Bioavailability and safety of tocotrienols (pharmacokinetics)

How much of orally taken tocotrienols reach the plasma and the organs, what amounts are free of side effects and safe? To date there are a number of studies.

At a glance: Tocotrienols taken orally are well absorbed, are safe for use at up to 3200 mg/day and produce bioactive concentrations (which have been found to be tumour-inhibiting in animal studies). The influence on blood lipids (cholesterol reduction) does not exist if the test subjects already have the same values.

1.study, deals specifically with delta-tocotrienol: [PMC4939900Pharmacokinetics and Safety of Vitamin E δ-tocotrienol after Single and Multiple Doses in Healthy Subjects with Measurement of Vitamin E Metabolites]

36 people received VEDT (Deltagold®, consisting predominantly of delta-tocotrienol) in doses of 100 to 3200 mg/day, once or twice daily. The maximum concentrations of 483 to 3746 ng/ml were reached within 4 to 9.3 hours. The half-life was between 1.7 and 6.9 degrees. Both the maximum concentration and the average concentration (area) reached a high maximum in a dose of 300 mg/day, which surprisingly decreased in 400 mg/d (only in a single dose), only to be exceeded by 800 and 1600 mg. In the group that received the T3 in two parts, a lower maximum concentration and a lower average concentration were found, which only significantly (five-fold) exceeded the single dose at 1600 mg/d [Table].

Blood lipids (cholesterol, HDL, LDL, TG) were not significantly affected in the healthy participants. This shows that the significant reduction in cholesterol found in several studies only occurs in elevated levels. Sent values ​​were not affected.

2.study  with TRF (palm tocotrienols) [PMID 17330512 Dose Dependent Elevation of Plasma tocotrienol Levels and Its Effect on Arterial Compliance, Plasma Total Antioxidant Status, and Lipid Profile in Healthy Humans Supplemented with tocotrienol Rich Vitamin E Tokyo 2006]

36 healthy men received 80, 160, 320 mg tocotrienol or placebo (randomized, endpoint-blind). The TRF used contained relatively high (26.2%) alpha-tocopherol. Result: after 2 months, the test subjects had significantly higher plasma concentrations depending on the dose (e.g. in 320 mg/d about 100 ng/ml d-T3, 280 ng/ml g-T3, 420 ng/ml a-T3). Alpha-tocopherol was only slightly increased. Blood lipids (cholesterol) and blood pressure were not affected in the healthy participants.

3.study  with TRF deals with the transport of the tocotrienolsn to the organs and has a positive influence on the liver [PMID 22298568 Oral tocotrienols Are Transported to Human Tissues and Delay the Progression of the Model for End-Stage Liver Disease Score in Patients]

80 people undergoing surgery received 400 mg of mixed tocotrienols or alpha-tocopherol. After 12 weeks, the tocotrienols increased significantly in blood, skin, adipose tissue, brain, heart muscle and liver. The concentration in the brain reached values ​​that were found to be neuroprotective in experimental models against stroke. In patients awaiting a liver transplant, the "MELD score" was improved in 50% of the tocotrienol patients, compared to over 20% of the patients in alpha-tocopherol. The T3 concentrations after 12 weeks were:
in the skin around the 2 nmol/g,
in Brain 2.57 nmol/g (predominantly a-T3)
in Heart 16.54 nmol/g (predominantly g-T3)
in fat 35.87 nmol/g
in the liver 1.24 nmol/g

Tocotrienols are effectively transported to vital organs of the body and accumulate there to effective concentrations.

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