Non-clinical pharmacokinetic behavior of ginsenosides

Abstract

Ginsenosides, the major active ingredients of ginseng and other plants of the genus Panax, have been used as natural medicines in the East for a long time; in addition, their popularity in the West has increased owing to their various beneficial pharmacological effects. There is therefore a wealth of literature regarding the pharmacological effects of ginsenosides. In contrast, there are few comprehensive studies that investigate their pharmacokinetic behaviors. This is because ginseng contains the complicated mixture of herbal materials as well as thousands of constituents with complex chemical properties, and ginsenosides undergo multiple biotransformation processes after administration. This is a significant issue as pharmacokinetic studies provide crucial data regarding the efficacy and safety of compounds. Moreover, there have been many difficulties in the development of the optimal dosage regimens of ginsenosides and the evaluation of their interactions with other drugs. Therefore, this review details the pharmacokinetic properties and profiles of ginsenosides determined in various animal models administered through different routes of administration. Such information is valuable for designing specialized delivery systems and determining optimal dosing strategies for ginsenosides.

Keywords: Bioavailability; Ginsenosides; Pharmacokinetic; Protopanaxadiol; Protopanaxatriol.

Fig. 1

Therapeutic effects of ginsenosides and effective organs.

Fig. 2

Chemical structures of protopanaxadiol (PPD)- and protopanaxatriol (PPT)-type ginsenosides and the main metabolic pathways of PPD and PPT groups. “Arrow (→)” denotes metabolic changes of ginsenosides in vivo.