Anti-Inflammatory Product Formulation

While glucosamine and chondroitin are likely the first nutritional ingredients that come to mind when discussing “inflammation,” this is really primarily focused in the joint category. In actuality, the inflammatory response can occur anywhere in the body. Acute or chronic inflammation may occur in different parts or organs of the body, including the brain, heart, lungs, eyes, nasal passages, gastrointestinal tract, throat, reproductive organs, urinary tract, joints, bones, blood vessels and other regions. Inflammation is associated with cardiovascular disease, obesity and other health disorders.

Inflammation is a normal, important function whereby the body removes damaged cells, eliminates microorganisms and helps repair damaged tissue. When the body doesn’t heal itself properly, a self-perpetuating inflammatory process occurs. The body responds to inflammation due to tissue injury, irritation, infection and invasion of a virus, chemicals, heat or trauma, and from wear and tear disorders. Inflammatory symptoms that may occur are stiffness, redness, pain, heat, swelling, tenderness, fatigue, muscle aches, spasms and loss of function.

Although consumers with inflammation may be on a therapeutic regimen from a health care provider, they may have an interest in nutritional support as well. Product developers should think outside the box, review the science and find data on the particular body systems that may be under inflammatory attack. Many ingredients help reduce pain, swelling and other symptoms of inflammation. This provides a unique edge to a combination formulation, since body systems under stress usually experience an inflammatory response.

There are several steps a formulator would take in augmenting a product with ingredients to address the inflammatory response. First, it is critical to understand the physiology and mechanisms of inflammation. Next, select the body system/organ of interest and determine what nutrients have been shown to exert beneficial effects against unwanted inflammation in that area. Then determine what supportive ingredients might be appropriate, as well as the safety profile of the combination formula.

Formulation Opportunities

Two areas that offer opportunity for incorporating inflammatory support ingredients into broader product formulations are weight management and heart health products. In weight management, for example, it has been shown that inflammation is associated with obesity. Fat cells secrete various inflammatory mediators such as prostaglandin E2 (PGE2), plasminogen activator inhibitor-1, IL-1, IL-6, IL-8, the pro-inflammatory cytokine tumor necrosis factor-alpha (TNF-alpha) and others. Additionally, activated immune cells produce cytokines. It has been shown the amount of these inflammatory substances within fat tissue significantly raises concentration levels in the body.

Curcumin, an Indian spice, and resveratrol found in grape skin have been shown to inhibit nuclear factor kappa-beta mediated cytokines in fat cells. These would be great to add to a specialized weight management formula to help protect against inflammation.

Formulations for cardiovascular or respiratory health often incorporate Ginkgo biloba for its ability to improve circulatory function; it also supports the inflammatory response process. Platelet aggregation occurs during inflammation and is stimulated by platelet activating factor (PAF). During inflammation of the bronchioles, PAF promotes the activation of bronchiole vasoconstriction. Ginkgo biloba’s terpenes and other natural compounds help inhibit PAF.

When addressing circulatory health, formulators may also look at supporting the integrity of the blood vessels, which become permeable and porous during the inflammatory response. This allows proteins and other substances into the inflamed tissue; the tissue enrobes the foreign compound(s) with a specialized coat of fibrin, causing swelling. Nutrients such as proteolytic enzymes have been shown to help break fibrin. Proteolytic enzymes used to support the inflammatory response should be taken on an empty stomach so that they are not utilized during the digestive process to digest protein.

A formulator could also consider the use of different bioflavonoids to help promote healing during inflammation. Quercetin contains effective bioflavonoids to support the inflammatory process. It has been shown to help increase capillary permeability, which would decrease swelling during inflammation. It helps to allow fluid to leave from the inflamed tissue; it also inhibits Ca2+-dependent ATPase and cyclic AMP phosphodiesterase, which cause histamine to be released from mast cells and basophils.

Gastritis is one type of inflammation of the stomach lining. Gamma oryzanol is one particular nutrient with clinical support in this area. Clinical trials using 300 mg/d show significant (23 percent) improvement after just two weeks. As with all nutrients in the inflammation category, product labels should encourage consumers to discuss the use of the formula with their health care provider. Amino acids such as L-cysteine and L-glutamine could be good additions to a GI support formula.

Other ingredients with broader effects in addition to their efficacy in the inflammatory realm include antioxidants such as vitamins C and E, coenzyme Q10 (CoQ10), green tea, hawthorn, grape seed, bilberry and pine bark extract, which diminish the free radical damage associated with inflammation; and the omega-3 fatty acids, which help balance eicosanoids. Additionally, willow bark is an effective natural anti-inflammatory and pain reliever; however, it may not be cost effective in a nutritional formula.

Finally, while there are many ways to create formulations to support the inflammatory response, it is important to keep in mind FDA does not approve the word inflammation in marketing copy. Therefore, it is wise to seek legal counsel before making any structure/function claims.

Judi Quilici-Timmcke, Ph.D., is president of Q-Tech Services Inc. (JudiQ.com) and a product formulation specialist. She worked previously in product development positions at Weider and Rexall Showcase.