Orally bioavailable standardized derivatives in sports nutrition

Orally bioavailable standardized derivatives in sports nutrition

Special focus on recovery after intense physical activity

Paolo Morazzoni, Antonella Riva

It is difficult for both professional athletes and individuals undertaking regular physical activity to achieve the correct balance between the benefits of and damages caused by exercise. Indeed, an increasing number of physically active people in developed countries are at risk of developing overtraining syndrome (OTS) – like condition. Major symptoms include parasympathetic (e.g., fatigue, depression) and sympathetic (e.g., insomnia, irritability, restlessness) alterations as well as anxiety, weight loss and lack of mental concentration.

The current interpretation of this pathophysiological condition is based on an inflammatory/oxidative hypothesis where a local acute inflammatory event (micro-trauma), generated by mixed eccentric/concentric muscle and joint activity, develops into a local chronic event and finally a systemic inflammatory response. This inflammatory status is marked by a clear increase in inflammatory and catabolic cytokines such as IL-1β, IL-6 and TNF-α, reduced muscle glycogen levels (associated with a feeling of heavy legs and muscular fatigue) and reduced plasma glutamine levels (associated with immune dysfunction and susceptibility to infection) [1,2].

Fast recovery from this condition in both athletes and those exerting regular physical exercise requires rest periods and sometimes high doses of NSAIDs which, however, have undesired side effects [3]. The use of antioxidant vitamins for the management of endurance training has also shown controversial clinical outcomes as recently reported in targeted and controlled human studies [4,5].

Consequently, properly selected plant derivatives able to support a ‘healthy inflammatory condition’ can be a valid nutraceutical option provided they meet quality, standardization, safety, bioavailability, clinical tolerability and efficacy standards. Indena S.p.A. has used its long experience to establish a technology platform based on the phytosome approach which allows the production of orally bioavailable, highly standardized botanicals. The company has developed two new ingredients, turmeric phytosome (Meriva®) and Boswellia serrata phytosome (Casperome®), both of which demonstrate elevated oral bioavailability and clinically documented efficacy in several disorders characterized by low grade chronic inflammation, including those related to intense physical activity.

Turmeric phytosome, in particular, has shown a significant effect in modulating delayed onset muscle soreness (DOMS) due to eccentric muscle activity in healthy active volunteers [6]. In a randomized, placebo controlled, single-blind pilot trial, 20 healthy male volunteers were randomized to turmeric phytosome (1 g twice daily, equivalent to 200 mg curcumin) or placebo. Supplementation was started 48 hours before a downhill running test and was continued for 24 hours after the test (4 days in total). Results showed that subjects in the curcumin group reported less pain in the lower limbs and showed less evidence on magnetic resonance imaging of muscle injury in the posterior and medial compartments of both thighs. Markers of muscle damage and inflammation tended to be lower in the curcumin group, with a significant reduction in IL-8 at 2 hours.

In a second study, turmeric phytosome demonstrated ability to modulate cytokine and inflammatory markers following endurance cycling [7]. In this study, 11 male recreational athletes underwent three double-blind trials with turmeric phytosome, placebo and no supplementation while undertaking a cycling exercise set at a 95% lactate threshold. The results were consistent with above-normal scoring in the subjective assessment of psychological stress in the curcumin group. The study also showed modulation of inflammatory markers, although the sample size and other factors such as dosage (500 mg) precluded statistical significance being reached.
These two studies show that turmeric phytosome has a beneficial subjective and objective influence on exercise hang-over, attenuating the damage associated with intense physical activity. In addition, turmeric phytosome has no doping effects.

More recently, a second ingredient, Boswellia serrata phytosome (Casperome®) with marked oral bioavailability of its active ingredients (i.e., boswellic acids) has been developed. In young rugby players, it was effective and well tolerated as part of an integrated approach to manage osteo-muscular pain, which is the most common sports complaint, particularly in rugby players [8]. In this registry study, 52 healthy young rugby players with acute knee pain and inflammation individually chose to follow either standard management to control joint pain or standard management together with Boswellia serrata phytosome. Supplementation consisted of 500 mg/day for 5 days, followed by 250 mg/day for 23 days. The results showed a significant beneficial effect of Boswellia serrata phytosome on the following parameters: local pain, pain-free walking distance (treadmill test), joint effusion, structural damage, thermal imaging of the anterior knee and inflammatory biomarkers. These effects were accompanied by good clinical tolerability and absence of side effects.

Once again, the global results obtained with Meriva® and Casperome® demonstrate that rigorous standardization criteria, preclinical safety control and clinically tested oral bioavailability are very important factors in the clinical testing of nutraceuticals for consumer health including sports nutrition.

1. Kreher JB, Schwartz JB (2012) Overtraining syndrome: a practical guide. Sports Health 4(2):128–138
2. Margonis K, Fatouros JG, Jamurtas AZ et al (2007) Oxidative stress biomarkers responses to physical overtraining: implication for diagnosis. Free Radic Biol Med 43(6):901–910
3. Van WiJk K, Lenaerts K, Van Bijnen AA et al (2012) Aggravation of exercise-induced intestinal injury by ibuprofen in athletes. Med Sci Sports Exerc 44(12):2257–2262
4. Theodorou AA, Nikolaidis MG, Paschalis W et al (2011) No effect of antioxidant supplementation on muscle performance and blood redox status adaptations to eccentric training. Am J Clin Nutr 93:1373–1383
5. Paulsen G, Cumming KT, Holden G et al (2014) Vitamin C and E supplementation hampers cellular adaptation to endurance training in humans: a double-blind randomized, controlled trial. J Physiol 592:1887–1901
6. Drobnic F, Riera J, Appendino G et al (2014) Reduction of delayed onset muscle soreness by a novel curcumin delivery system (Meriva®): a randomized, placebo-controlled trial. J Int Soc Sports Nutr 11:31
7. Sciberras JN, Galloway SDR, Fenech A et al (2015) The effect of turmeric (Curcumin) supplementation on cytokine and inflammatory marker responses following 2 hours of endurance cycling. J Int Soc Sports Nutr 12:5
8. Franceschi F, Togni S, Belcaro G et al (2016) A novel lecithin based delivery form of Boswellia acids (Casperome®) for the management of osteo-muscular pain: a registry study in young rugby players.
Eur Rev Med Pharmacol Sci 19:4156–4161

by Cec Editore