Tocotrienol Supplements: Are They Really Safe for You?

Vitamin E tocotrienols supplements, linked to multiple health benefits, are often referred to as 'superfoods.' But are they actually safe to administer?

1922- the iconic discovery year of vitamin E. Herbert McLean Evans and Katharine Scott Bishop, two scientists from the University of California, Berkeley, discovered the biological function and chemical structure of tocopherols. It was quickly recognized for its antioxidant properties and its role in supporting heart health, immunity, and youthful skin.

However, the narrative shifted with the discovery of tocotrienols and their supplements, which emerged as a superior antioxidant. Let's explore the efficacy and safety guidelines of tocotrienol supplementation.

Wait, do you know the difference between the different forms of vitamin E?

The Story Behind Vitamin E Tocotrienols

Tocotrienols, a natural form of vitamin E, were first discovered in 1964 in a rubber plant. The prominent discovery drew the attention of scientists and researchers worldwide to explore the potential benefits of the other halves of tocopherols. Later, in the 1990s, the compound was further explored for its anticancer properties.

Then came the revolutionary breakthrough in 2002 by Dr. Barrie Tan, who identified annatto as a rich source of tocotrienols, free of tocopherols. His innovation, DeltaGold, an annatto-derived tocotrienol supplement, further strengthened the position of tocotrienols in the world of nutritional science.

Also Read, The Complete Guide to Vitamin E Tocotrienols

What Do Global Regulatory Authorities Say?

Currently, the World Health Organization (WHO) does not have any specific statements or guidelines about tocotrienol supplements. The Union Nation agency doesn't highlight anything about the safety standards or adverse effects of the tocotrienol supplements. On the other hand, the Food and Drug Administration (FDA) has evaluated the safety of tocotrienols.

The FDA has granted DeltaGold tocotrienol supplement GRAS (Generally Regarded as Safe) status. In simple words, the GRAS status means tocotrienols are safe for human consumption, as intended. Despite the endorsement, the lack of specific guidelines from the FDA underscores the need for further research and clinical studies to evaluate the long-term safety of tocotrienol supplementation.

Evaluating the Safety Standards of Tocotrienol Supplements

In modern times, tocotrienol supplements are a boon for cardiovascular health, strong bones, a healthy liver, skin vitality, improved metabolism, and more. The ideal dose of tocotrienols depends on the medical condition and purpose of the supplementation. However, with fame comes the criticism.

How safe are vitamin E tocotrienols for humans? Or are tocotrienol supplements safe for regular use?

Adverse Effects of Tocotrienols at Higher Dose

According to Dr. Barrie Tan, who has consumed tocotrienols more than anyone else on the planet, even 1000 mg of the compound per day won't do any harm to humans. The FDA or the WHO does not classify the exact dose of tocotrienols. However, a healthy adult can intake about 200-600mg of tocotrienols per day.

But what happens if, by any chance, someone takes a higher dose? In a rodent study, even 2,500 mg/kg of tocotrienol per day, based on body weight, did not show any significant toxicological effects. Clinical studies involving human participants have indicated that 1000 mg of tocotrienols per day is well-tolerated over extended periods.

How Safe Is δ-Tocotrienol Oral Dose in Humans

δ-Tocotrienol supplements, due to their unique structure and bioavailability, have shown effective potential as an anti-carcinogenic adjuvant and certain other health benefits. But is vitamin E δ-tocotrienol safe when taken orally?

According to studies, tocotrienol doses, when administered orally, range from 100 to 1600 mg, given to healthy adults once or twice a day for two consecutive weeks, with no drug-related adverse reactions. Instead, at safe levels, tocotrienol may support chemoprevention.

Read Out: How Much Tocotrienol Is Too Much? Understanding the Right Tocotrienol Dose

Is Tocotrienol Supplementation Safe for Postmenopausal Women

A woman's body undergoes hundreds of physical and hormonal changes postmenopause. Tocotrienols may help support bone density and hormonal balance in women with osteopenia, without affecting their quality of life.

A study found that postmenopausal osteopenic women who took 430 to 860 mg of annatto-derived, tocotrienol-rich extract daily for 12 weeks showed significant improvement. Even in higher doses, the liver and kidney parameters remained within normal ranges. The supplementation doesn't impact physical activity, body composition, nutrient intake, or drug alteration, indicating its safety levels.

Find In Detail: Why Postmenopausal Women Need Vitamin E Tocotrienols

Tocotrienols Safety for Topical Uses

As an antioxidant, tocotrienols are 40-60 times more potent than tocopherols. Thanks to its greater bioavailability and deeper cellular penetration, tocotrienol is also an active ingredient in skincare and cosmetics. They boost skin collagen and may help reverse or slow skin damage caused by free radicals.

According to the Cosmetic Ingredient Review (CIR) Expert Panel, tocotrienols are safe for use in cosmetic products. After considering critical factors such as potential toxicity, skin irritation, and sensitization, researchers found that tocotrienols have no adverse dermal effects. On the other hand, the topical application of tocotrienols has shown a significant reduction in skin irritation, serum histamine levels, and dermal thickening, highlighting their ability as a skin supplement.

Tocotrienol Safety With Cholesterol Reducing Drugs

In the early 1980s, Asaf Qureshi and Elson first reported the cholesterol-lowering properties of tocotrienols in the Journal of Medicinal Chemistry. However, there is still debate about its safety levels.

A placebo-controlled clinical study investigated the safety and efficacy of tocotrienols in patients with hyperlipidemia. Participants who received 200 mg of tocotrienols daily for 12 weeks reported no adverse effects. Unlike tocopherols, which do not react with LDL, tocotrienols may significantly reduce the level of low-density lipoprotein in the human body.

Observed Side Effects of Tocotrienols

The current researchers haven't found any notable side effects related to using tocotrienols. A severe allergic reaction to annatto-derived tocotrienols is rare. But, as they said, prevention is always better than a cure.

Some individuals might face rashes, itching, swelling, or dizziness. A minor part of the population also reported shortness of breath with tocotrienol supplementation. Thus, if you are considering tocotrienol supplements, consider your medical experts and take them in optimal amounts.

Tocotrienols and Drug Interactions

The above studies support the idea that tocotrienol supplements are safe for all individuals. However, the question now turns to the activity of tocotrienols with other drugs and medications. Do tocotrienol supplements have a synergic or antagonist effect when combined with other drugs or therapies?

Antagonist To Certain Drugs

Vitamin E tocotrienol, because of its unique structure, may interact with certain drugs, altering their mechanism and effects. In clinical studies, high doses of vitamin E supplementation have interacted with anticoagulant medications, such as aspirin and warfarin.

It also inhibits the mechanism associated with tamoxifen and cyclosporine. However, the good news here is that even in patients taking other medications, the ideal to medium dose (less than 300 mg/day) of the supplement appears safe, resulting in no significant adverse drug interactions.

Synergistic to Chemotherapeutic Agents

Tocotrienol supplements have potential anticancer therapies. Preclinical studies suggest that tocotrienols complement certain standard anticancer approaches by supporting oxidative balance and cellular function. With proper research and trials, tocotrienols may become a valuable adjunct in the future.

Find Out More: Understanding Possible Early Warning Signs of Cancer: What to Look Out For

What is the exact mechanism behind this? It may be because tocotrienols reduce cellular oxidative stress, which in turn influences cell signaling pathways and gene expression. However, further clinical studies are necessary to confirm these benefits and establish safe and effective dosages.

Final Takeaway

Tocotrienols, indeed a potent antioxidant, also have promising health benefits. With no or minimal risk factors associated, they can be considered safe for most of the population. After medical consultation, you can add tocotrienol supplementation alongside your medication to maximize the biological results. However, one thing you must acknowledge is that tocotrienol supplements aren't a replacement for standard medical care.

Disclaimer: These statements have not been assessed or evaluated by the Food and Drug Administration. The supplements listed above are not intended to diagnose, treat, cure, or prevent any disease. The findings are solely based on preliminary research and ongoing studies. Individual results after trying these health tips and measures may vary.

Key Takeaway

• Tocotrienols, a form of vitamin E, are more potent antioxidants compared to tocopherols.

• DeltaGold tocotrienol supplementation is GRAS-approved (Generally Recognized as Safe) according to FDA standards.

• Safe daily doses of tocotrienols range from 200 to 600 mg, with clinical studies showing that doses of up to 1,000 mg per day are well tolerated.

• The ideal safe dose of tocotrienols depends on the individual's medical and personal factors.

• While tocotrienols are generally safe, some individuals may experience mild side effects such as skin irritation or dizziness.

Disclaimer: This content is for informational purposes only and is not intended as medical advice. These statements have not been evaluated by the FDA. Products mentioned are not intended to diagnose, treat, cure, or prevent any disease.

Sources Used:

1. Fiume, M. M., Bergfeld, W. F., Belsito, D. V., et al. (2018). Safety Assessment of Tocopherols and Tocotrienols as Used in Cosmetics. September–October 2018. Available: https://journals.sagepub.com/doi/abs/10.1177/1091581818794455

2. Fiume, M. M., et al. (2018). Safety Assessment of Tocopherols and Tocotrienols as Used in Cosmetics. September–October 2018. Available: https://journals.sagepub.com/doi/abs/10.1177/1091581818794455

3. Shen, C.-L., et al. (2018). A 12-week evaluation of annatto tocotrienol supplementation for postmenopausal women: Safety, quality of life, body composition, physical activity, and nutrient intake. June 28, 2018. Available: https://bmccomplementmedtherapies.biomedcentral.com/articles/10.1186/s12906-018-2263-0

4. Eitsuka, T., et al. (2016). Synergistic anticancer effect of tocotrienol combined with chemotherapeutic agents or dietary components: A review. September 22, 2016. Available: https://www.mdpi.com/1422-0067/17/10/1605