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Pharmaceutics 2018, 10(3), 90; https://doi.org/10.3390/pharmaceutics10030090

Bioavailability of Eurycomanone in Its Pure Form and in a Standardised Eurycoma longifolia Water Extract

1
Herbal Medicine Research Centre, Institute for Medical Research, Jalan Pahang, Kuala Lumpur 50588, Malaysia
2
Aurigene Discovery Technologies Limited, Electronic City, Hosur Road, Bangalore 560100, Karmataka, India
3
Medical Resource Research Centre, Institute for Medical Research, Jalan Pahang, Kuala Lumpur 50588, Malaysia
*
Author to whom correspondence should be addressed.
Received: 22 May 2018 / Revised: 19 June 2018 / Accepted: 20 June 2018 / Published: 11 July 2018
(This article belongs to the Special Issue Drug Metabolism, Pharmacokinetics and Bioanalysis)
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Abstract

Eurycoma longifolia is one of the commonly consumed herbal preparations and its major chemical compound, eurycomanone, has been described to have antimalarial, antipyretic, aphrodisiac, and cytotoxic activities. Today, the consumption of E. longifolia is popular through the incorporation of its extract in food items, most frequently in drinks such as tea and coffee. In the current study, the characterisation of the physicochemical and pharmacokinetic (PK) attributes of eurycomanone were conducted via a series of in vitro and in vivo studies in rats and mice. The solubility and chemical stability of eurycomanone under the conditions of the gastrointestinal tract environment were determined. The permeability of eurycomanone was investigated by determining its distribution coefficient in aqueous and organic environments and its permeability using the parallel artificial membrane permeability assay system and Caco-2 cultured cells. Eurycomanone’s stability in plasma and its protein-binding ability were measured by using an equilibrium dialysis method. Its stability in liver microsomes across species (mice, rat, dog, monkey, and human) and rat liver hepatocytes was also investigated. Along with the PK evaluations of eurycomanone in mice and rats, the PK parameters for the Malaysian Standard (MS: 2409:201) standardised water extract of E. longifolia were also evaluated in rats. Both rodent models showed that eurycomanone in both the compound form and extract form had a half-life of 0.30 h. The differences in the bioavailability of eurycomanone in the compound form between the rats (11.8%) and mice (54.9%) suggests that the PK parameters cannot be directly extrapolated to humans. The results also suggest that eurycomanone is not readily absorbed across biological membranes. However, once absorbed, the compound is not easily metabolised (is stable), hence retaining its bioactive properties, which may be responsible for the various reported biological activities. View Full-Text
Keywords: eurycomanone; Eurycoma longifolia; bioavailability; pharmacokinetic eurycomanone; Eurycoma longifolia; bioavailability; pharmacokinetic
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).
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Ahmad, N.; Samiulla, D.S.; Teh, B.P.; Zainol, M.; Zolkifli, N.A.; Muhammad, A.; Matom, E.; Zulkapli, A.; Abdullah, N.R.; Ismail, Z.; Syed Mohamed, A.F. Bioavailability of Eurycomanone in Its Pure Form and in a Standardised Eurycoma longifolia Water Extract. Pharmaceutics 2018, 10, 90.

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