Bioavailability of an R-α-Lipoic Acid/γ-Cyclodextrin Complex in Healthy Volunteers
R-α-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 γ-cyclodextrin (CD), yielding R-LA/CD. R-LA/CD was orally admini...
Main Authors: | , , , , , , , , , |
---|---|
Format: | Article |
Language: | English |
Published: |
MDPI AG
2016-06-01
|
Series: | International Journal of Molecular Sciences |
Subjects: | |
Online Access: | http://www.mdpi.com/1422-0067/17/6/949 |
id |
doaj-0cf951f3e51f45e58506f4aad05a4aca |
---|---|
record_format |
Article |
spelling |
doaj-0cf951f3e51f45e58506f4aad05a4aca2020-11-24T23:53:11ZengMDPI AGInternational Journal of Molecular Sciences1422-00672016-06-0117694910.3390/ijms17060949ijms17060949Bioavailability of an R-α-Lipoic Acid/γ-Cyclodextrin Complex in Healthy VolunteersNaoko Ikuta0Hinako Okamoto1Takahiro Furune2Yukiko Uekaji3Keiji Terao4Ryota Uchida5Kosuke Iwamoto6Atsushi Miyajima7Takashi Hirota8Norihiro Sakamoto9Graduate School of Medicine, Kobe University, Kobe 650-0017, JapanGraduate School of Medicine, Kobe University, Kobe 650-0017, JapanCycloChem Bio Co., Ltd., Kobe 650-0047, JapanCycloChem Bio Co., Ltd., Kobe 650-0047, JapanGraduate School of Medicine, Kobe University, Kobe 650-0017, JapanDepartment of Biopharmaceutics, Faculty of Pharmaceutical Science, Tokyo University of Science, Chiba 278-8510, JapanDepartment of Biopharmaceutics, Faculty of Pharmaceutical Science, Tokyo University of Science, Chiba 278-8510, JapanDepartment of Biopharmaceutics, Faculty of Pharmaceutical Science, Tokyo University of Science, Chiba 278-8510, JapanDepartment of Biopharmaceutics, Faculty of Pharmaceutical Science, Tokyo University of Science, Chiba 278-8510, JapanGraduate School of Medicine, Kobe University, Kobe 650-0017, JapanR-α-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 γ-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, γ-CD complexation is a promising technology for delivering functional but unstable ingredients like R-LA.http://www.mdpi.com/1422-0067/17/6/949R-α-lipoic acidcyclodextrinbioavailabilitypharmacokineticshealthy volunteersclinical studyoral administration |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
Naoko Ikuta Hinako Okamoto Takahiro Furune Yukiko Uekaji Keiji Terao Ryota Uchida Kosuke Iwamoto Atsushi Miyajima Takashi Hirota Norihiro Sakamoto |
spellingShingle |
Naoko Ikuta Hinako Okamoto Takahiro Furune Yukiko Uekaji Keiji Terao Ryota Uchida Kosuke Iwamoto Atsushi Miyajima Takashi Hirota Norihiro Sakamoto Bioavailability of an R-α-Lipoic Acid/γ-Cyclodextrin Complex in Healthy Volunteers International Journal of Molecular Sciences R-α-lipoic acid cyclodextrin bioavailability pharmacokinetics healthy volunteers clinical study oral administration |
author_facet |
Naoko Ikuta Hinako Okamoto Takahiro Furune Yukiko Uekaji Keiji Terao Ryota Uchida Kosuke Iwamoto Atsushi Miyajima Takashi Hirota Norihiro Sakamoto |
author_sort |
Naoko Ikuta |
title |
Bioavailability of an R-α-Lipoic Acid/γ-Cyclodextrin Complex in Healthy Volunteers |
title_short |
Bioavailability of an R-α-Lipoic Acid/γ-Cyclodextrin Complex in Healthy Volunteers |
title_full |
Bioavailability of an R-α-Lipoic Acid/γ-Cyclodextrin Complex in Healthy Volunteers |
title_fullStr |
Bioavailability of an R-α-Lipoic Acid/γ-Cyclodextrin Complex in Healthy Volunteers |
title_full_unstemmed |
Bioavailability of an R-α-Lipoic Acid/γ-Cyclodextrin Complex in Healthy Volunteers |
title_sort |
bioavailability of an r-α-lipoic acid/γ-cyclodextrin complex in healthy volunteers |
publisher |
MDPI AG |
series |
International Journal of Molecular Sciences |
issn |
1422-0067 |
publishDate |
2016-06-01 |
description |
R-α-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 γ-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, γ-CD complexation is a promising technology for delivering functional but unstable ingredients like R-LA. |
topic |
R-α-lipoic acid cyclodextrin bioavailability pharmacokinetics healthy volunteers clinical study oral administration |
url |
http://www.mdpi.com/1422-0067/17/6/949 |
work_keys_str_mv |
AT naokoikuta bioavailabilityofanralipoicacidgcyclodextrincomplexinhealthyvolunteers AT hinakookamoto bioavailabilityofanralipoicacidgcyclodextrincomplexinhealthyvolunteers AT takahirofurune bioavailabilityofanralipoicacidgcyclodextrincomplexinhealthyvolunteers AT yukikouekaji bioavailabilityofanralipoicacidgcyclodextrincomplexinhealthyvolunteers AT keijiterao bioavailabilityofanralipoicacidgcyclodextrincomplexinhealthyvolunteers AT ryotauchida bioavailabilityofanralipoicacidgcyclodextrincomplexinhealthyvolunteers AT kosukeiwamoto bioavailabilityofanralipoicacidgcyclodextrincomplexinhealthyvolunteers AT atsushimiyajima bioavailabilityofanralipoicacidgcyclodextrincomplexinhealthyvolunteers AT takashihirota bioavailabilityofanralipoicacidgcyclodextrincomplexinhealthyvolunteers AT norihirosakamoto bioavailabilityofanralipoicacidgcyclodextrincomplexinhealthyvolunteers |
_version_ |
1725470782031659008 |