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Strawberry Decreases Intraluminal and Intestinal Wall Hydrolysis of Testosterone Undecanoate

1
College of Pharmacy, University of Anbar, Ramadi 31001, Iraq
2
School of Pharmacy, University of Nottingham, Nottingham NG7 2RD, UK
*
Author to whom correspondence should be addressed.
Molecules 2021, 26(1), 233; https://doi.org/10.3390/molecules26010233
Received: 18 November 2020 / Revised: 26 December 2020 / Accepted: 31 December 2020 / Published: 5 January 2021
Male hypogonadism is often treated by testosterone (T) replacement therapy such as oral administration of the ester prodrug, testosterone undecanoate (TU). However, the systemic exposure to T following oral TU is very low due to esterase-mediated metabolism, particularly in the small intestine. The aim of this work was to examine the esterase-inhibitory effect of natural fruit extract of strawberry (STW) on the intestinal degradation of TU as a potential approach to increasing the oral bioavailability of T. Herein, the hydrolysis of TU was assessed in fasted state simulated intestinal fluid with added esterase activity (FaSSIF/ES) and Caco-2 cell homogenates in the presence of STW extract. It is noteworthy that STW substantially inhibited the degradation of TU in FaSSIF/ES and Caco-2 cell homogenates at concentrations that could be achieved following oral consumption of less than one serving of STW fruit. This can significantly increase the fraction of unhydrolyzed TU in the intestinal lumen as well as in enterocytes. In addition, it was demonstrated that TU has high intestinal lymphatic transport potential as the association of TU with plasma-derived human chylomicrons was in the range of 84%. Therefore, oral co-administration of TU with STW could potentially increase the intestinal stability of TU and consequently the contribution of lymphatically delivered TU to the systemic exposure of T in vivo. View Full-Text
Keywords: testosterone undecanoate; FaSSIF; intestinal degradation; first-pass metabolism; strawberry testosterone undecanoate; FaSSIF; intestinal degradation; first-pass metabolism; strawberry
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MDPI and ACS Style

Zgair, A.; Dawood, Y.; Ibrahem, S.M.; Lee, J.B.; Feng, W.; Fischer, P.M.; Gershkovich, P. Strawberry Decreases Intraluminal and Intestinal Wall Hydrolysis of Testosterone Undecanoate. Molecules 2021, 26, 233. https://doi.org/10.3390/molecules26010233

AMA Style

Zgair A, Dawood Y, Ibrahem SM, Lee JB, Feng W, Fischer PM, Gershkovich P. Strawberry Decreases Intraluminal and Intestinal Wall Hydrolysis of Testosterone Undecanoate. Molecules. 2021; 26(1):233. https://doi.org/10.3390/molecules26010233

Chicago/Turabian Style

Zgair, Atheer, Yousaf Dawood, Suhaib M. Ibrahem, Jong B. Lee, Wanshan Feng, Peter M. Fischer, and Pavel Gershkovich. 2021. "Strawberry Decreases Intraluminal and Intestinal Wall Hydrolysis of Testosterone Undecanoate" Molecules 26, no. 1: 233. https://doi.org/10.3390/molecules26010233

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