Bioavailability of coenzyme Q10 loaded in an oleogel formulation for oral therapy : Comparison with a commercial-grade solid formulation
Copyright © 2020 Elsevier B.V. All rights reserved..
Coenzyme Q10 (CoQ10) is essential in mitochondrial bioenergetics and is a potent endogenous antioxidant. Low CoQ10 levels are associated with neurodegenerative, metabolic, muscular and cardiovascular disorders. Early treatment with high doses (5-50 mg/kg/day) demonstrated to limit the onset and progression of neuropathology. Recently, we developed an oleogel matrix able to support a high dose of oil-dissolved CoQ10, easy to swallow by CoQ10-deficient patients who suffer from secondary dysphagia. In the present study, we evaluated the bioavailability of oleogel-dissolved CoQ10 and plasma antioxidant status in healthy adults in single-dose and repeated-dose studies. The single-dose study demonstrated that, in terms of CoQ10 bioavailability, 1 g CoQ10/5g oleogel-disk was equivalent to the solid form (1 g CoQ10/three 00-size-capsules), whereas the repeated-dose study (14-days-administration) demonstrated a significantly higher increase in plasma CoQ10 when administered through the oleogel, which could be compatible with the levels necessary to achieve an adequate therapeutic response. Also, a trend to a higher plasma apparent half-life (greater than24 h) was observed for the oleogel-loaded-CoQ10. In conclusion, the oleogel matrix does not compromise the oil-dissolved CoQ10 bioavailability and can prevent the non-adherence to this vital supplementation in patients with high CoQ10 requirements. No significant variation in the plasma antioxidant status (vitamins A, E and C, glutathione and TBARs) was observed.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2020 |
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| Erschienen: |
2020 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:582 |
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| Enthalten in: |
International journal of pharmaceutics - 582(2020) vom: 30. Mai, Seite 119315 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Ehrenhaus Masotta, Natalia [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Completed 18.02.2021 Date Revised 18.02.2021 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1016/j.ijpharm.2020.119315 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM308682238 |
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| 100 | 1 | |a Ehrenhaus Masotta, Natalia |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a Bioavailability of coenzyme Q10 loaded in an oleogel formulation for oral therapy |b Comparison with a commercial-grade solid formulation |
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| 500 | |a Date Revised 18.02.2021 | ||
| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Copyright © 2020 Elsevier B.V. All rights reserved. | ||
| 520 | |a Coenzyme Q10 (CoQ10) is essential in mitochondrial bioenergetics and is a potent endogenous antioxidant. Low CoQ10 levels are associated with neurodegenerative, metabolic, muscular and cardiovascular disorders. Early treatment with high doses (5-50 mg/kg/day) demonstrated to limit the onset and progression of neuropathology. Recently, we developed an oleogel matrix able to support a high dose of oil-dissolved CoQ10, easy to swallow by CoQ10-deficient patients who suffer from secondary dysphagia. In the present study, we evaluated the bioavailability of oleogel-dissolved CoQ10 and plasma antioxidant status in healthy adults in single-dose and repeated-dose studies. The single-dose study demonstrated that, in terms of CoQ10 bioavailability, 1 g CoQ10/5g oleogel-disk was equivalent to the solid form (1 g CoQ10/three 00-size-capsules), whereas the repeated-dose study (14-days-administration) demonstrated a significantly higher increase in plasma CoQ10 when administered through the oleogel, which could be compatible with the levels necessary to achieve an adequate therapeutic response. Also, a trend to a higher plasma apparent half-life (greater than24 h) was observed for the oleogel-loaded-CoQ10. In conclusion, the oleogel matrix does not compromise the oil-dissolved CoQ10 bioavailability and can prevent the non-adherence to this vital supplementation in patients with high CoQ10 requirements. No significant variation in the plasma antioxidant status (vitamins A, E and C, glutathione and TBARs) was observed | ||
| 650 | 4 | |a Comparative Study | |
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Randomized Controlled Trial | |
| 650 | 4 | |a Coenzyme Q10 (PubChem CID: 9962735) | |
| 650 | 4 | |a Dysphagia | |
| 650 | 4 | |a Glutathione (PubChem CID: 124886) | |
| 650 | 4 | |a Oleogel | |
| 650 | 4 | |a Oral therapy | |
| 650 | 4 | |a Pharmacokinetic | |
| 650 | 4 | |a Relative bioavailability | |
| 650 | 4 | |a Ubiquinone | |
| 650 | 4 | |a Vitamin A (PubChem CID: 445354) | |
| 650 | 4 | |a Vitamin C (PubChem CID: 54670067) | |
| 650 | 4 | |a Vitamin E (PubChem CID: 14985) | |
| 650 | 7 | |a Antioxidants |2 NLM | |
| 650 | 7 | |a Biomarkers |2 NLM | |
| 650 | 7 | |a Capsules |2 NLM | |
| 650 | 7 | |a Drug Carriers |2 NLM | |
| 650 | 7 | |a Organic Chemicals |2 NLM | |
| 650 | 7 | |a oleogels |2 NLM | |
| 650 | 7 | |a Ubiquinone |2 NLM | |
| 650 | 7 | |a 1339-63-5 |2 NLM | |
| 650 | 7 | |a coenzyme Q10 |2 NLM | |
| 650 | 7 | |a EJ27X76M46 |2 NLM | |
| 700 | 1 | |a Höcht, Christian |e verfasserin |4 aut | |
| 700 | 1 | |a Contin, Mario |e verfasserin |4 aut | |
| 700 | 1 | |a Lucangioli, Silvia |e verfasserin |4 aut | |
| 700 | 1 | |a Rojas, Ana M |e verfasserin |4 aut | |
| 700 | 1 | |a Tripodi, Valeria P |e verfasserin |4 aut | |
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