and confirmed in ubiquinone standard solutions. Ubiquinol, generated by ubiquinone reduction with vitamin C during soft-shell capsules’ storage, may lead to higher bioavailability and health outcomes. However, such conversion and inappropriate content in products, which specify ubiquinone, are unacceptable in terms of regulation. Therefore, proper CoQ10 stabilization through final formulations regardless of the used CoQ10 form is needed.

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Formation of CoQ10 reduced form by mixing CoQ10 oxidized form γCD complex and vitamin C in powder

Cited by 8 publications

References 6 publications

Strategies for oral delivery and mitochondrial targeting of CoQ10

Strategies for oral delivery and mitochondrial targeting of CoQ10

Coenzyme Q10-Polyethylene Glycol Monostearate Nanoparticles: An Injectable Water-Soluble Formulation

Stability of Reduced and Oxidized Coenzyme Q10 in Finished Products

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