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Int. J. Mol. Sci. 2017, 18(9), 1853; doi:10.3390/ijms18091853

Self-Nanoemulsifying Drug Delivery System for Resveratrol: Enhanced Oral Bioavailability and Reduced Physical Fatigue in Rats

1
School of Pharmacy, College of Pharmacy, Kaohsiung Medical University, 100, Shih-Chuan 1st Rd., Kaohsiung 80708, Taiwan
2
Department of Sports Medicine, Kaohsiung Medical University, 100, Shih-Chuan 1st Rd., Kaohsiung 80708, Taiwan
3
Department of Medical Research, College of Medicine, Kaohsiung Medical University Hospital, 100, Tzyou 1st Rd., Kaohsiung 80708, Taiwan
*
Authors to whom correspondence should be addressed.
Received: 29 June 2017 / Revised: 18 August 2017 / Accepted: 22 August 2017 / Published: 25 August 2017
(This article belongs to the Special Issue Natural and Semi-Synthetic Small Molecules in Drug Discovery)
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Abstract

Resveratrol (RES), a natural polyphenolic compound, exerts anti-fatigue activity, but its administration is complicated by its low water solubility. To improve RES bioavailability, this study developed a self-nanoemulsifying drug delivery system (SNEDDS) for RES and evaluated its anti-fatigue activity and rat exercise performance by measuring fatigue-related parameters, namely lactate, ammonia, plasma creatinine phosphokinase, and glucose levels and the swimming time to exhaustion. Through solubility and emulsification testing, the optimized SNEDDS composed of Capryol 90, Cremophor EL, and Tween 20 was developed; the average particle size in this formulation, which had favorable self-emulsification ability, was approximately 41.3 ± 4.1 nm. Pharmacokinetic studies revealed that the oral bioavailability of the optimized RES-SNEDDS increased by 3.2-fold compared with that of the unformulated RES-solution. Pretreatment using the RES-SNEDDS before exercise accelerated the recovery of lactate after exercise; compared with the vehicle group, the plasma ammonia level in the RES-SNEDDS group significantly decreased by 65.4%, whereas the glucose level significantly increased by approximately 1.8-fold. Moreover, the swimming time to exhaustion increased by 2.1- and 1.8-fold, respectively, compared with the vehicle and RES-solution pretreatment groups. Therefore, the developed RES-SNEDDS not only enhances the oral bioavailability of RES but may also exert anti-fatigue pharmacological effect. View Full-Text
Keywords: resveratrol; self-nanoemulsifying drug delivery system; anti-fatigue resveratrol; self-nanoemulsifying drug delivery system; anti-fatigue
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Yen, C.-C.; Chang, C.-W.; Hsu, M.-C.; Wu, Y.-T. Self-Nanoemulsifying Drug Delivery System for Resveratrol: Enhanced Oral Bioavailability and Reduced Physical Fatigue in Rats. Int. J. Mol. Sci. 2017, 18, 1853.

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