International Journal of Healthcare Sciences ISSN 2348-5728 (Online) Vol. 8, Issue 1, pp: (250-254), Month: April 2020 - September 2020, Available at: www.researchpublish.com
20-Hydroxyecdysone’s Cyclodextrin Complex: A Novel Anabolic Phytosteroid (APS)? Victor Chiruta1 1
Faculty of Health Science, University of South Australia, Adelaide, Australia
Abstract: 20-Hydroxyecdysone (20-HE) is currently undergoing a Phase 2 Clinical Trial for the treatment of sarcopenia. 20-HE is also currently being investigated by the World Anti-Doping Agency (WADA) as an anabolic agent. There are promising in vitro and in vivo results for 20-HE’s anabolic effect on muscles. However, 20-HE is molecularly a steroid, thus having relatively poor water solubility and poor human oral bioavailability. Cyclodextrins (CDs) are being used in pharmaceutics to improve the water solubility and oral bioavailability of lipophilic compounds. This paper explores 20-HE’s pharmacodynamics and pharmacokinetics, with a particular interest on how the 20-HE-CD complex can improve the oral bioavailability of 20-HE. Consequently, making 20HE-CD a novel anabolic phytosteroid (APS). Keywords: 20-hydroxyecdysone, ecdysteroid, cyclodextrin, phytosteroid.
I. INTRODUCTION 20-HE is an ecdysteroid primarily isolated from the plant Cyanotis arachnoidea[1], but also present in spinach[2] and quinoa[3]. In the 1980s, ecdysteroids were suspected to be used by Russian weightlifters in the Olympics [4]. This led to a study in 2000, comparing the anabolic efficacy of ecdysteroids to a group of anabolic androgenic steroids (AAS) known as steranabols[5]. Following the positive results, in 2015, 20-HE was compared for anabolic efficacy in vitro and in vivo with a range of endogenous and exogenous anabolic compounds [4]. 20-HE had greater anabolic effects on muscle than the compared compounds. In 2015, a non-clinical study found that 20-HE prevented catabolic expression in cartilage[6]. In 2016, another non-clinical study discovered that 20-HE combats muscle atrophy[7]. In 2016, WADA undertook an investigation to potentially prohibit this compound under the schedule of ‘S2.1 Other Anabolic Agents’[8]. 20-HE’s previous use in the olympics, its promising non-clinical results, and the WADA investigation into its use as an anabolic agent gives the rationale for the clinical trials of 20-HE, for the treatment of muscular degenerative diseases[9]. 20-HE deserves examination as a potential APS.
II. PHARMACODYNAMICS A. Chemical Structure 20-HE
TP
Fig. 1. Structure of 20-HE and testosterone propionate (TP). 20-HE is a structural analogue of TP.
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