Transdermal delivery of carnosine into equine skeletal muscle

Abstract

The dipeptide carnosine consists of β-alanine and L-histidine. It plays a major role in skeletal muscle metabolism, especially as an intracellular buffer and antioxidant. Increasing intramuscular carnosine has been shown to improve recovery from exercise and increase anaerobic threshold and time-to-exhaustion. Dietary supplementation with carnosine does not effectively increase intramuscular carnosine due to the presence of carnosinase in the blood. However, an effective transdermal delivery process could expediently increase intramuscular concentrations of carnosine. This study’s objective was to examine the efficacy of a transdermal system for delivering carnosine into the skeletal muscle of horses, using a randomised, placebo controlled, crossover study. Carnosine plus a proprietary transdermal delivery agent or the agent alone (placebo) were applied to the middle gluteal muscles of 10 Thoroughbred racehorses, and muscle biopsies were taken before and 30, 60, and 120 min after application. Muscle carnosine concentration was measured using an enzyme-linked immunosorbent assay. A two-way repeated measures analysis of variance was used to test for the main effects of time and treatment (placebo or carnosine) as well as an interaction between time and treatment. Independent F-tests examined the change in intramuscular carnosine levels from baseline to each time point (30, 60, and 120 min). There was a significant main effect of treatment (P=0.004), no significant main effect for time (P=0.18), and a non-significant interaction of treatment with time (P=0.08). Mean intramuscular carnosine concentrations increased from baseline to 120 min. Compared to concentrations following placebo application, carnosine was greater by ~35% at 30 min (P=0.002) and ~46% after 60 min (P=0.044), but not at 120 min (P=0.20). The results indicated that intramuscular carnosine can be increased using a transdermal delivery system within 60 min of application which could have important implications for the health of horses, and their capacity to perform and recover from physical activity.