Bioavailability of an R-[alpha]-Lipoic Acid/[gamma]-Cyclodextrin Complex in Healthy Volunteers

R-[alpha]-lipoic acid (R-LA) is a cofactor of mitochondrial enzymes and a very strong antioxidant. R-LA is available as a functional food ingredient but is unstable against heat or acid. Stabilized R-LA was prepared through complexation with [gamma]-cyclodextrin (CD), yielding R-LA/CD. R-LA/CD was o...

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Bibliographic Details
Published in:International journal of molecular sciences 2016-06, Vol.17 (6), p.949
Main Authors: Ikuta, Naoko, Okamoto, Hinako, Furune, Takahiro, Uekaji, Yukiko, Terao, Keiji, Uchida, Ryota, Iwamoto, Kosuke, Miyajima, Atsushi, Hirota, Takashi, Sakamoto, Norihiro
Format: Article
Language:English
Subjects:
Antioxidants
Bioavailability
Enzymes
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Summary:R-[alpha]-lipoic acid (R-LA) is a cofactor of mitochondrial enzymes and a very strong antioxidant. R-LA is available as a functional food ingredient but is unstable against heat or acid. Stabilized R-LA was prepared through complexation with [gamma]-cyclodextrin (CD), yielding R-LA/CD. R-LA/CD was orally administered to six healthy volunteers and showed higher plasma levels with an area under the plasma concentration-time curve that was 2.5 times higher than that after oral administration of non-complexed R-LA, although the time to reach the maximum plasma concentration and half-life did not differ. Furthermore, the plasma glucose level after a single oral administration of R-LA/CD or R-LA was not affected and no side effects were observed. These results indicate that R-LA/CD could be easily absorbed in the intestine. In conclusion, [gamma]-CD complexation is a promising technology for delivering functional but unstable ingredients like R-LA.
ISSN:1661-6596
1422-0067
DOI:10.3390/ijms17060949