Recent research finding
Enhancement of bioavailability of R-α lipoic acid by γ-cyclodextrin in human healthy volunteers

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*This research was done through collaboration with Kobe University and Tokyo University of Science, and reported in 31th Cyclodextrin Symposium (Shimane, Sep. 11~12, 2014).

Background

Our company have attractive technologies in functional food and personal care fields which raise the water solubility, stability and bioavailability of a functional ingredient by using the inclusion property of cyclodextrin (CD).

In spite of high anti-aging functions of R-α lipoic acid, its stability and bioavailability are fairly low. So some of health benefits of R-α lipoic acid can not be shown up easily. Recently, we succeeded the enhancement of bioavailability of R-α lipoic acid with γCD in rats (* please refer to the newest result of research "47th" of our homepage for details.). That effect was achieved through the stabilization of R-α lipoic acid by complexation with γCD. Therefore, we commercialized "R-α lipoic acid-γCD complex" as functional health food and cosmetics materials.

In this research, the bioavailability of R-α lipoic acid with γCD was also examined in human healthy volunteers.

Health benefits of R-α lipoic acid

Study design

*This study was approved by the ethics committees of Kobe university.

single-dose crossover comparative bioavailability trial consisted of two studies (Study 1 and Study 2) was conducted.

<Human subject> Healthy 6 males aged 20-45 years
<Test material> R-α lipoic acid -γCD :6g (containing 600mg of R-α lipoic acid) / dose
<Comparative material> R-α lipoic acid : 600mg /dose

<Collection points of blood>

Result:Effect of γCD on the bioavailability R-α lipoic acid

<Fig.1>
Plasma concentration time-profiles of R-α lipoic acid in human healthy volunteers after oral supplementation (n=6,mean±S.D.)

Table1. Effect of γCD on the bioavailability R-α lipoic acid in human (n=6,mean±S.D.)

  Cmax (ng/mL) AUC0→180 min
(ng・min/mL)
Tmax (min) T1/2 (min)
R-α lipoic acid Mean 1678.3 78043.6 20.8 38.9
SD 1008.9 43459.9 10.7 12.2
R-α lipoic acid-γCD Mean 4101.9** 195884.1** 17.5 23.3
SD 959.3 17667.6 6.1 10.3

The bioavailability of R-α lipoic acid was enhanced by complexation with γCD.

Conclusion

The bioavailability of R-α lipoic acid was enhanced by complexation with γCD in not only rats but also human healthy volunteers.

Any adverse effects were not shown by the single-dose of R-α lipoic acid-γCD complex.

R-α lipoic acid-γCD complex is prospective as an excellent anti-aging functional ingredient.