The benefits of micronutrients for human health are widely known and supported by a constantly growing pool of scientific research. However, emerging data suggests that vitamins in higher doses can also offer benefits far beyond the currently recognised nutritional range
Understanding the role of vitamins in the pharmaceutical industry has the potential to lead to the creation of groundbreaking, safe and high quality products to improve the health of individuals worldwide.
Nutrient inadequacies across the globe Modern lifestyles may lead to suboptimal micronutrient intake and status.
A study reviewed vitamin intakes in a number of developed countries and discovered that consumption levels are below recommendations in many populations.1
The variation between the countries is likely because of the differences in regulatory guidelines, levels of fortification and local dietary habits.The impact of low micronutrient intake is a serious public health concern, resulting in vulnerability to several diseases. Nutrient inadequacies or deficiencies are particularly prevalent under clinical conditions, with vulnerable populations such as ill or elderly patients, and patients recovering in hospitals or care facilities, far more likely to have a low vitamin intake and status. In Europe, 5% of the entire population is affected by, or at risk of, malnutrition, but this number increases dramatically to 60% of people in care homes.2 Nutrition inadequacies in such groups can lead to an increased risk of infection and, therefore, a longer time spent in clinical care.
With careful consideration, pharma-grade vitamins, carotenoids and lipids can also be used as active pharmaceutical ingredients (APIs) to support the development of customised solutions for specific applications. For example, vitamin E is one micronutrient with a wide range of additional benefits for a variety of at-risk groups. A study into vitamin E and cardiovascular disease (CVD) showed that vitamin E supplementation at a dose of 400 mg (100 x the recommended intake for a healthy adult male in the UK) reduces the risk of cardiovascular events in diabetics with haptoglobin genotype 2-2 (Hp 2-2).3,4
As diabetic individuals with Hp 2-2 have considerably increased oxidative stress, and are also more likely to suffer from a cardiovascular event, these results offer an important opportunity to greatly improve the lives of many. Additionally, vitamin E at a dose of 400–800 mg has also been shown to reduce the risk of non-alcoholic fatty liver disease, an increasingly prevalent issue in adults and children worldwide.5 There is also scientific data to support the role of high-dose vitamin E in improving cognitive health and burns.6,7
An area in which micronutrients and macronutrients in higher doses may prove particularly effective is in supporting cardiovascular health. CVD has been the leading cause of death worldwide for the last 15 years, responsible for approximately 31% of deaths.8,9 Research suggests that the increased intake of eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) can offer benefits for CVD patients.
A systematic review and meta-analysis combined evidence from 10 randomised controlled trials to conclude that n-3 polyunsaturated fatty acid (PUFA) intake significantly reduced serum triglyceride levels by 0.78 mmol/L, lowering the risk of cardiovascular event.10
Vitamin B2 has also been linked to cardiovascular health benefits in certain at-risk groups. A study discovered vitamin B2 intervention reduced mean blood pressure in individuals with the TT genotype.11 The findings indicated that genetically susceptible individuals would need to lose 10 kilos of weight to receive the same blood pressure lowering benefits available through vitamin B2 supplementation, even in the recommended daily allowance (RDA) range. The results of this study have important implications for the prevention and treatment of hypertension, as the TT genotype is particularly prevalent in many countries.
Other health issues that vitamins in higher doses have been shown to have a positive impact on include the common cold, multiple sclerosis and even cancer.12,13
From the vast array of clinical data available, it is clear that vitamins — as well as EPA and DHA in higher doses — can help to achieve a healthier population. This research, alongside an in-depth understanding of drug-nutrient interactions, must be used to define how vitamins and EPA and DHA should be used within the pharmaceutical industry.
Examples of when drug-nutrient interactions occur include statins, contraceptives, proton pump inhibitors and cases wherein vitamins have a synergistic effect with drugs. This can lead to the raising or lowering of the bioavailability of a nutrient induced by drug intake, meaning the desired results may not be achieved. For example, nutrients and certain food items can lead to an induction or inhibition of enzymes in the gut, potentially causing a change in the oral bioavailability of drugs.
As a case in point, grapefruit juice acts as a selective intestinal CPY3A4 inhibitor, which means the exposure of some drugs can be increased more than fivefold and, therefore, increase the risk of adverse effects.
Comprehensive research on the effects of combining pharmaceuticals with supplements is key to allowing manufacturers to understand how to develop safe, bespoke treatments for patients. Grading of Recommendations Assessment, Development and Evaluation (GRADE) is a method for assessing the quality of evidence for the use of specific vitamins in pharmaceutical applications, which can be used as a reference. Certifications of suitability (CEPs) and US Drug Master Files (DMFs) for essential micronutrients are also necessary measures to ensure that high-quality products are developed safely to support specific claims.
The wealth of scientific research available signals a promising era for vitamins, EPA and DHA in pharmaceutical applications. The essential role of vitamins in health has been well-known for a number of decades, but the knowledge of their importance beyond essentiality opens a range of opportunities in the pharmaceutical and healthcare industries. Further detailed investigations into drug-nutrient interactions are needed to ensure safe treatment.