What is the Origin of Penetration Enhancers?

This pharmacological concept developed in pharmaceutical science and dermatological research to overcome the skin's inherent function as a protective barrier against external substances. The term is descriptive of their functional mechanism: they 'enhance' the 'penetration' of the active pharmaceutical ingredient.

What is the Mechanism of Penetration Enhancers?

These agents operate through various physicochemical pathways, often by disrupting the highly ordered lipid bilayers within the stratum corneum, making the intercellular pathways more fluid and permeable. Specific examples include solvents like ethanol, sulfoxides like DMSO, or various fatty acids, which temporarily alter the skin's structure. This transient modification allows lipophilic hormones like testosterone or estradiol to diffuse more readily across the epidermal layers and into the dermal microcirculation for systemic distribution.

Penetration Enhancers

Meaning

Penetration enhancers are chemical agents intentionally incorporated into topical or transdermal drug delivery formulations to reversibly decrease the barrier resistance of the stratum corneum, the outermost layer of the skin. Their clinical purpose is to increase the flux of a therapeutic compound, such as a steroid hormone, across the skin barrier and into the systemic circulation, thereby optimizing drug bioavailability. They are essential components in many transdermal hormone replacement therapies, ensuring predictable and effective dosing.