|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|
Absorbs UVB and near-UVA wavelengths. Its SPF is proportional to its concentration in the range between 0-10%.
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Table of contents:
- 1. Sources
- 2. Skin penetration
- 3. Effects on the skin
- 4. Stability
- 5. Safety
Octocrylene is an oil-soluble sunscreen that absorbs in the UVB and near-UVA regions. First introduced in sun care and cosmetic products in the late 1990s, it has become increasingly popular over the years because of its ability to photostabilize the UVA filter avobenzone. A 2009 survey of topical sunscreen products in the United States found that 36% contained both avobenzone and octocrylene, up from 10% in 2003 and none in 1997.
In Switzerland, an investigation of 116 personal care products revealed that octocrylene was the third most popular UV filter, present in 43% of the products. A larger study in Germany that analyzed 4,477 cosmetic products found avobenzone to be present in 30.7% of the products, behind only octinoxate (38.5%), titanium dioxide (40.1%) and avobenzone (48.7%).
Octocrylene has also been detected in tap water samples from Spain, up to a concentration of 170 ng/L.
2. Skin penetration
Sunscreen agents should ideally penetrate only into the shallow layers of the skin so that the risk of adverse systemic reactions is minimized. Studies on human skin indicate that octocrylene can penetrate into the stratum corneum and the epidermis, but either cannot penetrate through the epidermis, or permits only a minuscule amount through the epidermis into the dermis. However, the total absorbed dose of octocrylene is increased in irradiated skin, though the reason for this is not clear.
Nanoencapsulation of octocrylene using the polymer poly(epsilon-caprolactone) (PCL) can increase its retention in the skin, thereby avoiding systemic absorption.
3. Effects on the skin
The UV absorption profile of octocrylene spans from 290 to 360 nm, covering the UVB and short UVA wavelengths. Its peak absorption has been variously reported to be at 303, 304 or 307 nm.
Octocrylene's sun protection factor (SPF) is directly proportional to its concentration, at least in the range between 0-10%. When compared against 17 other UV filters authorized in the EU by using the highest concentration allowed by European legislation for each filter, octocrylene was among the most efficacious, ahead of oxybenzone, octisalate and homosalate.
Octocrylene's photoprotection can be augmented by encapsulating it within solid nanoparticles, which act as physical sunscreens on their own and can provide a synergistic UV-blocking effect. Rice bran and raspberry seed oil-based lipid nanocarriers formulated into creams containing 3.5% of the UV filters avobenzone and octocrylene also led to improved photoprotection, reflecting up to 91% of UVA and 93% of UVB rays.
3.2 Prevention of photoaging
One study has evaluated whether the photoprotection afforded by a daily use cream containing octocrylene, avobenzone and Mexoryl SX can inhibit damage to the skin induced by daily exposure to UV radiation. The buttock skin of 12 volunteers was exposed 5 days per week for 6 weeks to one minimal erythema dose of solar simulated radiation per exposure, and both treated and untreated skin were assessed for erythema, pigmentation, skin hydration, skin microtopography, histology and immunochemistry, and collagen and metalloproteinase mRNA levels. The unprotected skin sites saw melanization as well as changes in skin hydration and microtopography. The thickness of the stratum corneum and stratum granulosum was increased, and in the dermis the expression of the extracellular matrix glycoprotein tenascin was enhanced, whereas the expression of type I pro-collagen was reduced. Moreover, types I and III collagen mRNA were also slightly increased, and there was a 2.8-fold enhancement of the mRNA level of matrix metalloproteinase-2 (MMP-2). These changes were all prevented by the daily use cream, indicating that daily photoprotection with octocrylene, avobenzone and ecamsule can significantly inhibit UV-induced skin damage.
3.3 Other effects and uses
Apart from its photoprotective effect, octocrylene also has anti-inflammatory properties. When a preparation containing 10% octocrylene (the highest concentration allowed in Europe) was subjected to the phorbol-myristate-acetate test using mice, 83% edema inhibition was observed. The effect was dose-dependent -- 0.5% octocrylene caused no inhibition, while at concentrations of 1.25%, 2.5% and 5% inhibitions of more than 20%, 50% and 70% were seen, respectively.
A sunscreen containing octocrylene, ecamsule, avobenzone and titanium dioxide has been found to be effective in preventing the development of UV-induced skin lesions in patients with photosensitive lupus erythematosus.
In a comparison with 17 other UV filters authorized in the European Union, octocrylene was not among the most photostable, but it is believed to be an efficient singlet quencher, which may account for why it can photostabilize a number of other sunscreen actives such as avobenzone, octinoxate and oxybenzone.
The photostability of octocrylene can be further improved by 6 to 8-fold upon forming inclusion complexes with hydroxypropyl-beta-cyclodextrin (HP-beta-CD) in lotion formulations.
Octocrylene is an approved sunscreen ingredient in both the United States and Europe, where it can be included up to a concentration of 10%. Its safety profile is considered excellent overall, with low irritation, phototoxicity, and photoallergic potential. It was also not subchronically toxic, developmentally toxic or genotoxic in animals, supporting its use as a human photoprotectant.
However, some researchers have recommended that octocrylene should be avoided in sunscreens for children and pregnant mothers, due to its propensity to cause contact dermatitis in the former and the fact that a significant correlation exists between the use of products containing octocrylene and its presence in human breast milk.
5.1 Enhanced production of reactive oxygen species
The absorption of octocrylene increases under irradiation. Unfortunately, this increases the chance of an enhancement in the level of reactive oxygen species (ROS) in the skin, which has been demonstrated to occur when octocrylene penetrates into the epidermis. The presence of antioxidants in the formulation can help prevent the damage caused by these ROS by deactivating free radicals.
5.2 Photocontact and contact allergy
Octocrylene is both a photocontact allergen and a contact allergen. Although allergic reactions to UV filters are uncommon, studies in Europe have reported increasing numbers of patients with photocontact allergy to octocrylene since 2003. In fact, there is evidence that octocrylene is now among the organic UV absorbers that most frequently elicit photoallergic contact dermatitis in Europe.
Similarly, there are many reports of photocontact or contact allergy to octocrylene in the literature. Octocrylene appears to be a strong contact allergen in children, which has led some researchers to suggest that it should probably be avoided in sunscreens for this age group.
Octocrylene's allergenic potency may be attributable to its photoinduced reactivity towards primary amines and alcohols, causing it to react with peptides or free amino acids of the human skin. In addition, it is known that many adult patients with photocontact allergy to octocrylene have previously used topical products containing ketoprofen, leading to the suggestion that photosensitization to ketoprofen leads to photocontact allergy to octocrylene.
5.3 Potential endocrine disruptor
Octocrylene has been shown to stimulate the proliferation of human breast cancer cells in vitro through what appears to be an estrogen receptor-mediated process. A more recent study found that it did not upregulate endocrine-related genes in an aquatic inverterbrate at any of the tested concentrations however.
5.4 No enhancement of pesticide absorption
Some sunscreen formulations have been demonstrated to enhance the dermal penetration of herbicides and pesticides. Additional studies revealed that certain sunscreen agents such as Padimate O, octinoxate, homosalate and octisalate can increase the total penetration of the herbicide 2,4-dichlorophenoxyacetic acid (2,4-D) to varying degrees. Octocrylene, however, had no effect or even slowed the lag time for the penetration of 2,4-D in two separate studies.
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