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 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.
Graduate School of Medicine, Kobe University, Kobe 650-0017, Japan. naoko.ikuta@people.kobe-u.ac.jp.
Naoko
N
Ikuta
Graduate School of Medicine, Kobe University, Kobe 650-0017, Japan. hinako.okamoto@cyclochem.com.|CycloChem Bio Co., Ltd., Kobe 650-0047, Japan. hinako.okamoto@cyclochem.com.
Hinako
H
Okamoto
CycloChem Bio Co., Ltd., Kobe 650-0047, Japan. takahiro.furune@cyclochem.com.
Takahiro
T
Furune
CycloChem Bio Co., Ltd., Kobe 650-0047, Japan. yukiko.uekaji@cyclochem.com.
Yukiko
Y
Uekaji
Graduate School of Medicine, Kobe University, Kobe 650-0017, Japan. keiji.terao@cyclochem.com.|CycloChem Bio Co., Ltd., Kobe 650-0047, Japan. keiji.terao@cyclochem.com.
Keiji
K
Terao
Department of Biopharmaceutics, Faculty of Pharmaceutical Science, Tokyo University of Science, Chiba 278-8510, Japan. j3b13702@ed.tus.ac.jp.
Ryota
R
Uchida
Department of Biopharmaceutics, Faculty of Pharmaceutical Science, Tokyo University of Science, Chiba 278-8510, Japan. gan.ln284@gmail.com.
Kosuke
K
Iwamoto
Department of Biopharmaceutics, Faculty of Pharmaceutical Science, Tokyo University of Science, Chiba 278-8510, Japan. miyajima@my-pharm.ac.jp.
Atsushi
A
Miyajima
Department of Biopharmaceutics, Faculty of Pharmaceutical Science, Tokyo University of Science, Chiba 278-8510, Japan. hirotas5@rs.noda.tus.ac.jp.
Takashi
T
Hirota
Graduate School of Medicine, Kobe University, Kobe 650-0017, Japan. nori@med.kobe-u.ac.jp.
Norihiro
N
Sakamoto
D000328:Adult; D000975:Antioxidants / Q000008:administration & dosage / Q000493:pharmacokinetics; D001682:Biological Availability; D004338:Drug Combinations; D064368:Healthy Volunteers; D006801:Humans; D008297:Male; D008063:Thioctic Acid / Q000008:administration & dosage* / Q000009:adverse effects / Q000737:chemistry / Q000493:pharmacokinetics*; D047408:gamma-Cyclodextrins / Q000008:administration & dosage* / Q000009:adverse effects / Q000737:chemistry / Q000493:pharmacokinetics*
D000975:Antioxidants; D004338:Drug Combinations; D047408:gamma-Cyclodextrins; D008063:Thioctic Acid
R-α-lipoic acid; bioavailability; clinical study; cyclodextrin; healthy volunteers; oral administration; pharmacokinetics