Derivatised α‐tocopherol as α CoQ 10 carrier in a novel water‐soluble formulation

• Published in: BioFactors (Oxford) 2003-01, Vol.18 (1-4), p.173-183
• Main Authors: Sikorska, Marianna, Borowy‐Borowski, Henryk, Zurakowski, Bogdan, Roy Walker, P.
• Format: Article
• Language: English
• ISSN: 0951-6433; 1872-8081
• DOI: 10.1002/biof.5520180220

We have derivatised α‐tocopherol (vitamin E) to a water‐soluble polyoxyethanyl‐α ‐ tocopheryl sebacate (PTS) and discovered that it formed a non‐covalent complex with CoQ 10 at a molar ratio of 2:1 (PTS‐CoQ 10 ). This complex was water‐soluble and remained stable for extended periods of time. After oral delivery of the formulation into rats PTS was hydrolysed to vitamin E and elevated levels of both vitamin E and CoQ 10 in blood plasma were detected within 1 h. Thus, this aqueous formulation contains a combination of two potent antioxidants. The formulation's efficacy was tested against ischemic brain damage caused by a transient (8∼min) bilateral occlusion of the common carotid arteries in rats. The animals received PTS‐CoQ 10 by two intraperitoneal injections given immediately after ischemia and 3 h later and the brain damage was assessed up to 12 days post‐ischemia. A significant neuroprotection was observed in the CA1 hippocampal region, for example at 12 days approximately 50% of CA1 neurons were still alive in the treated animals versus less than 5% in the non‐treated group. Our data is consistent with previously published observations indicating the therapeutic potential of antioxidants for treatments of ischemia/reperfusion injuries and the formulation described here is particularly appropriate for the application in acute conditions, such as stroke or cardiac arrest.