Iron Chelator Prodrug that Prevents Skin Damage from UV Radiation

Technology #15352

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Researchers
Nikki A. Thiele
Managed By
Anita Rao
Assistant Director 352-392-8929

Studies Suggest Prodrug Can Be Added to Topical Products for Preventing and Treating Skin Damage

When applied topically, this oxidative stress-activatable double prodrug chelates iron in the body, helping to prevent skin damage caused by ultraviolet (UV) radiation from the sun. Over time, UV radiation can stress the skin by triggering the release of free iron, which subsequently leads to the production of reactive oxygen species (ROS). At high levels, ROS can damage lipids, proteins, and DNA. Humans lack the ability to remove iron from the body, causing accelerations in aging processes. Researchers at the University of Florida have developed a pharmaceutical prodrug for an iron chelator, which upon activation can bind iron and make it chemically inert. This has the potential to reduce or prevent oxidative stress effects, such as wrinkling and skin cancers. Available skincare products, such as sunscreen, could easily integrate the technology.

Application

Double prodrug that is activated by serial hydrolysis and oxidation by ROS to chelate iron, thereby preventing, treating or reducing oxidative stress effects

Advantages

  • Passively permeates a silicone membrane, suggesting it may be added to sunscreen, anti-aging cosmetics, and other topical products to prevent or treat skin damage
  • Exhibits better membrane permeability and protection against oxidative stress than the parent drug
  • Hydrolysis of the double prodrug occurs chemically, improving on available prodrugs that rely on enzymatic hydrolysis or are unable to hydrolytically revert to the active drug
  • Full conversion into the active chelator occurs only in the presence of oxidative stress elements such as hydrogen peroxide, increasing targeting ability

Technology

This iron chelator double prodrug, after activation by chemical hydrolysis and hydrogen peroxide oxidation, reduces iron and free radical buildup on human skin caused by UV radiation. Since wrinkles and other skin damage are produced from high levels of iron and free radicals, a reduction in these elements through iron chelation leads to a reduction in damage. The double prodrug exhibits several advantages over its parent chelator and other derivatives: it has improved membrane permeability, can undergo nonenzymatic hydrolysis during its conversion to the active chelator, and is targeted to areas of high oxidative stress. Fewer cells died after exposure to hydrogen peroxide in the presence of this double prodrug than in the presence of the parent chelator, which is a strong chelator that lacks effective targeting abilities and sufficient membrane permeability. Our double prodrug derivatives can be incorporated into topical products to protect against harmful UV radiation.