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.
Highlights
Fatigue is defined as physical and/or mental weariness resulting in inability to maintain exercise at the same intensity, leading to deterioration in performance [1]
Menzies et al showed that RES treatment for nine weeks combined with exercise training could stimulate mitochondrial biogenesis [11]
We focused on the alleviation of physical fatigue, which is an important issue in the field of sports medicine
Summary
Fatigue is defined as physical and/or mental weariness resulting in inability to maintain exercise at the same intensity, leading to deterioration in performance [1]. Menzies et al showed that RES treatment for nine weeks combined with exercise training could stimulate mitochondrial biogenesis [11] These anti-fatigue effects of RES are positive, the pretreatment protocols are time-consuming, possibly due to the low bioavailability of RES. SNEDDS can improve the rate and extent of absorption, enhancing the bioavailability of lipophilic drugs. We hypothesized that the use of nano-formulation might improve the oral bioavailability and anti-fatigue efficiency of RES. The purpose of this study was to develop and characterize a RES-SNEDDS in order to enhance RES solubility and further improve RES oral bioavailability. This study investigated whether pretreatment with a single dose of the developed RES-SNEDDS enhances anti-fatigue effects and exercise performance in rats
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