|Grade||Level of Evidence|
|A||Multiple double-blind, controlled clinical trials.|
|B||1 double-blind, controlled clinical trial.|
|C||At least 1 controlled or comparative clinical trial.|
|D||Uncontrolled, observational, animal or in-vitro studies only.|
|Grade||Effect||Size of Effect||Comments|
Scavenges free radicals and helps terminate radical chain reactions.
Absorbs UV light and inhibits UV-induced skin damage such as erythema, collagen degradation, abnormal accumulation of elastic fibers and epidermal hyperplasma.
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Table of contents:
Ferulic acid is the most abundant hydroxycinnamic acid in the plant world. It is bound to the hemicellulose chains of unlignified primary cell walls through ester linkages, and is also polymerized with lignin, a component of the secondary cell wall, through ether bonds.
2.1 Oral administration
The bioavailability of dietary ferulic acid varies widely and is governed by the food matrix. Ferulic acid in cereals is bound to arabinoxylans and lignin, restricting its release in the small intestine. After intestinal absorption, ferulic acid appears in the plasma mainly as its sulfoconjugates, and is excreted in the urine.
2.2 Topical administration
The use of ferulic acid in cosmetics is hindered by its pH- and temperature-related instabilities. pH also impacts the permeation of ferulic acid, with faster permeation observed for a solution / gel of ferulic acid at pH 6 compared to at pH 7.4. This is thought to be due to the carboxylic moiety, which is believed to be more in the ionized form at pH 7.4 than at pH 6. The non-ionized form is beneficial to skin partitioning because of its lipophilicity.
To improve the physicochemical stability of ferulic acid in formulations, attempts have been made to protect it from decomposition using controlled release technologies. For instance, ferulic acid chemically incorporated into a polymer backbone protects it from premature degradation without compromising its antioxidant and antibacterial activities. In addition, the inclusion of ferulic acid with α-cyclodextrin not only improves its photostability but also slows its delivery, increasing its bioavailability in the skin.
Ferulic acid has been shown to penetrate the skin up to a depth of at least 500 μm when incorporated in oil-in-water emulsions or gels. The penetration enhancer oleic acid as well as various vesicular liposomal systems can improve permeation and skin deposition. 
The transdermal penetration level of ferulic acid is relatively low; more ferulic acid is retained in the skin rather than penetrating through it. Transdermal absorption is further retarded by entrapping ferulic acid within niosomes. However, a transdermal hydrogel patch is under development.
3. Effects on the skin
3.1 Antioxidant effect
Ferulic acid is a potent antioxidant -- in one study, it was found to be more effective than α-tocopherol (vitamin E), β-carotene, and ascorbic acid (vitamin C). It has the ability to inhibit lipid peroxidation and to scavenge reactive oxygen species and free radicals such as hydroxyl radicals, hypochlorous acid, peroxyl radicals and DPPH radicals.
Ferulic acid has distinctive structural motifs that may contribute to its free radical scavenging capability. The carboxylic acid group with an adjacent unsaturated C-C double bond not only provides attack sites for free radicals, preventing them from attacking the membrane, but also acts as an anchor for the molecule, binding it to the lipid bilayer and thus providing some protection against lipid peroxidation. In addition, any reactive radical colliding with ferulic acid easily abstracts a hydrogen atom to form a highly resonance-stabilized phenoxy radical that is unable to initiate or propagate a radical chain reaction.
Ferulic acid absorbs UV radiation with an absorption maximum at 307 nm, which theoretically can result in a sunscreen effect. Also, by scavenging free radicals and suppressing radiation-induced oxidative reactions, ferulic acid may help preserve the physiological integrity of cells exposed to air and impinging UV radiation. Indeed, ferulic acid dissolved in a saturated aqueous solution has been shown to afford significant protection to human skin against UVB-induced erythema, an indicator of UV-induced skin damage.
Ferulic acid also attenuates the UV-induced degradation of collagen fibers by inhibiting the activities of matrix metalloproteinase-1, 2 and 9. In mouse skin, it also suppressed the abnormal accumulation of elastic fibers and epidermal hyperplasia induced by UVB irradiation.
In practice, ferulic acid is often combined with vitamin C and vitamin E as this combination provides synergistic photoprotection of the skin. One such commercially available solution containing 15% ascorbic acid (vitamin C), 1% vitamin E and 0.5% ferulic acid (SkinCeuticals C E Ferulic) has been tested in several studies and has been shown to reduce erythema, the formation of thymine dimers and sunburn cells, and to inhibit the development of malignant skin tumours induced by chronic UV exposure. It has also been found to provide more effective photoprotection than 3 other commercial creams containing 0.1% kinetin (Kinerase), 1% idebenone (Prevage) or 0.5% idebenone (TRUE Youth Revealing Complex).
Another combination that has been tested is vitamin C, ferulic acid and phloretin, which attenuates UV-induced immunosuppression, sunburn cell formation, thymine dimer formation, matrix metalloproteinase-9 expression, and p53 protein expression.
3.3 Age-related improvements
Ferulic acid, γ-oryzanol and phytic acid from rice bran extracts are known to hydrate, lighten, smoothen and thicken the skin as well as increase its elasticity when entrapped in niosomes and incorporated in gel or cream formulations, but it is not clear which of the active ingredients are responsible for these effects.
4. Side Effects
Topical application of ferulic acid for up to 24h did not cause skin irritation as measured by transepidermal water loss, erythema and skin pH value in a safety study. Moreover, ferulic acid does not penetrate well through the skin, indicating a lower systemic risk.
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